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25 results on '"W. Piotrowski"'

1. RASS‐Enabled S/P−C and S−N Bond Formation for DEL Synthesis

Author

Dillon T. Flood, Xuejing Zhang, Xiang Fu, Zhenxiang Zhao, Shota Asai, Brittany B. Sanchez, Emily J. Sturgell, Julien C. Vantourout, Paul Richardson, Mark E. Flanagan, David W. Piotrowski, Dominik K. Kölmel, Jinqiao Wan, Mei‐Hsuan Tsai, Jason S. Chen, Phil S. Baran, and Philip E. Dawson

Subjects
General Medicine
Published
2020

2. Self‐Referenced Temperature Imaging with Dual Light Emitting Diode Excitation and Single‐Band Emission of AVO 4 :Eu 3+ (A=Y, La, Lu, Gd) Nanophosphors

Author

Artur Bednarkiewicz, W. Piotrowski, Benoit Fond, Linda Dalipi, Lukasz Marciniak, and Karolina Elzbieciak-Piecka

Subjects
Materials science, business.industry, chemistry.chemical_element, General Medicine, Single band, Dual (category theory), law.invention, chemistry, law, Optoelectronics, Europium, business, Excitation, Light-emitting diode
Published
2021

3. Liver-Targeted Small-Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis

Author

Dennis O. Scott, Spiros Liras, Roger B. Ruggeri, Heather Eng, Adam S. Kamlet, Ryosuke Arakawa, David W. Piotrowski, Robert Dullea, Christopher T. Salatto, Karen Atkinson, Michael W. Bolt, Anne-Marie R. Dechert-Schmitt, Paul DaSilva-Jardine, Allyn T. Londregan, Brian Raymer, Kenneth Dahl, Daniel P. Canterbury, Donna N. Petersen, Paula M. Loria, Chris Limberakis, Emi Kimoto, Kim F. McClure, Kevin Beaumont, Liuqing Wei, Akihiro Takano, Kevin P. Maresca, Jun Xiao, Amanda King-Ahmad, Christer Halldin, Benjamin Reidich, and Jeffrey R. Chabot

Subjects
0301 basic medicine, Drug, media_common.quotation_subject, Ribosome, Catalysis, Small Molecule Libraries, Structure-Activity Relationship, 03 medical and health sciences, 0302 clinical medicine, Humans, media_common, Dose-Response Relationship, Drug, Molecular Structure, Chemistry, PCSK9, PCSK9 Inhibitors, Subtilisin, General Medicine, General Chemistry, Prodrug, Proprotein convertase, Small molecule, 030104 developmental biology, Liver, Biochemistry, 030220 oncology & carcinogenesis, Hepatocytes, Kexin, Proprotein Convertase 9
Abstract

Targeting of the human ribosome is an unprecedented therapeutic modality with a genome-wide selectivity challenge. A liver-targeted drug candidate is described that inhibits ribosomal synthesis of PCSK9, a lipid regulator considered undruggable by small molecules. Key to the concept was the identification of pharmacologically active zwitterions designed to be retained in the liver. Oral delivery of the poorly permeable zwitterions was achieved by prodrugs susceptible to cleavage by carboxylesterase 1. The synthesis of select tetrazole prodrugs was crucial. A cell-free in vitro translation assay containing human cell lysate and purified target mRNA fused to a reporter was used to identify active zwitterions. In vivo PCSK9 lowering by oral dosing of the candidate prodrug and quantification of the drug fraction delivered to the liver utilizing an oral positron emission tomography 18F-isotopologue validated our liver-targeting approach.

Published
2017

5. ChemInform Abstract: Regio- and Enantioselective Synthesis of Azole Hemiaminal Esters by Lewis Base Catalyzed Dynamic Kinetic Resolution

Author

Liuqing Wei, Jun Xiao, David W. Piotrowski, Jiangli Yan, Anne-Marie R. Dechert-Schmitt, Mark T. Barrila, Thomas A. Brandt, and Adam S. Kamlet

Subjects
chemistry.chemical_compound, chemistry, Enantioselective synthesis, Hemiaminal, Regioselectivity, Tetrazole, General Medicine, Lewis acids and bases, Enantiomeric excess, Combinatorial chemistry, Adduct, Kinetic resolution
Abstract

We report a modular three-component dynamic kinetic resolution (DKR) that affords enantiomerically enriched hemiaminal esters derived from azoles and aldehydes. The novel and scalable reaction can be used to synthesize valuable substituted azoles in a regioselective manner by capping (e.g., acylation) of the equilibrating azole-aldehyde adduct. With the use of a prolinol-derived DMAP catalyst as the chiral Lewis base, the products can be obtained in high chemical yield and with high enantiomeric excess. The DKR was performed on a multikilogram scale to produce a tetrazole prodrug fragment for a leading clinical candidate that posed formidable synthesis challenges.

Published
2016

6. The method of the likelihood and the Fisher information in the construction of physical models

Author

S. Zaja̧c, Jan Sładkowski, Jacek Syska, and Edward W. Piotrowski

Subjects
Information transfer, Computer science, Probability and statistics, Condensed Matter Physics, Electronic, Optical and Magnetic Materials, Extreme physical information, symbols.namesake, Quantum game theory, Master equation, symbols, Entropy (information theory), Applied mathematics, Fisher information, Likelihood function
Abstract

The subjects of the paper are the likelihood method (LM) and the expected Fisher information (FI) considered from the point od view of the construction of the physical models which originate in the statistical description of phenomena. The master equation case and structural information principle are derived. Then, the phenomenological description of the information transfer is presented. The extreme physical information (EPI) method is reviewed. As if marginal, the statistical inter-pretation of the amplitude of the system is given. The formalism developed in this paper would be also applied in quantum information processing and quantum game theory.

Published
2009

8. ChemInform Abstract: Enantioselective Synthesis of 1,2,4-Triazolines Catalyzed by a Cinchona Alkaloid-Derived Organocatalyst

Author

David W. Piotrowski, Meihua Tu, Qian Shao, Jiean Chen, and Yong Huang

Subjects
biology, Chemistry, Organocatalysis, Alkaloid, Triazole derivatives, Enantioselective synthesis, Cinchona, Organic chemistry, General Medicine, biology.organism_classification, Catalysis
Abstract

A highly enantioselective protocol for the synthesis of polysubstituted 1,2,4-triazolines (IV), that is complementary to existing protocols, from azlactones (I) and azodicarboxylates (II) using a chiral organocatalyst is reported.

