STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF CENTRAL-NERVOUS-SYSTEM AGENTS .13. RIAZOL-1-YL)PROPYL]-1-(2-METHOXYPHENYL)PIPERAZINE, A NEW PUTATIVE 5-HT1A RECEPTOR ANTAGONIST, AND ITS ANALOGS

Authors
MOKROSZ JL PALUCHOWSKA MH CHOJNACKAWOJCIK E FILIP M CHARAKCHIEVAMINOL S DERENWESOLEK A MOKROSZ MJ
Citation
Jl. Mokrosz et al., STRUCTURE-ACTIVITY RELATIONSHIP STUDIES OF CENTRAL-NERVOUS-SYSTEM AGENTS .13. RIAZOL-1-YL)PROPYL]-1-(2-METHOXYPHENYL)PIPERAZINE, A NEW PUTATIVE 5-HT1A RECEPTOR ANTAGONIST, AND ITS ANALOGS, Journal of medicinal chemistry, 37(17), 1994, pp. 2754-2760
Citations number
33
Categorie Soggetti
Chemistry Medicinal
Journal title
Journal of medicinal chemistry → ACNP
ISSN journal
00222623
Volume
37
Issue
17
Year of publication
1994
Pages
2754 - 2760
Database
ISI
SICI code
0022-2623(1994)37:17<2754:SRSOCA>2.0.ZU;2-Y
Abstract
A new set of 4-alkyl-1-(o-methoxyphenyl)piperazines containing a termi nal benzotriazole fragment were synthesized, and their 5-HT1A and 5-HT 2 affinity was determined. It was shown that the benzotriazole moiety contributes to both the 5-HT1A and 5-HT2 receptor affinity. It was dem onstrated in several behavioral models that triazol-1-yl)propyl]-1-(2- methoxyphenyl)piperazine (11) is a new, potent presynaptic and postsyn aptic 5-HT1A receptor antagonist. However, it is not selective For 5-H T1A versus alpha(1) receptors.