Search Results - "P. J. Pauwels"

Large-amplitude 5-HT1A receptor activation: a new mechanism of profound, central analgesia by Colpaert, F C, Tarayre, J P, Koek, W, Pauwels, P J, Bardin, L, Xu, X-J, Wiesenfeld-Hallin, Z, Cosi, C, Carilla-Durand, E, Assié, M B, Vacher, B

“…We report the discovery of F 13640 and evidence suggesting this agent to produce powerful, broad-spectrum analgesia by novel molecular and neuroadaptative…”
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In vitro and in vivo receptor binding and effects on monoamine turnover in rat brain regions of the novel antipsychotics risperidone and ocaperidone by Leysen, J E, Janssen, P M, Gommeren, W, Wynants, J, Pauwels, P J, Janssen, P A

“…Risperidone and ocaperidone are new benzisoxazol antipsychotics with particularly beneficial effects in schizophrenia. We report a comprehensive study on the…”
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Mutation in a protein kinase C phosphorylation site of the 5-HT1A receptor preferentially attenuates Ca2+ responses to partial as opposed to higher-efficacy 5-HT1A agonists by WURCH, T, COLPAERT, F. C, PAUWELS, P. J

“…The Thr(149)Ala mutation in a putative protein kinase C phosphorylation site of the 5-HT(1A) receptor's second intracellular loop has been shown to affect the…”
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Stimulated [35S]GTP gamma S binding by 5-HT1A receptor agonists in recombinant cell lines. Modulation of apparent efficacy by G-protein activation state by Pauwels, P J, Tardif, S, Wurch, T, Colpaert, F C

“…G-protein activation by different 5-HT receptor ligands was investigated in h5-HT1A receptor-transfected C6-glial and HeLa cells using agonist-stimulated…”
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Present and future of 5-HT receptor agonists as antimigraine drugs by Pauwels, P J, John, G W

“…Serotonin (5-hydroxytryptamine; 5-HT) is thought to play an important role in the pathogenesis of migraine. The discovery of the 5-HT1B/1D/1F agonist…”
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Heterogeneous ligand-mediated Ca(++) responses at wt and mutant alpha(2A)-adrenoceptors suggest multiple ligand activation binding sites at the alpha(2A)-adrenoceptor by Pauwels, P J, Colpaert, F C

“…Ligand:receptor interactions were analysed at wild-type, Asp(79)Asn and Thr(373)Lys alpha(2A) AR by measuring Ca(++) responses in the co-presence of a G(alpha…”
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The receptor binding profile of the new antihypertensive agent nebivolol and its stereoisomers compared with various beta-adrenergic blockers by Pauwels, P J, Gommeren, W, Van Lommen, G, Janssen, P A, Leysen, J E

“…Nebivolol [the (S,R,R,R)- + (R,S,S,S)-racemic mixture], the 10 stereoisomers, and known beta-adrenergic blockers were investigated in vitro for binding to beta…”
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Partial to complete antagonism by putative antagonists at the wild-type alpha(2C)-adrenoceptor based on kinetic analyses of agonist:antagonist interactions by Pauwels, P J, Colpaert, F C

“…1. Activation of the recombinant human alpha(2C)-adrenoceptor (alpha(2C) AR) by (-)-adrenaline in CHO-K1 cells transiently co-expressing a chimeric G(alpha…”
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The 5-HT1D receptor antagonist GR 127,935 is an agonist at cloned human 5-HT1Dα receptor sites by PAUWELS, P. J, COLPAERT, F. C

“…The cAMP response of the 5-HT1D receptor antagonist GR 127,935 was compared with 5-CT and ketanserin at cloned human 5-HT1D alpha receptor sites in transfected…”
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Blockade of nitric oxide formation does not prevent glutamate-induced neurotoxicity in neuronal cultures from rat hippocampus by Pauwels, P J, Leysen, J E

“…This study examined the role of nitric oxide (NO) in glutamate-induced, N-methyl-D-aspartate (NMDA) receptor-mediated neurotoxicity in rat hippocampal neuronal…”
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Different regulation of RGS2 mRNA by haloperidol and clozapine by Robinet, Elisa A, Wurch, Thierry, Pauwels, Petrus J