Published
2014

9. ChemInform Abstract: Regioselective Hydroarylations and Parallel Kinetic Resolution of Vince Lactam

Author

Adam S. Kamlet, Cathy Préville, David W. Piotrowski, and Kathleen A. Farley

Subjects
chemistry.chemical_compound, Chemistry, Stereochemistry, Ligand, Amide, Lactam, Substituent, Regioselectivity, General Medicine, Enantiomer, Vince lactam, Kinetic resolution
Abstract

Two regioselective and complementary hydroarylation reactions of an unsymmetrical cyclic olefin have been developed. The products can be transformed in one step into constrained γ-amino acids. Regioselective arylation of Vince lactam is controlled by the choice of phosphine ligand enantiomer and the substituent on the amide nitrogen atom. The method was extended to a general regiodivergent parallel kinetic resolution of the racemic lactam.

Published
2014

10. The discovery of indoxacarb: oxadiazines as a new class of pyrazoline-type insecticides

Author

Kevin C. Lee, David W. Piotrowski, Stephen Frederick Mccann, William Eldo Barnette, George Philip Lahm, Sandra M. Griswold, Rafael Shapiro, Paula Louise Sharpe, Patrick D. Lowder, Robert W. March, Margaret M. Hughes, Brian J. Myers, Bonita M. Reeves, Keith Dumont Wing, Jeffery K. Long, and Gary David Annis

Subjects
Low toxicity, Indoxacarb, Stereochemistry, Enantioselective synthesis, Pyrazoline, General Medicine, Chemical synthesis, chemistry.chemical_compound, chemistry, Biochemistry, Insect Science, Moiety, High activity, Enantiomer, Agronomy and Crop Science
Abstract

The evolution of the insecticidal pyrazoline moiety that was originally discovered in 1972 has led to the discovery of a new crop insecticide, indoxacarb, which is the first commercialized pyrazoline-type sodium-channel blocker. Both monocyclic and fused-tricyclic pyrazolines and pyridazines, as well as structurally related semicarbazones were examined prior to the discovery of analogous tricyclic oxadiazines which had similarly high activity as well as favorable environmental dissipation rates and low toxicity to non-target organisms. The eventual leading candidate, DPX-JW062, was originally obtained as a racemic molecule, but a chiral synthesis was developed which produces material that is 50% ee in the insecticidal (+)-S-enantiomer (DPX-MP062, indoxacarb).

Published
2001

11. ChemInform Abstract: Stereodefined Cyclopentanes by Hydroarylation-Ring Opening

Author

David W. Piotrowski and Jana Polivkova

Subjects
Addition reaction, Cyclopentanes, Nucleophile, Chemistry, Organic chemistry, General Medicine, Ring (chemistry)
Abstract

Title compounds are synthesized by ring opening of protected lactams [(IV) and (V), resp.], which are derived from hydroarylation of (I), using a variety of nucleophiles.

Published
2013

12. ChemInform Abstract: Substituted Azabicyclo[2.2.1]heptanes via Nitrenium Ion Rearrangement

Author

David W. Piotrowski, Marianne Rolph, and Liuqing Wei

Subjects
Bicyclic molecule, Chemistry, polycyclic compounds, Halogenation, Organic chemistry, Nitrenium ion, General Medicine
Abstract

N-Chlorination of exo-arylated bicyclic substrates and subsequent AgNO3-mediated nitrenium ion rearrangement produces endo-arylated products, which represent the skeleton of pharmaceutically important alkaloid systems.

Published
2012

13. ChemInform Abstract: Oxazole Activation for Azomethine Ylide Trapping: Singly and Doubly Tethered Substrates

Author

David W. Piotrowski and Edwin Vedejs

Subjects
chemistry.chemical_compound, Dipole, chemistry, Bicyclic molecule, Intermolecular force, Azomethine ylide, General Medicine, Trapping, Alkylation, Ring (chemistry), Photochemistry, Oxazole
Abstract

Bicyclic oxazolium salts 18, 24, 37, and 44 can be generated from tethered haloalkyloxazoles by internal alkylation. Reductive alkylation of the oxazolium salts using CsF/PhSiH 3 converts the salts initially into the corresponding 4-oxazoline derivatives. Subsequent electrocyclic ring opening generates stabilized azomethine ylides that can be trapped by suitable dipolarophiles. Intermolecular dipole trapping followed by DDQ oxidation affords the ring-fused pyrroles 22 and 26

Published
2010

16. ChemInform Abstract: Oxazolium-Derived Azomethine Ylides. External Oxazole Activation and Internal Dipole Trapping in the Synthesis of an Aziridinomitosene

Author

Fabio C. Tucci, David W. Piotrowski, and Edwin Vedejs

Subjects
chemistry.chemical_compound, chemistry, Nucleophile, Azomethine ylide, Organic chemistry, General Medicine, Oxazoline, Aziridine, Alkylation, Medicinal chemistry, Derivative (chemistry), Cycloaddition, Oxazole
Abstract

Intermolecular alkylation of the aziridinyl oxazole 20 using PhSO(2)CH(2)CH(2)OTf is possible despite the presence of potentially nucleophilic aziridine nitrogen. The resulting oxazolium salt 22 reacts with BnNMe(3)(+)CN(-) to produce the azomethine ylide 24b via electrocyclic ring opening of an oxazoline 23b. Internal cycloaddition affords 26 in 66% yield. After saponification and base-induced cleavage of the N-phenylsulfonylethyl group, conventional cyclization provides access to 33. Deprotection and DDQ oxidation completes the synthesis of the aziridinomitosene derivative 9b. The starting cis-disubstituted aziridine ester 16 can be prepared by the aza-Darzens reaction of 15 with tert-butyl chloroacetate.

Published
2000

18. The Statistical Analysis for Incomplete Diallel Cross Series. Fixed Model Analysis of Variance

Author

W. Mǎdry, L. Ubysz‐Borucka, and W. Piotrowski

Subjects
Statistics and Probability, Estimation, Series (mathematics), Winter wheat, General Medicine, Quantitative genetics, Diallel cross, Statistics, Econometrics, Statistical analysis, Analysis of variance, Statistics, Probability and Uncertainty, Vector space, Mathematics
Abstract

This paper presents modern statistical methods used for quantitative genetics and plant breeding. It contains biometrioal analysis principles of fixed model for an identical, incomplete diallel cross series. The theory of vector space is used for estimation of parameters assumed in the model and for performance of the analysis of variance. As a result, the estimation of all groups of parameters treated in the model, is independent. Theoretical results are illustrated by numerical examples from winter wheat breeding.

