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14. SAR Study of 1-Aryl-4-(phenylarylmethyl)piperazines as Ligands for Both Dopamine D2 and Serotonin 5-HT1A Receptors Showing Varying Degrees of (Ant)agonism. Selection of a Potential Atypical Antipsychotic

Author

Feenstra, Roelof Willem, primary, van den Hoogenband, Adri, additional, Stroomer, Cornelis Nicolaas Jozef, additional, van Stuivenberg, Herman Heinrich, additional, Tulp, Martin Theodorus Maria, additional, Long, Stephen Kenneth, additional, van der Heyden, Johannes Antonius Maria, additional, and Kruse, Cornelis Gerrit, additional

Published
2006
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15. Synthesis, Structure−Activity Relationships, and Biological Properties of 1-Heteroaryl-4-[ω-(1H-indol-3-yl)alkyl]piperazines, Novel Potential Antipsychotics Combining Potent Dopamine D2 Receptor Antagonism with Potent Serotonin Reuptake Inhibition

Author

Smid, Pieter, primary, Coolen, Hein K. A. C., additional, Keizer, Hiskias G., additional, van Hes, Rolf, additional, de Moes, Jan-Peter, additional, den Hartog, Arnold P., additional, Stork, Bob, additional, Plekkenpol, Rob H., additional, Niemann, Leonarda C., additional, Stroomer, Cees N. J., additional, Tulp, Martin Th. M., additional, van Stuivenberg, Herman H., additional, McCreary, Andrew C., additional, Hesselink, Mayke B., additional, Herremans, Arnoud H. J., additional, and Kruse, Chris G., additional

Published
2005
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35. C5-Substituted Derivatives of 5-OMe-BPAT: Synthesis and Interactions with Dopamine D2and Serotonin 5-HT1AReceptors

Author

Homan, Evert J., Tulp, Martin Th.M., Nilsson, Jonas E., Wikström, Håkan V., and Grol, Cor J.

Abstract

Eight new C5-substituted derivatives of the potential atypical antipsychotic agent 5-methoxy-2-[N-(2-benzamidoethyl)-N-n-propylamino]tetralin (5-OMe-BPAT, 1) have been prepared by chemical conversion of the 5-trifluoromethylsulfonyloxy (triflate) analogue 4via various Stille-type cross-couplings, a Heck reaction, and an amidation in moderate to good yields. The 5-acetyl, 5-cyano, 5-methyl, 5-(2-furyl), 5-phenyl, methyl 5-carboxylate, and the 5-carboxamido analogues 5–11thus obtained, the previously disclosed 5-methoxy, 5-hydroxy, and 5-unsubstituted analogues 1–3, and the 5-triflate analogue 4were evaluated for their ability to compete for [3H]-spiperone binding to rat striatal membranes containing dopamine D2receptors, and their ability to compete for [3H]-8-OH-DPAT binding to rat frontal cortex membranes containing serotonin 5-HT1Areceptors in vitro. Compounds 1–11displayed weak to high affinities for dopamine D2receptors, with Ki-values ranging from 550 nM for the 5-carboxamido analogue to 4.9 nM for the 5-hydroxy analogue. The relative affinities of the 5-methoxy, 5-hydroxy, and 5-unsubstituted analogues suggested that these compounds may bind to the same site and in a similar way as the 5-oxygenated DPATs, with the 5-methoxy substituent of 1functioning as a hydrogen bond acceptor. The serotonin 5-HT1Areceptor tolerated more structural diversity at the C5-position of 1, as revealed by the higher Ki-values of 1–11, which ranged from 60 nM for the 5-carboxamido analogue to 1.0 nM for the 5-unsubstituted analogue. Partial least-squares (PLS) analysis of a set of 24 molecular descriptors, generated for each analogue, revealed no significant correlation between the dopamine D2receptor affinities of 1–11and their molecular properties, supporting the view that they may have different binding modes at this receptor subtype. A PLS model with moderate predictability (Q2=0.49) could be derived for the serotonin 5-HT1Areceptor affinities of 1–11. According to the model, a relatively lipophilic, nonpolar C5-substituent should be optimal for a high affinity at this receptor subtype.

Published
1999
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36. Fragmentation pathways in electron impact mass spectra of methoxyhalobiphenyls

Author

Tulp, Martin Th. M., Safe, Stephen H., and Boyd, Robert K.

Abstract

The electron impact mass spectra of various methoxyhalobiphenyls have been reinvestigated. Previous findings, concerning the effect of the methoxy group upon the main fragmentation routes, have been confirmed and extended. In addition, studies of unimolecular and collision induced fragmentations of ions, using linked scan techniques, have been made. Such an approach permits the identification of substances with a minimal chromatographic separation prior to mass spectrometry. It has also led to some clarification of the fragmentation pathways leading to the observed cracking patterns.

Published
1980
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37. Receptor Binding Profiles of Amiloride Analogues Provide no Evidence for a Link Between Receptors and the Na+/H+ Exchange, But Indicate a Common Structure on Receptor Proteins

Author

Garritsen, Anja, Ijzerman, Adriaan, Tulp, Martin Th., Cragoe, Edward, and Soudijn, Willem

Abstract

Amiloride and its analogues affect radioligand binding to the adenosine-A1 receptor. In this paper, the specificity of this effect is investigated by generating receptor binding profiles for amiloride and two of its analogues. A limited structure-activity relationships study is performed to probe the relationship between inhibition of receptor binding by amiloride analogues and the effects of these compounds on Na+ transport, in particular Na+/H+ exchange. The receptor binding profiles of amiloride, benzamil and 5'-(N,N-hexamethylene)amiloride (HMA) indicate that the compounds affect a variety of receptors and that none of the compounds is highly selective for any of these. The SAR study indicates that it is very unlikely that a direct coupling between receptors and Na+/H+ exchange or another amiloride-sensitive ion transport system is responsible for the inhibition of receptor binding. A correlation between the signal transduction systems coupled to the receptors involved and the potency of the amiloride analogues is also absent. The varying nature of the receptors, affected by amiloride or its analogues, suggests a wide-spread presence of an amiloride binding site on receptors and other membrane proteins.

Published
1991
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38. Identification of hydroxylated chlorodibenzo-p-dioxins, chlorodibenzofurans, chlorodiphenyl ethers and chloronaphthalenes as their methyl ethers by gas chromatography mass spectrometry

Author

Tulp, Martin Th. M. and Hutzinger, Otto

Abstract

The methyl ethers of a number of hydroxylated (poly)chlorodibenzo-p-dioxins, chlorodibenzofurans, chlorodiphenyl ethers and chloronaphthalenes, representing all different hydroxy substitutions, were synthesized and their mass spectra investigated. With the exception of the methoxy derivatives of the chlorodibenzofurans, it appeared that the mass fragmentation patters of the structural isomers of each class of compounds were very specifica and allowed unambiguous assignment of the position of the methoxy group in the molecule. The different fragmentation patterns can be explained in terms of plausible mechanisms resulting in stable charge delocalized (oxonium) ions. Because of its diagnostic value, this method is useful in the structure elucidation of hydroxylated metabolites of pure isomers of chlorodibenzo-p-dioxins, chlorodiphenyl ethers and chloronaphthalenes.

Published
1978
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