High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor

Authors
Modica, M Santagati, M Santagati, A Russo, F Cagnotto, A Goegan, M Mennini, T
Citation
M. Modica et al., High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor, BIOORG MED, 10(10), 2000, pp. 1089-1092
Citations number
8
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
10
Year of publication
2000
Pages
1089 - 1092
Database
ISI
SICI code
0960-894X(20000515)10:10<1089:HPASAD>2.0.ZU;2-E
Abstract
This paper reports the synthesis and affinities on the 5HT(1A) versus the a lpha(1)A receptors of new arylpiperazinylalkylthiothienopyrimidine and thia diazole derivatives 16-24. Arylpiperazines 16-23 show affinities values in the nanomolar range for the 5HT(1A) receptor. The compound 16 is highly pot ent (K-i 0.26 nM, selectivity 28), the derivatives 20 and 21 are less poten t, but highly selective (K-i 9.40 and 5.06 nM, selectivity 207 and 73, resp ectively). (C) 2000 Elsevier Science Ltd. All rights reserved.