Published
1985

19. INTERACTION OF NEUROTENSIN WITH THE SUBSTANCE P RECEPTOR MEDIATING HISTAMINE RELEASE FROM RAT MAST CELLS AND THE FLARE IN HUMAN SKIN

Author

John C. Foreman, W. Piotrowski, and C.C. Jordan

Subjects
Adult, Male, medicine.medical_specialty, Physalaemin, Receptors, Cell Surface, Vascular permeability, Substance P, Human skin, Pharmacology, Histamine Release, Substance-P Receptor, Capillary Permeability, chemistry.chemical_compound, Internal medicine, medicine, Animals, Humans, Drug Interactions, Mast Cells, Receptor, Neurotensin, Skin, Dose-Response Relationship, Drug, digestive, oral, and skin physiology, Receptors, Neurokinin-1, Rats, Endocrinology, chemistry, Female, Peptides, Histamine, Research Article
Abstract

1 Substance P induced histamine release from rat peritoneal mast cells in a dose-dependent manner over the concentration range 1 to 10 microM. 2 At concentrations in the range 2.5 to 1 0 microM, neurotensin produced only about 5% release of histamine, which was substantially less than the maximum effect obtained with substance P. 3 Neurotensin, 2.5 to 10 microM produced graded inhibition of histamine release induced by substance P. The inhibitory effect of neurotensin was not seen when histamine release was induced by an antigen-antibody effect of neurotensin was not seen when histamine release was induced by an antigen-antibody reaction or by the ionophore, A 23187. Some evidence was obtained to suggest that compound 48/80 may interact with the same receptor as substance P and neurotensin. 4 [D-Arg8]neurotensin, [D-Arg9]neurotensin, xenopsin and the C-terminal octapeptide of substance P (SP4-11) all inhibited histamine release by substance P, but physalaemin did not. 5 Neurotensin inhibited the wheal and flare reactions induced by substance P in human skin. 6 [D-Trp7,9]substance P released histamine from rat mast cells and was about 12 times more potent than substance P itself. [D-Trp7,9]SP1-11 also produced wheal and flare responses in human skin, being 1.8 times more potent than substance P in the production of flare.

Published
1982

21. Baseline characteristics of patients in the Reduction of Events with Darbepoetin alfa in Heart Failure trial (RED-HF)

