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Drug action at the 5-HT(1A) receptor in vivo: autoreceptor and postsynaptic receptor occupancy examined with PET and [carbonyl-(11)C]WAY-100635

Autor: Paul M. Grasby, Philip J. Cowen, Ewen Sedman, Elizabeth Mocaer, Peter A. Sargent, Martin R. Wilkins, Eugenii A Rabiner, Roger N. Gunn

Serotonin 1A (5-HT 1A ) receptors have been implicated in the pathophysiology and treatment of anxiety and depression and are a target for novel drug development. In this qualitative study, positron emission tomography (PET) and [ carbonyl - 11 C]WAY

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8f31829a120b10eb2cac3229636fe2c7
https://ora.ox.ac.uk/objects/uuid:220fd3e0-fc1d-40bc-b8c0-263bc8d7d2e4

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Improvement in the Selectivity and Metabolic Stability of the Serotonin 5-HT1A Ligand, S 15535: A Series of cis- and trans-2-(Arylcycloalkylamine) 1-Indanols

Autor: Patrick Genissel, Anne Dekeyne, Adrian Newman-Tancredi, Bertrand Goument, Marc Bertrand, Millan Mark, Valérie Charlot, Jean-Louis Peglion, Christian Nisole, Hélène Giraud, Nicole Despaux

Publikováno v: Journal of Medicinal Chemistry. 45:165-176

S 15535 (1) displays a distinctive profile of agonist and antagonist (weak partial agonist) activity at pre- and postsynaptic 5-HT(1A) receptors, respectively. It has proven to be active in several models predictive of anxiolytic, antidepressant, and

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::90cce17930fabc2876ec44906a8bc3b9
https://doi.org/10.1021/jm010975+

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Population pharmacokinetic–pharmacodynamic modelling of S 15535, a 5-HT1A receptor agonist, using a behavioural model in rats

Autor: Roeline Jochemsen, Delphine Martin, Peter Vis, Meindert Danhof, Oscar Della Pasqua, Menno R. Kruk, Elisabeth Mocaer

Publikováno v: European Journal of Pharmacology. 414:233-243

The pharmacokinetic-pharmacodynamic relationship of S 15535 (1-(benzodioxan-5-yl) 4-(indan-2-yl)piperazine) and its active 5-hydroxy metabolite S 32784 (1-(benzodioxan-5-yl) 4-(5-hydroxyindan-2-yl)piperazine), and buspirone as a reference, were studi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::954dffa8d84d71ad051352e1e116717a
https://doi.org/10.1016/s0014-2999(01)00801-9

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Roles of 5-HT1A receptors in the dorsal raphe and dorsal hippocampus in anxiety assessed by the behavioral effects of 8-OH-DPAT and S 15535 in a modified Geller–Seifter conflict model

Autor: Luigi Cervo, E Mocaër, A. Bertaglia, Rosario Samanin

Publikováno v: Neuropharmacology. 39:1037-1043

8-OH-DPAT [8-hydroxy-2-(di-N-propylamino)tetralin], a 5-HT(1A) receptor agonist, and S 15535 (4-benzodioxan-5-yl)1-(indan-2-yl)piperazine, a partial agonist at 5-HT(1A) receptors, were administered into the dorsal raphe nucleus and dorsal hippocampus

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ab67f95da7141d7393f05159caea65e8
https://doi.org/10.1016/s0028-3908(99)00189-6

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S 15535, a benzodioxopiperazine acting as presynaptic agonist and postsynaptic 5-HT1A receptor antagonist, prevents the impairment of spatial learning caused by intrahippocampal scopolamine

Autor: Rosario Samanin, Claudia Balducci, Millan Mark, Mirjana Carli, Pierenrico Bonalumi

Publikováno v: British Journal of Pharmacology. 128:1207-1214

The effect of S 15535 (4-benzodioxan-5-yl)1-(indan-2-yl)piperazine), an agonist at presynaptic and antagonist at postsynaptic 5-HT1A receptors, on the impairment of spatial learning caused by intrahippocampal scopolamine in a two-platform spatial dis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8f62e0072a923663e0b8761bf5b158db
https://doi.org/10.1038/sj.bjp.0702915

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Induction of burst firing in ventral tegmental area dopaminergic neurons by activation of serotonin (5-HT)1A receptors: WAY 100,635-reversible actions of the highly selective ligands, flesinoxan and S 15535

Autor: Millan Mark, Françoise Lejeune

Publikováno v: Synapse. 30:172-180

This study examined the influence of the highly selective 5-HT1A receptor ligands, flesinoxan, S 15535, and WAY 100,635, upon the electrical activity of dopaminergic neurons in the ventral tegmental area (VTA), as compared to serotonergic neurons in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::13360bb06ddc8076c617e985c35d4aa1
https://doi.org/10.1002/(sici)1098-2396(199810)30:2<172::aid-syn7>3.0.co

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Agonist and Inverse Agonist Efficacy at Human Recombinant Serotonin 5-HT 1A Receptors as a Function of Receptor:G-protein Stoichiometry

Autor: Adrian Newman-Tancredi, Laurence Verrièle, C. Chaput, Mark Millan, C. Conte

Publikováno v: Neuropharmacology. 36:451-459

Membrane preparations were made from Chinese Hamster Ovary (CHO) cells expressing 1.6 and 4.2 pmol/mg of recombinant human 5-HT 1A receptors, as determined by saturation binding with the selective antagonist, [ 3 H]-S 15535 ([ 3 H]-4-(benzodioxan-5-y

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a480362c0773496f0fa6ec86c66c4e1
https://doi.org/10.1016/s0028-3908(97)00022-1

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S 15535: a highly selective benzodioxopiperazine 5-HT1A receptor ligand which acts as an agonist and an antagonist at presynaptic and postsynaptic sites respectively

Autor: Jean-Louis Peglion, Karin Bervoets, Millan Mark, Hervé Canton, Mauricette Brocco, Jean-Michel Rivet, Alain P. Gobert, Peter S. Widdowson, Françoise Lejeune

Publikováno v: European Journal of Pharmacology. 230:99-102

The novel benzodioxopiperazine, S 15535 (4-(benzodioxan-5-yl)1-(indan-2-yl)piperazine), displayed high affinity for 5-HT 1A binding sites (1.8 nM) whereas its affinity was 100-fold lower at other 5-HT 1A receptor types, at α 1 , α 2 - and β-adreno

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1258dbd68ccec5ca69564723e55a3ec1
https://doi.org/10.1016/0014-2999(93)90416-f

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ChemInform Abstract: Characterization of Potent and Selective Antagonists at Postsynaptic 5- HT1A Receptors in a Series of N4-Substituted Arylpiperazines

Autor: Valérie Audinot, Millan Mark, Alain Gobert, Mauricette Brocco, K Bervoets, S Le Marouille-Girardon, H Canton, Jean-Louis Peglion

Publikováno v: ChemInform. 27

Benzocycloalkyl and benzocycloalkenyl moities linked, directly or via an alkyl chain, to oxygen-bearing heteroarylpiperazines were synthesized, in an attempt to obtain potent and selective antagonists at postsynaptic 5-HT 1A receptors. From the numer

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::3e94cf15c7824413d41583c98b721f8d
https://doi.org/10.1002/chin.199604185

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