Document Report Card

ID: ALA1122904

Journal: J Med Chem

Title: Bioactive conformation of 1-arylpiperazines at central serotonin receptors.

Authors: Huff JR, King SW, Saari WS, Springer JP, Martin GE, Williams M.

Abstract: A number of 1-arylpiperazines have been characterized as direct-acting serotonin agonists. Conformational parameters of this class that may affect receptor recognition and binding have been examined through the analysis of X-ray data and synthesis of rigid analogues. Radioligand binding studies indicate that 2,3,4,4a,5,6-hexahydro-9-(trifluoromethyl)-1H-pyrazino[1,2-a]quinoline, an arylpiperazine that mimics the X-ray conformation of the serotonin agonist 1-(6-chloropyrazin-2-yl)piperazine, exhibits high affinity for serotonin receptors, suggesting that the two rings of 1-arylpiperazines are relatively coplanar in the bioactive conformation.

CiteXplore: 4009617

DOI: 10.1021/jm00145a017