Author

McMurray, J.J.V., Anand, I. S., Diaz, R., Maggioni, A. P., O'Connor, C., Pfeffer, M. A., Solomon, S. D., Tendera, M., van Veldhuisen, D. J., Albizem, M., Cheng, S., Scarlata, D., Swedberg, K., Young, J. B., Amuchastegui, M., Belziti, C., Bluguermann, J., Caccavo, M., Cartasegna, L., Colque, R., Cuneo, C., Fernandez, A., Gabito, A., Goicochea, R., Gonzalez, M., Gorosito, V., Grinfeld, L., Hominal, M., Kevorkian, R., Litvak Bruno, M., Llanos, J., Mackinnon, I., Manuale, O., Marzetti, E., Nul, D., Perna, E., Riccitelli, M., Sanchez, A., Santos, D., Schygiel, P., Toblli, J., Vogel, D., Aggarwal, A., Amerena, J., De Looze, F., Fletcher, P., Hare, D., Ireland, M., Krum, H., Lattimore, J., Marwick, T., Sindone, A., Thompson, P., Waites, J., Altenberger, J., Ebner, C., Lenz, K., Pacher, R., Poelzl, G., Charlier, F., de Ceuninck, M., De Keulenaer, G., Dendale, P., Marechal, P., Mullens, W., Thoeng, J., Vanderheyden, M., Vanhaecke, J., Weytjens, C., Wollaert, B., Albuquerque, D., Almeida, D., Aspe y Rosas, J., Bocchi, E., Bordignon, S., Clausell, N., Kaiser, S., Leaes, P., Martins Alves, S., Montera, M., Moura, L., Pereira de Castro, R., Rassi, S., Reis, A., Saraiva, J., Simoes, M., Souza Neto, J., Teixeira, M., Benov, H., Chompalova, B., Donova, T., Georgiev, P., Gotchev, D., Goudev, A., Grigorov, M., Guenova, D., Hergeldjieva, V., Ivanov, D., Kostova, E., Manolova, A., Marchev, S., Nikolov, F., Popov, A., Raev, D., Tzekova, M., Czarnecki, W., Giannetti, N., Haddad, H., Heath, J., Huynh, T., Lepage, S., Liu, P., Lonn, E., Ma, P., Manyari, D., Moe, G., Parker, J., Pesant, Y., Rajda, M., Ricci, J., Roth, S., Sestier, F., Sluzar, V., Sussex, B., Vizel, S., Antezana, G., Bugueno, C., Castro, P., Conejeros, C., Manriquez, L., Martinez, D., Potthoff, S., Stockins, B., Vukasovic, J., Gregor, P., Herold, M., Jerabek, O., Jirmar, R., Kuchar, R., Linhart, A., Podzemska, B., Soucek, M., Spac, J., Spacek, R., Vodnansky, P., Bronnum-Schou, J., Clemmensen, K., Egstrup, K., Jensen, G., Kjoller-Hansen, L., Kober, L., Markenvard, J., Rokkedal, J., Skagen, K., Torp-Pedersen, C., Tuxen, C., Videbak, L., Laks, T., Vahula, V., Harjola, V., Kettunen, R., Kotila, M., Bauer, F., Cohen Solal, A., Coisne, D., Davy, J., De Groote, P., Dos Santos, P., Funck, F., Galinier, M., Gibelin, P., Isnard, R., Neuder, Y., Roul, G., Sabatier, R., Trochu, J., Anker, S., Denny, S., Dreykluft, T., Flesch, M., Genth-Zotz, S., Hambrecht, R., Hein, J., Jeserich, M., John, M., Kreider-Stempfle, H., Laufs, U., Muellerleile, K., Natour, M., Sandri, M., Schaufele, T., von Hodenberg, E., Weyland, K., Winkelmann, B., Tse, H., Yan, B., Barsi, B., Csikasz, J., Dezsi, C., Edes, I., Forster, T., Karpati, P., Kerekes, C., Kis, E., Kosa, I., Lupkovics, G., Nagy, A., Preda, I., Ronaszeki, A., Tomcsanyi, J., Zamolyi, K., Agarwal, D., Bahl, V., Bordoloi, A., Chockalingam, K., Chopda, M., Chopra, V., Dugal, J., Ghaisas, N., Ghosh, S., Grant, P., Hiremath, S., Iyengar, S., Jagadeesa Subramania, B., Jain, P., Joshi, A., Khan, A., Mullasari, A., Naik, S., Oomman, A., Pai, V., Pareppally Gopal, R., Parikh, K., Patel, T., Prakash, V., Sastry, B., Sathe, S., Sinha, N., Srikanthan, V., Subburamakrishnan, P., Thacker, H., Wander, G., Admon, D., Katz, A., Klainman, E., Lewis, B., Marmor, A., Moriel, M., Mosseri, M., Shotan, A., Weinstein, J., Zimlichman, R., Agostoni, P., Albanese, M., Alunni, G., Bini, R., Boccanelli, A., Bolognese, L., Campana, C., Carbonieri, E., Carpino, C., Checco, L., Cosmi, F., D'Angelo, G., De Cristofaro, M., Floresta, A., Fucili, A., Galvani, M., Ivleva, A., Marra, S., Musca, G., Peccerillo, N., Perrone Filardi, P., Picchio, E., Russo, T., Scelsi, L., Senni, M., Tavazzi, L., Erglis, A., Jasinkevica, I., Kakurina, N., Veze, I., Volans, E., Bagdonas, A., Berukstis, E., Celutkiene, J., Dambrauskaite, A., Jarasuniene, D., Luksiene, D., Rudys, A., Sakalyte, G., Sliaziene, S., Aguilar-Romero, R., Cardona-Munoz, E., Castro-Jimenez, J., Chavez-Herrera, J., Chuquiure Valenzuela, E., De la Pena, G., Herrera, E., Leiva-Pons, J., Lopez Alvarado, A., Mendez Machado, G., Ramos-Lopez, G., Basart, D., Buijs, E., Cornel, J., de Leeuw, M., Dijkgraaf, R., Dunselman, P., Freericks, M., Hamraoui, K., Lenderlink, T., Linssen, G., Lodewick, P., Lodewijks, C., Lok, D., Nierop, P., Ronner, E., Somsen, A., van Dantzig, J., van der Burgh, P., van Kempen, L., van Vlies, B., Voors, A., Wardeh, A., Willems, F., Dickstein, K., Gundersen, T., Hole, T., Thalamus, J., Westheim, A., Dabrowski, M., Gorski, J., Korewicki, J., Kuc, K., Miekus, P., Musial, W., Niegowska, J., Piotrowski, W., Podolec, P., Polonski, L., Ponikowski, P., Rynkiewicz, A., Szelemej, R., Trusz-Gluza, M., Ujda, M., Wojciechowski, D., Wysokinski, A., Camacho, A., Fonseca, C., Monteiro, P., Apetrei, E., Bruckner, I., Carasca, E., Coman, I., Datcu, M., Dragulescu, S., Ionescu, P., Iordachescu-Petica, D., Manitiu, I., Popa, V., Pop-Moldovan, A., Radoi, M., Stamate, S., Tomescu, M., Vita, I., Aroutiounov, G., Ballyuzek, M., Bart, B., Churina, S., Glezer, M., Goloshchekin, B., Kobalava, Z., Kostenko, V., Lopatin, Y., Martynov, A., Orlov, V., Semernin, E., Shogenov, Z., Sidorenko, B., Skvortsov, A., Storzhakov, G., Sulimov, V., Talibov, O., Tereshenko, S., Tsyrline, V., Zadionchenko, V., Zateyshchikov, D., Dzupina, A., Hranai, M., Kmec, J., Micko, K., Murin, J., Pella, D., Sojka, G., Spisak, V., Vahala, P., Vinanska, D., Badat, A., Bayat, J., Dawood, S., Delport, E., Ellis, G., Garda, R., Klug, E., Mabin, T., Naidoo, D., Pretorius, M., Ranjith, N., Van Zyl, L., Weich, H., Anguita, M., Berrazueta, J., Bruguera i Cortada, J., de Teresa, E., Gomez Sanchez, M., Gonzalez Juanatey, J., Gonzalez-Maqueda, I., Jordana, R., Lupon, J., Manzano, L., Pascual Figal, D., Pulpon, L., Recio, J., Ridocci Soriano, F., Rodriguez Lambert, J., Roig Minguell, E., Romero, J., Valdovinos, P., Klintberg, L., Kronvall, T., Lycksell, M., Morner, S., Rydberg, E., Timberg, I., Wikstrom, G., Moccetti, T., Ashok, J., Banerjee, P., Carr-White, G., Cleland, J., Connolly, E., Francis, M., Greenbaum, R., Kadr, H., Lindsay, S., McMurray, J., Megarry, S., Memon, A., Murdoch, D., Senior, R., Squire, I., Tan, L., Witte, K., Adams, K., Adamson, P., Adler, A., Altschul, L., Altschuller, A., Amirani, H., Anand, I., Andreou, C., Ansari, M., Antonishen, M., Banchs, H., Banerjee, S., Banish, D., Bank, A., Barbagelata, A., Barnard, D., Bellinger, R., Benn, A., Berk, M., Berry, B., Bethala, V., Bilazarian, S., Bisognano, J., Bleyer, F., Blum, M., Boehmer, J., Bouchard, A., Boyle, A., Bozkurt, B., Brown, C., Burlew, B., Burnham, K., Butler, J., Call, J., Cambier, P., Cappola, T., Carlson, R., Chandler, B., Chandra, R., Chandraratna, P., Chernick, R., Colan, D., Colfer, H., Colucci, W., Connelly, T., Costantini, O., Dadkhah, S., Dauber, I., Davis, J., Davis, S., Denning, S., Drazner, M., Dunlap, S., Egbujiobi, L., Elkayam, U., Elliott, J., El-Shahawy, M., Essandoh, L., Ewald, G., Fang, J., Farhoud, H., Felker, G., Fernandez, J., Festin, R., Fishbein, G., Florea, V., Flores, E., Floro, J., Gabris, M., Garg, M., Gatewood, R., Geller, M., Ghali, J., Ghumman, W., Gibbs, G., Gillespie, E., Gilmore, R., Gogia, H., Goldberg, L., Gradus-Pizlo, I., Grainger, T., Gudmundsson, G., Gunawardena, D., Gupta, D., Hack, T., Hall, S., Hamroff, G., Hankins, S., Hanna, M., Hargrove, J., Haught, W., Hauptman, P., Hazelrigg, M., Herzog, C., Heywood, J., Hill, T., Hilton, T., Hirsch, H., Hunter, J., Ibrahim, H., Imburgia, M., Iteld, B., Jackson, B., Jaffrani, N., Jain, D., Jain, A., James, M., Jimenez, J., Johnson, E., Kale, P., Kaneshige, A., Kapadia, S., Karia, D., Karlsberg, R., Katholi, R., Kerut, E., Khoury, W., Kipperman, R., Klapholz, M., Kosinski, E., Kozinn, M., Kraus, D., Krueger, S., Kumar, S., Lader, E., Lee, C., Levy, W., Lewis, E., Light-McGroary, K., Loh, I., Lombardi, W., Machado, C., Maislos, F., Mancini, D., Markus, T., Mather, P., McCants, K., McGrew, F., McLaurin, B., McMillan, E., McNamara, D., Meyer, T., Meymandi, S., Miller, A., Minami, E., Modi, M., Mody, F., Mohanty, P., Moscoso, R., Moskowitz, R., Moustafa, M., Mullen, M., Naz, T., Noonan, T., O'Brien, T., Oellerich, W., Oren, R., Pamboukian, S., Pereira, N., Pitt, W., Porter, C., Prabhu, S., Promisloff, S., Ratkovec, R., Richardson, R., Ross, A., Saleh, N., Saltzberg, M., Sarkar, S., Schmedtje, J., Schneider, R., Schuyler, G., Shanes, J., Sharma, A., Siegel, C., Siegel, R., Silber, D., Singh, V., Singh, N., Singh, J., Sklar, J., Small, R., Smith, A., Smith, E., Smull, D., Sotolongo, R., Staniloae, C., Stapleton, D., Steele, P., Stehlik, J., Stein, M., Tang, W., Thadani, U., Torre-Amoine, G., Trichon, B., Tsai, C., Tummala, R., Van Bakel, A., Vicari, R., Vijay, N., Vijayaraghavan, K., Vittorio, T., Vossler, M., Wagoner, L., Wallis, D., Ward, N., Widmer, M., Wight, J., Wilkins, C., Williams, C., Williams, G., Winchester, M., Winkel, E., Wittmer, B., Wood, D., Wormer, D., Wright, R., Xu, Z., Yasin, M., Zolty, R., J. J. V., Mcmurray, I. S., Anand, R., Diaz, A. P., Maggioni, C., O'Connor, M. A., Pfeffer, S. D., Solomon, M., Tendera, D. J., van