Identification of 4-methyl-1, 2, 3, 4, 10, 10a-hexahydropyrazino [1, 2-a] indoles as 5-HT2C receptor agonists

S Röver, DR Adams, A Bénardeau, JM Bentley… - Bioorganic & medicinal …, 2005 - Elsevier
Synthesis and evaluation of the activity of new 4-methyl-1, 2, 3, 4, 10, 10a-
hexahydropyrazino [1, 2-a] indoles as 5-HT2C receptor agonists are described …

5-Methyl-1-(3-pyridylcarbamoyl)-1, 2, 3, 5-tetrahydropyrrolo [2, 3-f] indole: a novel 5-HT2C/5-HT2B receptor antagonist with improved affinity, selectivity, and oral …

IT Forbes, P Ham, DH Booth, RT Martin… - Journal of medicinal …, 1995 - ACS Publications
The preparation of a series of conformationally restricted analogues of indolylurea 1, namely
tetrahydropyrroloindoles and tetrahydropyrroloquinolines, is described. The binding …

Tetrahydroquinoline-based tricyclic amines as potent and selective agonists of the 5-HT2C receptor

TO Schrader, M Kasem, A Ren, K Feichtinger… - Bioorganic & Medicinal …, 2016 - Elsevier
The syntheses, structure-activity relationships (SARs), and biological activities of
tetrahydroquinoline-based tricyclic amines as 5-HT 2C receptor agonists are reported. An …

Synthesis and preliminary pharmacological evaluation of 2-benzyloxy substituted aryl ketones as 5-HT4 receptor antagonists

RD Clark, A Jahangir, JA Langston… - Bioorganic & Medicinal …, 1994 - Elsevier
Structural modification of the 2-methoxy group and at the 4-position of the piperidine ring of
the 5-HT 4 partial agonist 1 led to analogues with increased affinity for the 5-HT 4 receptor …

Novel 1-(azacyclyl)-3-arylsulfonyl-1H-pyrrolo [2, 3-b] pyridines as 5-HT6 agonists and antagonists

H Elokdah, D Li, G McFarlane, RC Bernotas… - Bioorganic & medicinal …, 2007 - Elsevier
1-Aminoethyl-3-arylsulfonyl-1H-indoles 1 are 5-HT6 receptor ligands with modest activity in
a 5-HT6 cyclase assay. Introduction of an additional nitrogen in the indole ring provides 1 …

Synthesis and SAR study of 4-arylpiperidines and 4-aryl-1, 2, 3, 6-tetrahydropyridines as 5-HT2C agonists

RJ Conway, C Valant, A Christopoulos… - Bioorganic & medicinal …, 2012 - Elsevier
A series of substituted 4-arylpiperidines and a smaller family of 4-aryl-1, 2, 3, 6-
tetrahydropyridines were synthesized and their biological activity at the 5-HT2C receptor …

5-HT3 Receptor antagonists. 2. 4-Hydroxy-4-quinolinecarboxylic acid derivatives

H Hayashi, Y Miwa, S Ichikawa, N Yoda… - Journal of medicinal …, 1993 - ACS Publications
A series of 4-hydroxy-3-quinolinecarboxylic acid derivatives (6) and 4-hydroxy-2-oxo-1, 2-
dihydro-3-quinolinecarboxylic acid derivatives (7) were designed and synthesized as 5-HT3 …

Novel and Selective Partial Agonists of 5-HT3 Receptors. 2. Synthesis and Biological Evaluation of Piperazinopyridopyrrolopyrazines, Piperazinopyrroloquinoxalines …

H Prunier, S Rault, JC Lancelot, M Robba… - Journal of medicinal …, 1997 - ACS Publications
In continuation of our previous work on piperazinopyrrolothienopyrazine derivatives, three
series of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and …

RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist

DW Bonhaus, KK Weinhardt, M Taylor, A DeSouza… - …, 1997 - Elsevier
The 5-HT2C receptor is one of three closely related receptor subtypes in the 5-HT2 receptor
family. 5-HT2A and 5-HT2B selective antagonists have been described. However, no 5 …

Novel Potent and Selective Central 5-HT3 Receptor Ligands Provided with Different Intrinsic Efficacy. 1. Mapping the Central 5-HT3 Receptor Binding Site by …

A Cappelli, M Anzini, S Vomero… - Journal of medicinal …, 1998 - ACS Publications
Synthesis and pharmacological evaluation of a series of condensed quinoline and pyridine
derivatives bearing a N-methylpiperazine moiety attached to the 2-position of the quinoline …