Semisynthetic Studies on and Biological Evaluation of N-Methyllaurotetanine Analogues as Ligands for 5-HT Receptors

S Madapa, WW Harding - Journal of Natural Products, 2015 - ACS Publications
N-Methyllaurotetanine (1) has been reported to display good affinity for the 5-HT1A receptor,
but no structure–affinity studies have been performed to date. The commercially available …

1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT2A Partial Agonists

CS Dowd, K Herrick-Davis, C Egan… - Journal of medicinal …, 2000 - ACS Publications
Phenylalkylamines such as 1-(4-bromo-2, 5-dimethoxyphenyl)-2-aminopropane (DOB; 1a)
and its corresponding iodo derivative DOI (2) are commonly used 5-HT2 serotonin agonists …

Activity of Parthenolide at 5HT2A Receptors

JT Weber, MF O'Connor, K Hayataka… - Journal of natural …, 1997 - ACS Publications
Parthenolide displaces [3H] ketanserin from 5HT2A receptors from rat and rabbit brain and
cloned 5HT2A receptors. K i's are in the 100− 250 μM range. These results suggest that …

(−)-5-Methyl-8-hydroxy-(di-n-propylamino) tetralin: A new 5-HT1A receptor antagonist

AC Trillat, M Mathé-Allainmat, B Brémont… - European journal of …, 1998 - Elsevier
−(±)-5-Me-8-OH-DPAT 4 was synthesized by a new synthetic pathway recently described by
us. The (+)-and (−)-enantiomers 4 were prepared from the primary amine 8 by crystallisation …

(±)-Nantenine analogs as antagonists at human 5-HT2A receptors: C1 and flexible congeners

S Chaudhary, S Pecic, O LeGendre, HA Navarro… - Bioorganic & medicinal …, 2009 - Elsevier
C1 and flexible analogs of (±)-nantenine were synthesized and evaluated for antagonist
activity at human 5-HT2A receptors in a calcium mobilization assay. This work has resulted …

A 3 dimensional model for 5-HT1A-receptor agonists based on stereoselective methyl-substituted and conformationally restricted analogs of 8-hydroxy-2 …

C Mellin, J Vallgaarda, DL Nelson… - Journal of medicinal …, 1991 - ACS Publications
The enantiomers of cis-andfrarcs-l, 2, 3, 4, 4a, 5, 10, 10a-octahydro-9-hydroxy-l-propylbenzo
[g] quinolines (10 and 11, respectively) and the enantiomers of trans-l, 2, 3, 4, 4a, 5, 6, 10b …

N-Oxide analogs of WAY-100635: new high affinity 5-HT1A receptor antagonists

S Marchais-Oberwinkler, B Nowicki, VW Pike… - Bioorganic & medicinal …, 2005 - Elsevier
WAY-100635 [N-(2-(1-(4-(2-methoxyphenyl) piperazinyl) ethyl))-N-(2-pyridinyl)
cyclohexanecarboxamide] 1 and its O-desmethyl derivative DWAY 2 are well-known high …

Discovery of Benzamide Analogues as a Novel Class of 5‐HT3 Receptor Agonists

CG Jørgensen, B Frølund, J Kehler… - ChemMedChem, 2011 - Wiley Online Library
A 5‐HT3 receptor agonist based on a benzamide scaffold was identified in a screening of a
small commercial compound library, and an elaborate SAR study originating from this hit …

Indolebutylamines as Selective 5-HT1A Agonists

T Heinrich, H Böttcher, GD Bartoszyk… - Journal of medicinal …, 2004 - ACS Publications
A series of new 1-[4-(indol-3-yl) butyl]-4-arylpiperazines was prepared to identify highly
selective and potent 5-HT1A agonists as potential pharmacological tools in studies of mood …

Arylpiperazines with N-acylated amino acids as 5-HT1A receptor ligands

P Zajdel, G Subra, AJ Bojarski, B Duszyńska… - Bioorganic & medicinal …, 2006 - Elsevier
A library consisting of 60 arylpiperazines modified with N-acylated amino acids was
prepared on BAL linker SynPhase™ Lanterns and evaluated in vitro for 5-HT1A receptor …