Veldhuisen, M., Albizem, S., Cheng, D., Scarlata, K., Swedberg, J. B., Young, M., Amuchastegui, C., Belziti, J., Bluguermann, M., Caccavo, L., Cartasegna, R., Colque, C., Cuneo, A., Fernandez, A., Gabito, R., Goicochea, M., Gonzalez, V., Gorosito, L., Grinfeld, M., Hominal, R., Kevorkian, M., Litvak Bruno, J., Llano, I., Mackinnon, O., Manuale, E., Marzetti, D., Nul, E., Perna, M., Riccitelli, A., Sanchez, D., Santo, P., Schygiel, J., Toblli, D., Vogel, A., Aggarwal, J., Amerena, F., De Looze, P., Fletcher, D., Hare, M., Ireland, H., Krum, J., Lattimore, T., Marwick, A., Sindone, P., Thompson, J., Waite, J., Altenberger, C., Ebner, K., Lenz, R., Pacher, G., Poelzl, F., Charlier, M., de Ceuninck, G., De Keulenaer, P., Dendale, P., Marechal, W., Mullen, J., Thoeng, M., Vanderheyden, J., Vanhaecke, C., Weytjen, B., Wollaert, D., Albuquerque, D., Almeida, J. Aspe y., Rosa, E., Bocchi, S., Bordignon, N., Clausell, S., Kaiser, P., Leae, S., Martins Alve, M., Montera, L., Moura, R., Pereira de Castro, S., Rassi, A., Rei, J., Saraiva, M., Simoe, J., Souza Neto, M., Teixeira, H., Benov, B., Chompalova, T., Donova, P., Georgiev, D., Gotchev, A., Goudev, M., Grigorov, D., Guenova, V., Hergeldjieva, D., Ivanov, E., Kostova, A., Manolova, S., Marchev, F., Nikolov, A., Popov, D., Raev, M., Tzekova, W., Czarnecki, N., Giannetti, H., Haddad, J., Heath, T., Huynh, S., Lepage, P., Liu, E., Lonn, P., Ma, D., Manyari, G., Moe, J., Parker, Y., Pesant, M., Rajda, J., Ricci, S., Roth, F., Sestier, V., Sluzar, B., Sussex, S., Vizel, G., Antezana, C., Bugueno, P., Castro, C., Conejero, L., Manriquez, D., Martinez, S., Potthoff, B., Stockin, J., Vukasovic, P., Gregor, M., Herold, O., Jerabek, R., Jirmar, R., Kuchar, A., Linhart, B., Podzemska, M., Soucek, J., Spac, R., Spacek, P., Vodnansky, J., Bronnum Schou, K., Clemmensen, K., Egstrup, G., Jensen, L., Kjoller Hansen, L., Kober, J., Markenvard, J., Rokkedal, K., Skagen, C., Torp Pedersen, C., Tuxen, L., Videbak, T., Lak, V., Vahula, V., Harjola, R., Kettunen, M., Kotila, F., Bauer, A., Cohen Solal, D., Coisne, J., Davy, P., De Groote, P., Dos Santo, F., Funck, M., Galinier, P., Gibelin, R., Isnard, Y., Neuder, G., Roul, R., Sabatier, J., Trochu, S., Anker, S., Denny, T., Dreykluft, M., Flesch, S., Genth Zotz, R., Hambrecht, J., Hein, M., Jeserich, M., John, H., Kreider Stempfle, U., Lauf, K., Muellerleile, M., Natour, M., Sandri, T., Schaufele, E., von Hodenberg, K., Weyland, B., Winkelmann, H., Tse, B., Yan, B., Barsi, J., Csikasz, C., Dezsi, I., Ede, T., Forster, P., Karpati, C., Kereke, E., Ki, I., Kosa, G., Lupkovic, A., Nagy, I., Preda, A., Ronaszeki, J., Tomcsanyi, K., Zamolyi, D., Agarwal, V., Bahl, A., Bordoloi, K., Chockalingam, M., Chopda, V., Chopra, J., Dugal, N., Ghaisa, S., Ghosh, P., Grant, S., Hiremath, S., Iyengar, B., Jagadeesa Subramania, P., Jain, A., Joshi, A., Khan, A., Mullasari, S., Naik, A., Oomman, V., Pai, R., Pareppally Gopal, K., Parikh, T., Patel, V., Prakash, B., Sastry, S., Sathe, N., Sinha, V., Srikanthan, P., Subburamakrishnan, H., Thacker, G., Wander, D., Admon, A., Katz, E., Klainman, B., Lewi, A., Marmor, M., Moriel, M., Mosseri, A., Shotan, J., Weinstein, R., Zimlichman, P., Agostoni, M., Albanese, G., Alunni, R., Bini, A., Boccanelli, L., Bolognese, C., Campana, E., Carbonieri, C., Carpino, L., Checco, F., Cosmi, G., D'Angelo, M., De Cristofaro, A., Floresta, A., Fucili, M., Galvani, A., Ivleva, S., Marra, G., Musca, N., Peccerillo, PERRONE FILARDI, Pasquale, E., Picchio, T., Russo, L., Scelsi, M., Senni, L., Tavazzi, A., Ergli, I., Jasinkevica, N., Kakurina, I., Veze, E., Volan, A., Bagdona, E., Beruksti, J., Celutkiene, A., Dambrauskaite, D., Jarasuniene, D., Luksiene, A., Rudy, G., Sakalyte, S., Sliaziene, R., Aguilar Romero, E., Cardona Munoz, J., Castro Jimenez, J., Chavez Herrera, E., Chuquiure Valenzuela, G., De la Pena, E., Herrera, J., Leiva Pon, A., Lopez Alvarado, G., Mendez Machado, G., Ramos Lopez, D., Basart, E., Buij, J., Cornel, M., de Leeuw, R., Dijkgraaf, P., Dunselman, M., Freerick, K., Hamraoui, T., Lenderlink, G., Linssen, P., Lodewick, C., Lodewijk, D., Lok, P., Nierop, E., Ronner, A., Somsen, J., van Dantzig, P., van der Burgh, L., van Kempen, B., van Vlie, A., Voor, A., Wardeh, F., Willem, K., Dickstein, T., Gundersen, T., Hole, J., Thalamu, A., Westheim, M., Dabrowski, J., Gorski, J., Korewicki, K., Kuc, P., Mieku, W., Musial, J., Niegowska, W., Piotrowski, P., Podolec, L., Polonski, P., Ponikowski, A., Rynkiewicz, R., Szelemej, M., Trusz Gluza, M., Ujda, D., Wojciechowski, A., Wysokinski, A., Camacho, C., Fonseca, P., Monteiro, E., Apetrei, I., Bruckner, E., Carasca, I., Coman, M., Datcu, S., Dragulescu, P., Ionescu, D., Iordachescu Petica, I., Manitiu, V., Popa, A., Pop Moldovan, M., Radoi, S., Stamate, M., Tomescu, I., Vita, G., Aroutiounov, M., Ballyuzek, B., Bart, S., Churina, M., Glezer, B., Goloshchekin, Z., Kobalava, V., Kostenko, Y., Lopatin, A., Martynov, V., Orlov, E., Semernin, Z., Shogenov, B., Sidorenko, A., Skvortsov, G., Storzhakov, V., Sulimov, O., Talibov, S., Tereshenko, V., Tsyrline, V., Zadionchenko, D., Zateyshchikov, A., Dzupina, M., Hranai, J., Kmec, K., Micko, J., Murin, D., Pella, G., Sojka, V., Spisak, P., Vahala, D., Vinanska, A., Badat, J., Bayat, S., Dawood, E., Delport, G., Elli, R., Garda, E., Klug, T., Mabin, D., Naidoo, M., Pretoriu, N., Ranjith, L., Van Zyl, H., Weich, M., Anguita, J., Berrazueta, J. Bruguera i., Cortada, E., de Teresa, M., Gomez Sanchez, J., Gonzalez Juanatey, I., Gonzalez Maqueda, R., Jordana, J., Lupon, L., Manzano, D., Pascual Figal, L., Pulpon, J., Recio, F., Ridocci Soriano, J., Rodriguez Lambert, E., Roig Minguell, J., Romero, P., Valdovino, L., Klintberg, T., Kronvall, M., Lycksell, S., Morner, E., Rydberg, I., Timberg, G., Wikstrom, T., Moccetti, J., Ashok, P., Banerjee, G., Carr White, J., Cleland, E., Connolly, M., Franci, R., Greenbaum, H., Kadr, S., Lindsay, J., Mcmurray, S., Megarry, A., Memon, D., Murdoch, R., Senior, I., Squire, L., Tan, K., Witte, K., Adam, P., Adamson, A., Adler, L., Altschul, A., Altschuller, H., Amirani, I., Anand, C., Andreou, M., Ansari, M., Antonishen, H., Banch, S., Banerjee, D., Banish, A., Bank, A., Barbagelata, D., Barnard, R., Bellinger, A., Benn, M., Berk, B., Berry, V., Bethala, S., Bilazarian, J., Bisognano, F., Bleyer, M., Blum, J., Boehmer, A., Bouchard, A., Boyle, B., Bozkurt, C., Brown, B., Burlew, K., Burnham, J., Butler, J., Call, P., Cambier, T., Cappola, R., Carlson, B., Chandler, R., Chandra, P., Chandraratna, R., Chernick, D., Colan, H., Colfer, W., Colucci, T., Connelly, O., Costantini, S., Dadkhah, I., Dauber, J., Davi, S., Davi, S., Denning, M., Drazner, S., Dunlap, L., Egbujiobi, U., Elkayam, J., Elliott, M., El Shahawy, L., Essandoh, G., Ewald, J., Fang, H., Farhoud, G., Felker, J., Fernandez, R., Festin, G., Fishbein, V., Florea, E., Flore, J., Floro, M., Gabri, M., Garg, R., Gatewood, M., Geller, J., Ghali, W., Ghumman, G., Gibb, E., Gillespie, R., Gilmore, H., Gogia, L., Goldberg, I., Gradus Pizlo, T., Grainger, G., Gudmundsson, D., Gunawardena, D., Gupta, T., Hack, S., Hall, G., Hamroff, S., Hankin, M., Hanna, J., Hargrove, W., Haught, P., Hauptman, M., Hazelrigg, C., Herzog, J., Heywood, T., Hill, T., Hilton, H., Hirsch, J., Hunter, H., Ibrahim, M., Imburgia, B., Iteld, B., Jackson, N., Jaffrani, D., Jain, A., Jain, M., Jame, J., Jimenez, E., Johnson, P., Kale, A., Kaneshige, S., Kapadia, D., Karia, R., Karlsberg, R., Katholi, E., Kerut, W., Khoury, R., Kipperman, M., Klapholz, E., Kosinski, M., Kozinn, D., Krau, S., Krueger, S., Kumar, E., Lader, C., Lee, W., Levy, E., Lewi, K., Light McGroary, I., Loh, W., Lombardi, C., Machado, F., Maislo, D., Mancini, T., Marku, P., Mather, K., Mccant, F., Mcgrew, B., Mclaurin, E., Mcmillan, D., Mcnamara, T., Meyer, S., Meymandi, A., Miller, E., Minami, M., Modi, F., Mody, P., Mohanty, R., Moscoso, R., Moskowitz, M., Moustafa, M., Mullen, T., Naz, T., Noonan, T., O'Brien, W., Oellerich, R., Oren, S., Pamboukian, N., Pereira, W., Pitt, C., Porter, S., Prabhu, S., Promisloff, R., Ratkovec, R., Richardson, A., Ro, N., Saleh, M., Saltzberg, S., Sarkar, J., Schmedtje, R., Schneider, G., Schuyler, J., Shane, A., Sharma, C., Siegel, R., Siegel, D., Silber, V., Singh, N., Singh, J., Singh, J., Sklar, R., Small, A., Smith, E., Smith, D., Smull, R., Sotolongo, C., Staniloae, D., Stapleton, P., Steele, J., Stehlik, M., Stein, W., Tang, U., Thadani, G., Torre Amoine, B., Trichon, C., Tsai, R., Tummala, A., Van Bakel, R., Vicari, N., Vijay, K., Vijayaraghavan, T., Vittorio, M., Vossler, L., Wagoner, D., Walli, N., Ward, M., Widmer, J., Wight, C., Wilkin, C., William, G., William, M., Winchester, E., Winkel, B., Wittmer, D., Wood, D., Wormer, R., Wright, Z., Xu, M., Yasin, R., Zolty, Faculteit Medische Wetenschappen/UMCG, and Cardiovascular Centre (CVC)

