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Preferential in vivo action of F15599, a novel 5-HT1A receptor agonist, at postsynaptic 5-HT1A receptors

Autor: Adrian Newman-Tancredi, Francesc Artigas, Laia Lladó-Pelfort, Pau Celada, M.B. Assié

Publikováno v: British Journal of Pharmacology. 160:1929-1940

Background and purpose: F15599, a novel 5-hydroxytryptamine (5-HT)1A receptor agonist with 1000-fold selectivity for 5-HT compared with other monoamine receptors, shows antidepressant and procognitive activity at very low doses in animal models. We e

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d5caec55a5f530867c7512328252d18f
https://doi.org/10.1111/j.1476-5381.2010.00738.x

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Signal transduction and functional selectivity of F15599, a preferential post-synaptic 5-HT1Areceptor agonist

Autor: Adrian Newman-Tancredi, P. Heusler, L. Bruins Slot, M.B. Assié, Fc C. Colpaert, Bernard Vacher, Cristina Cosi, Emilie Lauressergues, Jean-Claude Martel, J. Buritova, Didier Cussac

Publikováno v: British Journal of Pharmacology. 156:338-353

Background and purpose: Activation of post-synaptic 5-HT1A receptors may provide enhanced therapy against depression. We describe the signal transduction profile of F15599, a novel 5-HT1A receptor agonist. Experimental approach: F15599 was compared w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::da5a1f0e2a6c9ba8890550729ae27a28
https://doi.org/10.1111/j.1476-5381.2008.00001.x

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F15063, a potential antipsychotic with D2/D3antagonist, 5-HT1Aagonist and D4partial agonist properties: (I)in vitroreceptor affinity and efficacy profile

Autor: J.C. Martel, Cristina Cosi, Christiane Palmier, M.B. Assié, Francis Colpaert, Bernard Vacher, Didier Cussac, L. Bruins Slot, Adrian Newman-Tancredi, Isabelle Rauly-Lestienne

Publikováno v: British Journal of Pharmacology. 151:237-252

Background and purpose: Combining 5-HT1A receptor activation with dopamine D2/D3 receptor blockade should improve negative symptoms and cognitive deficits in schizophrenia. We describe the in vitro profile of F15063 (N-[(2,2-dimethyl-2,3-dihydro-benz

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::06ed74a2f4a60962e6adc70720c41e46
https://doi.org/10.1038/sj.bjp.0707158

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Differential in vivo Inhibition of [3H]Nemonapride Binding by Atypical Antipsychotics in Rat Striatum, Olfactory Lobes, and Frontal Cortex

Autor: Nathalie Consul-Denjean, M.B. Assié, Wouter Koek, Adrian Newman-Tancredi

Publikováno v: Pharmacology. 75:63-68

Dopamine D2 receptor blockade is thought to be mandatory for antipsychotic action because most of the currently used antipsychotics have high affinity at these receptors. Here, we examined the in vivo binding characteristics of the D2-like receptor a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::92ff0f6e15209604419331c77e763941
https://doi.org/10.1159/000086948

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Levomilnacipran (F2695), a norepinephrine-preferring SNRI: profile in vitro and in models of depression and anxiety

Autor: Laurent Bardin, J.A. O'Connor, M.B. Assié, Didier Cussac, Agnès Auclair, Adrian Newman-Tancredi, P. Heusler, Ronan Depoortère, M. Marien, Jean-Claude Martel

Publikováno v: Neuropharmacology. 70

Levomilnacipran (LVM; F2695) is the more active enantiomer of the serotonin/norepinephrine (5-HT/NE) reuptake inhibitor (SNRI) milnacipran and is currently under development for the treatment of major depressive disorder. LVM was benchmarked against

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::79a8dc4d5920704ec92e8c61e7fec90a
https://pubmed.ncbi.nlm.nih.gov/23499664

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5-HT1A receptors are involved in the effects of xaliproden on G-protein activation, neurotransmitter release and nociception

Autor: Adrian Newman-Tancredi, Laurent Bardin, Ronan Depoortère, Cussac Didier, Jean-Claude Martel, M.B. Assié

Background and purpose: Xaliproden (SR57746A) is a 5-HT1A receptor agonist and neurotrophic agent that reduces oxaliplatin-mediated neuropathy in clinical trials. The present study investigated its profile on in vitro transduction, neurochemical resp

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::31718fec259459503c7475fe553587e8
https://europepmc.org/articles/PMC2795245/

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Large-amplitude 5-HT1A receptor activation: a new mechanism of profound, central analgesia

Autor: Francis Colpaert, Wouter Koek, M.B. Assié, Elisabeth Carilla-Durand, Bernard Vacher, Xiao Jun Xu, Cristina Cosi, Petrus J. Pauwels, L. Bardin, J.P. Tarayre, Zsuzsanna Wiesenfeld-Hallin

Publikováno v: Neuropharmacology. 43(6)

We report the discovery of F 13640 and evidence suggesting this agent to produce powerful, broad-spectrum analgesia by novel molecular and neuroadaptative mechanisms. F 13640 stimulates G(alphaomicron) protein coupling to 5-HT(1A) receptors to an ext

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::30938c8de06b8a7fc3075e2c1e62ed29
https://pubmed.ncbi.nlm.nih.gov/12423664

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