S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: I. A mechanistic characterization

MJ Millan, CM la Cour, B Chanrion, DS Dupuis… - … of Pharmacology and …, 2012 - ASPET
Although most antidepressants suppress serotonin (5-HT) and/or noradrenaline reuptake,
blockade of 5-HT2C receptors and α2-adrenoceptors likewise enhances monoaminergic …

S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: II. A behavioral, neurochemical, and …

A Dekeyne, M Brocco, F Loiseau, A Gobert… - … of Pharmacology and …, 2012 - ASPET
The present studies characterized the functional profile of N-[4-methoxy-3-(4-
methylpiperazin-1-yl) phenyl]-1, 2-dihydro-3-H-benzo [e] indole-3-carboxamide)(S32212), a …

The role of activation of the 5-HT1A receptor and adenylate cyclase in the antidepressant-like effect of YL-0919, a dual 5-HT1A agonist and selective serotonin …

JJ Qin, HX Chen, N Zhao, L Yuan, YZ Zhang… - Neuroscience …, 2014 - Elsevier
This study aimed to explore the possible mechanisms underlying the antidepressant-like
effect of YL-0919, a novel antidepressant candidate with dual activity as a 5-HT 1A receptor …

SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety

MD Wood, C Reavill, B Trail, A Wilson, T Stean… - …, 2001 - Elsevier
SB-243213 (5-methyl-1-[[-2-[(2-methyl-3-pyridyl) oxy]-5-pyridyl] carbamoyl]-6-
trifluoromethylindoline hydrochloride) is a new, selective 5-hydroxytryptamine (5-HT) 2C …

Selective 5-hydroxytryptamine 2C receptor agonists derived from the lead compound tranylcypromine: identification of drugs with antidepressant-like action

SJ Cho, NH Jensen, T Kurome, S Kadari… - Journal of medicinal …, 2009 - ACS Publications
We report here the design, synthesis, and pharmacological properties of a series of
compounds related to tranylcypromine (9), which itself was discovered as a lead compound …

Deramciclane, a putative anxiolytic drug, is a serotonin 5-HT2C receptor inverse agonist but fails to induce 5-HT2C receptor down-regulation

EP Pälvimäki, H Majasuo, M Kuoppamäki… - …, 1998 - Springer
Abstract Deramciclane (EGIS-3886) is a novel anxiolytic agent that binds with high affinity to
5-HT 2A/2C receptors. The interactions of deramciclane with the serotonin 5-HT 2C receptor …

[HTML][HTML] Design, sustainable synthesis and biological evaluation of a novel dual α2A/5-HT7 receptor antagonist with antidepressant-like properties

V Canale, M Kotańska, A Dziubina, M Stefaniak… - Molecules, 2021 - mdpi.com
The complex pathophysiology of depression, together with the limits of currently available
antidepressants, has resulted in the continuous quest for alternative therapeutic strategies …

Pharmacological and behavioral profile of N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy) phenylmethyl) carbamide (2R, 3R) …

KE Vanover, DM Weiner, M Makhay, I Veinbergs… - … of Pharmacology and …, 2006 - ASPET
The in vitro and in vivo pharmacological properties of N-(4-fluorophenylmethyl)-N-(1-
methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy) phenylmethyl) carbamide (2 R, 3 R) …

[HTML][HTML] The Novel Pimavanserin Derivative ST-2300 with Histamine H3 Receptor Affinity Shows Reduced 5-HT2A Binding, but Maintains Antidepressant- and …

K Venkatachalam, S Zhong, M Dubiel, G Satała… - Biomolecules, 2022 - mdpi.com
The therapy of depression is challenging and still unsatisfactory despite the presence of
many antidepressant drugs on the market. Consequently, there is a continuous need to …

Inverse agonist and neutral antagonist actions of antidepressants at recombinant and native 5-hydroxytryptamine2C receptors: differential modulation of cell surface …

B Chanrion, CM La Cour, S Gavarini, M Seimandi… - Molecular …, 2008 - ASPET
Despite the importance of 5-hydroxytryptamine (5-HT) 2C (serotonin) receptors in the control
of depressive states, actions of antidepressants at these receptors remain poorly …