1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands

R Bernotas, S Lenicek, S Antane, GM Zhang… - Bioorganic & medicinal …, 2004 - Elsevier
Novel 1-(2-aminoethyl)-3-(arylsulfonyl)-1H-indoles were prepared. Binding assays indicated
they are 5-HT6 receptor ligands, among which N, N-dimethyl-N-{2-[3-(1-naphthylsulfonyl) …

A Novel, Potent, and Selective 5-HT7 Antagonist:  (R)-3-(2-(2-(4-Methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl)phenol (SB-269970)

PJ Lovell, SM Bromidge, S Dabbs… - Journal of medicinal …, 2000 - ACS Publications
Introduction. The human 5-HT7 receptor is a recently discovered member of the seven-
transmembrane G-protein-coupled receptor superfamily. 2 The most abundant isoform 5 …

Diaminopyrimidine and diaminopyridine 5-HT7 ligands

DJ Denhart, AV Purandare, JD Catt, HD King… - Bioorganic & medicinal …, 2004 - Elsevier
The present studies have identified a series of diaminopyrimidines and diaminopyridines as
novel 5-HT7 receptor ligands. Three regiosiomeric classes of pyrimidines and four …

The multiobjective based design, synthesis and evaluation of the arylsulfonamide/amide derivatives of aryloxyethyl-and arylthioethyl-piperidines and pyrrolidines as a …

P Zajdel, R Kurczab, K Grychowska, G Satała… - European journal of …, 2012 - Elsevier
An analysis of the virtual combinatorial library was used for refining a pilot set of 34
derivatives and designing a targeted 38-member library of the arylamide and …

Characterization of [125I]‐SB‐258585 binding to human recombinant and native 5‐HT6 receptors in rat, pig and human brain tissue

WD Hirst, JAL Minton, SM Bromidge… - British journal of …, 2000 - Wiley Online Library
SB‐258585 (4‐Iodo‐N‐[4‐methoxy‐3‐(4‐methyl‐piperazin‐1‐yl)‐phenyl]‐
benzenesulphonamide) is a high affinity ligand at 5‐HT6 receptors. It displays over 100 fold …

Synthesis of carboxylated flavonoids as new leads for LTD4 antagonists

ME Zwaagstra, H Timmerman, RS Abdoelgafoer… - European journal of …, 1996 - Elsevier
A series of 3′-and 5′-carboxylated chalcones, 6-or 8-carboxylated flavones and 6-
carboxylated flavanones,-flavanols and-flavans were prepared. The compounds were tested …

2-Alkyl-3-(1, 2, 3, 6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists

C Mattsson, C Sonesson, A Sandahl, HE Greiner… - Bioorganic & medicinal …, 2005 - Elsevier
A series of 2-alkyl-3-(1, 2, 3, 6-tetrahydropyridin-4-yl)-1H-indoles were synthesized and
evaluated for their 5-HT6 activity. The most potent agonist in this series was 5-chloro-2 …

Characterization and distribution of putative 5‐ht7 receptors in guinea‐pig brain

ZP To, DW Bonhaus, RM Eglen… - British journal of …, 1995 - Wiley Online Library
1 In the presence of (−)− cyanopindolol (1.0 μm) and sumatriptan (1.0 μm), 0.5 nM [3H]‐
carboxamidotryptamine ([3H]‐5‐CT) labelled a single population of receptors in guinea‐pig …

[引用][C] Probing the 5‐HT3 Receptor Site Using Novel Indole‐3‐glyoxylic Acid Derivatives.

SM Evans, BS HUANG, D Feng, M Gall, C Tsai… - …, 1994 - Wiley Online Library

New Benzo[h][1,6]naphthyridine and Azepino[3,2-c]quinoline Derivatives as Selective Antagonists of 5-HT4 Receptors:  Binding Profile and Pharmacological …

A Hinschberger, S Butt, V Lelong… - Journal of medicinal …, 2003 - ACS Publications
A series of benzo [h][1, 6] naphthyridine and azepino [3, 2-c] quinoline derivatives were
prepared and evaluated to determine the necessary requirements for high affinity on the 5 …