Subjects
Male, CHRONIC KIDNEY-DISEASE, Darbepoetin alfa, medicine.medical_treatment, heart failure, Ciencias de la Salud, Comorbidity, Severity of Illness Index, law.invention, DOUBLE-BLIND, Randomized controlled trial, law, Interquartile range, Cause of Death, Medicine, Cause of death, Aged, 80 and over, Clinical Trials as Topic, CARDIAC-RESYNCHRONIZATION THERAPY, HEALTH-STATUS, Ética Médica, Middle Aged, RANDOMIZED CONTROLLED-TRIAL, Hospitalization, IRON-DEFICIENCY, Treatment Outcome, purl.org/becyt/ford/3 [https], Female, TREATMENT OPTIONS, Cardiology and Cardiovascular Medicine, medicine.drug, medicine.medical_specialty, CIENCIAS MÉDICAS Y DE LA SALUD, Anemia, Cardiac resynchronization therapy, Heart failure, Anaemia, purl.org/becyt/ford/3.3 [https], Double-Blind Method, Internal medicine, Humans, Clinical Trials, ANEMIA, Erythropoietin, Aged, Demography, anaemia, business.industry, MORTALITY, medicine.disease, MORBIDITY CHARM PROGRAM, Clinical trial, Hematinics, Physical therapy, CAUSA DA MORTE, business
Abstract