“…Expression of RGS2 mRNA was transiently up-regulated in rat striatum (25% in the medial part and 50% in the lateral part), in contrast to cingulate cortex and…”
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Inhibition by 5-HT of forskolin-induced cAMP formation in the renal opossum epithelial cell line OK: mediation by a 5-HT1B like receptor and antagonism by methiothepin by Pauwels, P J, Palmier, C

“…The functional activity of various 5-HT receptor agonists, including 5-CT, sumatriptan, CP 93, 129 and 1-naphtylpiperazine, and of drugs known to bind with…”
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Sign-reversal during Persistent Activation in μ -Opioid Signal Transduction by BRUINS SLOT, L.A., PAUWELS, P.J., COLPAERT, F.C.

“…A concept of signal transduction in biological systems specifies that any instantaneous input is appreciated by its departure from the moving average of past…”
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Differentiation between Partial Agonists and Neutral 5-HT1B Antagonists by Chemical Modulation of 3-[3-(N,N-Dimethylamino)propyl]-4-hydroxy- N-[4-(pyridin-4-yl)phenyl]benzamide (GR-55562) by Lamothe, Marie, Pauwels, Petrus J, Belliard, Karine, Schambel, Philippe, Halazy, Serge

“…The synthesis and binding affinity at cloned h5-HT1B, h5-HT1D, and h5-HT1A receptors of…”
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Activity of serotonin (5-HT) receptor agonists, partial agonists and antagonists at cloned human 5-HT1A receptors that are negatively coupled to adenylate cyclase in permanently transfected HeLa cells by Pauwels, P J, Van Gompel, P, Leysen, J E

“…The activity of serotonin (5-HT) receptor agonists, partial agonists and antagonists, and various other neurotransmitter receptor antagonists at human 5-HT1A…”
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Neurotoxic action of veratridine in rat brain neuronal cultures: mechanism of neuroprotection by Ca++ antagonists nonselective for slow Ca++ channels by Pauwels, P J, Van Assouw, H P, Peeters, L, Leysen, J E

“…The effect of various Ca++ antagonists and local anesthetics on neuronal cell degeneration induced by veratridine was studied in primary rat brain neuronal…”
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Functional effects of the 5-HT1D receptor antagonist GR 127,935 at human 5-HT1Dα, 5-HT1Dβ, 5-HT1A and opossum 5-HT1B receptors by PAUWELS, P. J, PALMIER, C

“…The functional activity and selectivity of the novel 5-HT1D receptor antagonist GR 127,935 (2'-methyl-4'(5-methyl-1,2,4 oxadiazol-3-yl)-biphenyl-4-carboxylic…”
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Dimerization of sumatriptan as an efficient way to design a potent, centrally and orally active 5-HT1B agonist by PEREZ, M, PAUWELS, P. J, FOURRIER, C, CHOPIN, P, VALENTIN, J.-P, JOHN, G. W, MARIEN, M, HALAZY, S

“…A new bivalent ligand of formula 3 which results from the covalent coupling of two sumatriptan molecules with a p-xylyl spacer at the level of the sulfonamide…”
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Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors by PEREZ, M, PAUWELS, P. J, PALLARD-SIGOGNEAU, I, FOURRIER, C, CHOPIN, P, PALMIER, C, COLOVRAY, V, HALAZY, S

“…Hybrid molecules built up by covalent coupling of aminopropanol derivatives (especially pindolol) with antidepressant drugs like fluoxetine, paroxetine or…”
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Sequence and Functional Analysis of Cloned Guinea Pig and Rat Serotonin 5‐HT1D Receptors: Common Pharmacological Features Within the 5‐HT1D Receptor Subfamily by Wurch, Thierry, Palmier, Christiane, Colpaert, Francis C., Pauwels, Petrus J.

“…: This study was undertaken to investigate the pharmacology of cloned guinea pig and rat 5‐hydroxytryptamine (serotonin; 5‐HT)1D receptor sites. Guinea pig,…”
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