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9 results on '"Jefferson, R. G."'

3. European Red List of Habitats Part 2. Terrestrial and freshwater habitats

Author

Janssen, J. A. M., Rodwell, J. S., García Criado, M., Gubbay, S., Haynes, T., Nieto, A., Sanders, N., Landucci, F., Loidi, J., Ssymank, A., Tahvanainen, T., Valderrabano, M., Acosta, A., Aronsson, M., Arts, G., Attorre, F., Bergmeier, E., Bijlsma, R. -. J., Bioret, F., Biţă-nicolae, C., Biurrun, I., Calix, M., Capelo, J., Čarni, A., Chytrý, M., Dengler, J., Dimopoulos, P., Essl, F., Gardfjell, H., Gigante, D., Giusso Del Galdo, G., Hájek, M., Jansen, F., Jansen, J., Kapfer, J., Mickolajczak, A., Molina, J. A., Molnár, Z., Paternoster, D., Piernik, A., Poulin, B., Renaux, B., Schaminée, J. H. J., Šumberová, K., Toivonen, H., Tonteri, T., Tsiripidis, I., Tzonev, R., Valachovič, M., Aarrestad, P. A., Agrillo, E., Alegro, E., Alonso, I., Angus, S., Argagnon, O., Armiraglio, S., Assini, S., Aunina, L., Averis, A. B. G., Averis, A. M., Bagella, S., Barina, Z., Barron, S., Bell, S., Bendiksen, E., Bölöni, J., Brandrud, T. E., Brophy, J., Buffa, G., Campos, J. A., Casella, L., Christodoulou, C., Church, A., Corbett, P., Couvreur, J. -. M., Creer, J., Crowle, A., Dahlgren, J., De Keersmaeker, L., Delarze, R., Delescaille, L. -. M., Denys, L., De Saeger, S., Devany, F., De Vries, D., Diack, I., Dimitrov, M., Eide, W., Espirito Santo, D., Fagaras, M., Fievet, V., Finck, P., Fitzpatrick, U., Fotiadis, G., Framstad, E., Frankard, P., Giancola, C., Gussev, C. H., Hall, R., Hamill, B., Haveman, R., Heinze, S., Hennekens, S., Hobohm, C., Ivanov, P., Jacobson, A., Janauer, G., Janišová, M., Jefferson, R. G., Jones, P., Juvan, N., Kącki, Z., Kallimanis, A., Kazoglou, Y., Keith, D., Keulen, K., Király, G., Kirby, K., Kočí, M., Kontula, T., Leibak, E., Leyssen, A., Lotman, S., Lyngstad, A., Mäemets, H., Mainstone, C., Mäkelä, K., Marceno, C., Martin, J. R., Matevski, V., Mesterházy, A., Milanović, Đ., Millaku, F., Miller, R., Millet, J., Mjelde, M., Moen, A., Nygaard, B., Øien, D. -. I., O’Neill, F., Paal, J., Packet, J., Paelinckx, D., Panaïotis, C., Panitsa, M., Perrin, P., Pezzi, G., Prisco, I., Prosser, M., Provoost, S., Rašomavičius, V., Raths, U., Rees, S., Riecken, U., Roosaluste, E., Rove, I., Reymann, J., Rodriguez, J. P., Rothero, E., Rusakova, V., Rusina, S., Scanlan, C., Schuiling, R., Sciandrello, S., Sell, I., Šibík, J., Simkin, J., Škvorc, Ž., Spray, D., Stešević, D., Strand, G. H., Stupar, V., Thomaes, A., Trajanovska, S., Van Braekel, A., Van Landuyt, W., Vanderkerkhove, K., Vandevoorde, B., Van Uytvanck, J., Varga, A., Velkovski, N., Venanzoni, R., Verté, P., Viciani, D., Vrahnakis, M., Von Wachenfeldt, E., Wallace, H., Watt, S., Weeda, E., Wibail, L., Willner, W., P. W. I. L. S. O., N., and Xystrakis, . F.