AIMS: This report describes the baseline characteristics of patients in the Reduction of Events with Darbepoetin alfa in Heart Failure trial (RED-HF) which is testing the hypothesis that anaemia correction with darbepoetin alfa will reduce the composite endpoint of death from any cause or hospital admission for worsening heart failure, and improve other outcomes. METHODS AND RESULTS: Key demographic, clinical, and laboratory findings, along with baseline treatment, are reported and compared with those of patients in other recent clinical trials in heart failure. Compared with other recent trials, RED-HF enrolled more elderly [mean age 70 (SD 11.4) years], female (41%), and black (9%) patients. RED-HF patients more often had diabetes (46%) and renal impairment (72% had an estimated glomerular filtration rate < 60 mL/min/1.73 m2). Patients in RED-HF had heart failure of longer duration [5.3 (5.4) years], worse NYHA class (35% II, 63% III, and 2% IV), and more signs of congestion. Mean EF was 30% (6.8%). RED-HF patients were well treated at randomization, and pharmacological therapy at baseline was broadly similar to that of other recent trials, taking account of study-specific inclusion/exclusion criteria. Median (interquartile range) haemoglobin at baseline was 112 (106-117) g/L. CONCLUSION: The anaemic patients enrolled in RED-HF were older, moderately to markedly symptomatic, and had extensive co-morbidity. Fil: McMurray, John J. V.. University of Glasgow; Reino Unido Fil: Anand, Inder S.. University of Minnesota; Estados Unidos Fil: Diaz, Rafael. Estudios Clínicos Latinoamérica; Argentina Fil: Maggioni, Aldo P.. Associazione Nazionale Medici Cardiologi Ospedalieri; Italia Fil: O'Connor, Christopher. University of Duke; Estados Unidos Fil: Pfeffer, Marc A.. Brigham and Women’s Hospita; Estados Unidos Fil: Solomon, Scott D.. Brigham and Women’s Hospital; Estados Unidos Fil: Tendera, Micha. Medical University of Silesia; Polonia Fil: van Veldhuisen, Dirk J.. University of Groningen; Países Bajos Fil: Moetaz, Albizem. Amgen Inc.; Estados Unidos Fil: Cheng, Sunfa. Amgen Inc.; Estados Unidos Fil: Scarlata, Debra. Amgen Inc.; Estados Unidos Fil: Swedberg, Karl. University of Gothenburg; Suecia Fil: Young, James B.. Cleveland Clinic. Endocrinology and Metabolism Institute; Estados Unidos Fil: Toblli, Jorge Eduardo. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina Fil: RED-HF Committees Investigators. No especifíca

Published
2013

22. A new model of home-based telemonitored cardiac rehabilitation in patients with heart failure: effectiveness, quality of life, and adherence.

Author

Piotrowicz E, Baranowski R, Bilinska M, Stepnowska M, Piotrowska M, Wójcik A, Korewicki J, Chojnowska L, Malek LA, Klopotowski M, Piotrowski W, and Piotrowicz R

Subjects
Exercise Test, Female, Health Status Indicators, Humans, Male, Middle Aged, Oxygen Consumption, Surveys and Questionnaires, Treatment Outcome, Walking, Heart Failure rehabilitation, Home Care Services, Patient Compliance, Quality of Life, Telemedicine methods
Abstract

Aims: Despite proven benefits of cardiac rehabilitation (CR), currently proposed CR models are not acceptable for many heart failure (HF) patients. The purpose of this study was to evaluate a new model of home-based telemonitored cardiac rehabilitation (HTCR) using walking training compared with an outpatient-based standard cardiac rehabilitation (SCR) using interval training on a cycle ergometer., Methods and Results: The study included 152 HF patients (aged 58.1 + or - 10.2 years, NYHA class II and III, ejection fraction < or = 40%) who were randomized to HTCR (n = 77) or SCR (n = 75). All patients underwent 8 weeks of CR. Both groups were comparable in terms of demographic and clinical characteristics and medical therapy. The effectiveness of CR was assessed by changes in NYHA class, peak oxygen consumption, 6-min walking test distance, and SF-36 score. Cardiac rehabilitation resulted in a significant improvement of all parameters in both groups. All patients in the HTCR group completed the 8 weeks of CR, whereas 15 patients in the SCR group (20%) discontinued CR., Conclusion: In patients with HF, HTCR is equally as effective as SCR and provides a similar improvement in quality of life. Adherence to CR seems to be better for HTCR. Home-based telemonitored cardiac rehabilitation may be a useful alternative form of CR in patients with HF.

