98788-22-8Relevant academic research and scientific papers
1-Aryl-1,4-dihydro-3(2H)-isoquinolinones: Two modes of interaction with 5-HT(1A) receptors
Mokrosz,Duszynska,Wesolowska,Borycz,Chojnacka-Wojcik,Karolak-Wojciechowska
, p. 58 - 68 (2007/10/03)
Two series of 1-aryl-1,4-dihydro-3(2H)-isoquinoline derivatives were synthesized, and their in vitro and in vivo properties at 5-HT(1A) and 5- HT(2A) receptors were evaluated. In was shown that series a, containing a 1- (m-chlophenyl)piperazine fragment, interacts with 5-HT(1A) receptors in two different modes: as an ordinary 4-substituted 1-arylpiperazine and as a pseudo one. Series b, with a 1,2,3,4-tetrahydroisoquinoline moiety, binds to the receptor thanks to a pseudo 1-arylpiperazine fragment. Regardless of the mode of interaction, both those series demonstrated 5-HT(1A) receptor antagonistic properties in animal models. Different in vivo properties of 2b, due to a 7-methoxy substituent, indicate that the isoquinolinone portion also interacts with 5-HT(1A) receptors.
