482647-39-2Relevant academic research and scientific papers
Synthesis and structure-activity relationships of new arylpiperazines: Para substitution with electron-withdrawing groups decrease binding to 5-HT1A and D2A receptors
Santana, Lourdes,Uriarte, Eugenio,Fall, Yagamare,Teijeira, Marta,Teran, Carmen,Garcia-Martinez, Emilia,Tolf, Bo-Ragnar
, p. 503 - 510 (2007/10/03)
Compounds in which N-phenylpiperazines were linked by a propyloxy chain to position 6 or 7 of a coumarin ring were designed and synthesised, and their affinities for 5-HT1A and D2A receptors were determined by radioligand binding assays. The influence of para substitution in the phenyl ring, substitution at position 4 of the coumarin system, and the coumarin position at which the piperazinylalkyl chain is linked was explored. Electron-withdrawing phenyl ring substituents para to the piperazine strongly reduced activity at both receptors. Binding at 5HT1A was influenced by the bulk of substituents at position 4 of the coumarin system, and binding at D2A by their electronic properties. Neither binding affinity was significantly affected by whether the piperazinylalkyl chain was inserted at position 6 or 7 of the coumarin system.
