当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.

Novel, potent, and selective quinoxaline-based 5-HT(3) receptor ligands. 1. Further structure-activity relationships and pharmacological characterization.

Abstract：

:We investigated the pharmacological profile of a novel series of quinoxaline-based 5-HT(3) receptor ligands bearing an extra basic moiety on the piperazine N-4. High affinity and selectivity were dependent on the electronic properties of the substituents, and at cardiac level 3a and 3c modulated chronotropy but not inotropy. In von Bezold-Jarisch reflex test 3a-c were partial agonists while 3i was a full agonist. Preliminary pharmacokinetic studies indicated that 3a is a brain penetrating agent.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Butini S,Budriesi R,Hamon M,Morelli E,Gemma S,Brindisi M,Borrelli G,Novellino E,Fiorini I,Ioan P,Chiarini A,Cagnotto A,Mennini T,Fracasso C,Caccia S,Campiani G

doi

10.1021/jm901126m

subject

Has Abstract

pub_date

2009-11-12 00:00:00

pages

6946-50

issue

21

eissn

0022-2623

issn

1520-4804

journal_volume

52

pub_type

杂志文章

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