159671-82-6Relevant articles and documents
New benzocycloalkylpiperazines, potent and selective 5-HT(1A) receptor ligands
Ahmad, Youssef El,Laurent, Elisabeth,Maillet, Philippe,Talab, Akram,Teste, Jean Fran?ois,Dokhan, Raymond,Tran, Gilles,Ollivier, Roland
, p. 952 - 960 (2007/10/03)
A series of 1-(benzocycloalkyl)-4-(benzamidoalkyl)piperazine derivatives was prepared in order to obtain compounds with a high affinity and selectivity for 5-HT(1A) receptors. The modifications of aromatic substituents, the length of the alkyl chain, and the size of the ring were explored. Most of N-(1,2,3,4-tetrahydronaphthyl)-N'- (benzamidoethyl)piperazines (32-37) were bound to 5-HT(1A) receptors in a nanomolar range and presented a high degree of selectivity. After resolution, levorotatory enantiomers showed affinity and selectivity higher than those of dextrorotatory ones for 5-HT(1A) sites. The agonist type activity of selected derivatives was also confirmed in vitro on the inhibition of the activation of adenylate cyclase induced by forskolin and, in vivo, on the induction of the lower lip retraction in rats.