Subjects
Habitat, Conservation, IUCN, red list, European Directive
Published
2016

6. Highly Selective CB1 Cannabinoid Receptor Ligands and Novel CB1/VR1 Vanilloid Receptor “Hybrid” Ligands

Author

Di Marzo, V., Bisogno, T., De Petrocellis, L., Brandi, I., Jefferson, R. G., Winckler, R. L., Davis, J. B., Dasse, O., Mahadevan, A., Razdan, R. K., and Martin, B. R.

Abstract

Anandamide and the metabolically stabler analogs, (R)-1′-methyl-2′-hydroxy-ethyl-arachidonamide (Met-AEA) and N-(3-methoxy-4-hydroxy-benzyl)-arachidonamide (arvanil), are CB1 cannabinoid and VR1 vanilloid receptors agonists. We synthesized 1′,1′-dimethylheptyl-arvanil (O-1839) and six other AEA analogs obtained by addition of either a hydroxy, cyano, or bromo group on the C-20 atom of 1,1′-dimethylpentyl-Met-AEA (O-1811, O-1812 and O-1860, respectively) or 1,1′-dimethylpentyl-arvanil (O-1856, O-1895 and O-1861, respectively). The compounds were tested for their (i) affinity for CB1 and CB2 receptors, (ii) capability to activate VR1 receptors, (iii) inhibitory effect on the anandamide hydrolysis and on the anandamide membrane transporter, and (iv) cannabimimetic activity in the mouse ‘tetrad’ of in vivo assays. O-1812 is the first ligand ever proven to be highly (500- to 1000-fold) selective for CB1 vs both VR1 and CB2 receptors, while O-1861 is the first true “hybrid” agonist of CB1/VR1 receptors and a compound with potential therapeutic importance. The activities of the seven compounds in vivo did not correlate with their activities at either CB1 or VR1 receptors, thus suggesting the existence of other brain sites of action mediating some of their neurobehavioral actions in mice.

Published
2001
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9. Novel pyrazole cannabinoids: insights into CB(1) receptor recognition and activation.

Author

Wiley JL, Jefferson RG, Grier MC, Mahadevan A, Razdan RK, and Martin BR

Subjects
Analgesics, Non-Narcotic pharmacology, Animals, Binding Sites, Dronabinol pharmacology, Drug Interactions, Gerbillinae, Male, Mice, Mice, Inbred ICR, Piperidines chemistry, Pyrazoles chemistry, Rats, Receptors, Cannabinoid, Receptors, Drug agonists, Receptors, Drug antagonists & inhibitors, Rimonabant, Structure-Activity Relationship, Piperidines pharmacology, Pyrazoles pharmacology, Receptors, Drug metabolism
Abstract

Synthesis of an antagonist, SR141716A, that selectively binds to brain cannabinoid (CB(1)) receptors without producing cannabimimetic activity in vivo, suggests that recognition and activation of cannabinoid receptors are separable events. In the present study, a series of SR141716A analogs were synthesized and were tested for CB(1) binding affinity and in a battery of in vivo tests, including hypomobility, antinociception, and hypothermia in mice. These analogs retained the central pyrazole structure of SR141716A with replacement of the 1-, 3-, 4-, and/or 5-substituents by alkyl side chains or other substituents known to impart potent agonist activity in traditional tricyclic cannabinoid compounds. Although none of the analogs alone produced the profile of cannabimimetic effects seen with full agonists, several of the 3-substituent analogs with higher binding affinities showed partial agonism for one or more measures. Cannabimimetic activity was most noted when the 3-substituent of SR141716A was replaced with an alkyl amide or ketone group. None of the 3-substituted analogs produced antagonist effects when tested in combination with 3 mg/kg Delta(9)-tetrahydrocannabinol (Delta(9)-THC). In contrast, antagonism of Delta(9)-THC's effects without accompanying agonist or partial agonist effects was observed with substitutions at positions 1, 4, and 5. These results suggest that the structural properties of 1- and 5-substituents are primarily responsible for the antagonist activity of SR141716A.

Published
2001

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