Published
2010
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23. Alteration of myocardial sarcoplasmic reticulum Ca2+-ATPase and Na+-Ca2+ exchanger expression in human left ventricular volume overload.

Author

Leszek P, Szperl M, Klisiewicz A, Janas J, Biederman A, Rywik T, Piotrowski W, Kopacz M, and Korewicki J

Subjects
Aged, Aged, 80 and over, Biopsy, Cytokines blood, Female, Gene Expression physiology, Humans, Male, Middle Aged, Mitral Valve Insufficiency pathology, Mitral Valve Insufficiency physiopathology, Neurotransmitter Agents blood, Papillary Muscles pathology, Papillary Muscles physiopathology, Sarcoplasmic Reticulum pathology, Ventricular Dysfunction, Left pathology, Ventricular Dysfunction, Left physiopathology, Ventricular Remodeling physiology, Mitral Valve Insufficiency genetics, Myocardial Contraction genetics, Sarcoplasmic Reticulum genetics, Sarcoplasmic Reticulum Calcium-Transporting ATPases genetics, Sodium-Calcium Exchanger genetics, Ventricular Dysfunction, Left genetics, Ventricular Remodeling genetics
Abstract

Background: Reduced myocardial contractility is often attributed to altered Ca(2+) transients and expression of Ca(2+)-ATPase of the SR (SERCA) and Na+/Ca(2+)exchanger (NCX) genes., Aims: To assess myocardial expression of SERCA and NCX protein levels in left ventricular (LV) remodelling due to chronic severe mitral regurgitation (MR)., Methods: Myocardial expression of SERCA/NCX in biopsy specimens obtained during mitral surgery was assessed in 36 MR patients with LV remodelling and plasma neurohumoral/cytokine activation and in four non-failing hearts (NFH)., Results: Myocardial protein levels of SERCA were significantly (20%) lower in the MR group than in NFH group (p=0.016). No significant changes in NCX were observed. However, a lack of homogeneity with regard to SERCA/NCX proteins was observed. Moreover, SERCA was negatively correlated with BNP (r=-0.49, p=0.02), TNFalpha (r=-0.68, p=0.0005) and IL-6 (r=-0.52, p=0.02), whereas NCX was only negatively correlated with TNFalpha (r=-0.62, p=0.002)., Conclusions: MR patients showed wide variations in SERCA/NCX protein expression. Myocardial protein levels of SERCA were significantly lower in the MR population. Moreover, a correlation between BNP, cytokines (IL-6, TNFalpha) and the expression of SERCA/NCX proteins was observed.

Published
2007
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24. The ability of thapsigargin and thapsigargicin to activate cells involved in the inflammatory response.

Author

Ali H, Christensen SB, Foreman JC, Pearce FL, Piotrowski W, and Thastrup O

Subjects
Adult, Animals, Calcium blood, Glucuronidase metabolism, Guinea Pigs, Humans, In Vitro Techniques, Muramidase metabolism, Potassium metabolism, Rats, Rats, Inbred Strains, Thapsigargin, Blood Platelets drug effects, Histamine Release drug effects, Lactones, Leukocytes drug effects, Mast Cells drug effects, Plant Extracts pharmacology, Plants, Medicinal, Sesquiterpenes
Abstract

The ability of thapsigargin and thapsigargicin to activate mast cells and leukocytes has been investigated. The thapsigargin-induced histamine release from rat peritoneal mast cells was found to be dependent on the concentration of thapsigargin, the purity of the mast cell preparations, and the number of mast cells in suspension. Thapsigargin induced histamine release from human basophil leukocytes. Thapsigargin induced beta-glucuronidase and lysozyme release from human neutrophil leukocytes. Thapsigargin caused a release of histamine from mesentery, lung, and heart mast cells of the rat, but only to a minor extent from the corresponding guinea-pig cells. Thapsigargicin induced histamine release from mesentery, lung, and heart mast cells of the rat at concentrations from 0.1 microM but provoked only a release from the corresponding guinea-pig cells in the concentration-range 0.16 to 1.6 microM. Thapsigargin increased the cytoplasmic free calcium level in intact human blood platelets at concentrations from 3.0 nM.

Published
1985
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25. Interaction of neurotensin with the substance P receptor mediating histamine release from rat mast cells and the flare in human skin.

Author

Foreman JC, Jordan CC, and Piotrowski W

Subjects
Adult, Animals, Capillary Permeability drug effects, Dose-Response Relationship, Drug, Drug Interactions, Female, Humans, Male, Peptides pharmacology, Rats, Receptors, Neurokinin-1, Skin blood supply, Substance P pharmacology, Histamine Release drug effects, Mast Cells metabolism, Neurotensin pharmacology, Receptors, Cell Surface drug effects, Skin drug effects
Abstract

1 Substance P induced histamine release from rat peritoneal mast cells in a dose-dependent manner over the concentration range 1 to 10 microM. 2 At concentrations in the range 2.5 to 1 0 microM, neurotensin produced only about 5% release of histamine, which was substantially less than the maximum effect obtained with substance P. 3 Neurotensin, 2.5 to 10 microM produced graded inhibition of histamine release induced by substance P. The inhibitory effect of neurotensin was not seen when histamine release was induced by an antigen-antibody effect of neurotensin was not seen when histamine release was induced by an antigen-antibody reaction or by the ionophore, A 23187. Some evidence was obtained to suggest that compound 48/80 may interact with the same receptor as substance P and neurotensin. 4 [D-Arg8]neurotensin, [D-Arg9]neurotensin, xenopsin and the C-terminal octapeptide of substance P (SP4-11) all inhibited histamine release by substance P, but physalaemin did not. 5 Neurotensin inhibited the wheal and flare reactions induced by substance P in human skin. 6 [D-Trp7,9]substance P released histamine from rat mast cells and was about 12 times more potent than substance P itself. [D-Trp7,9]SP1-11 also produced wheal and flare responses in human skin, being 1.8 times more potent than substance P in the production of flare.

Published
1982
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