Mokrosz J L, Strekowski L, Duszyńska B, Harden D B, Mokrosz M J, Bojarski A J
Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, Kraków.
Pharmazie. 1994 Nov;49(11):801-6.
The 5-HT1A and 5-HT2A receptor affinity of model 1-(2-pyrimidinyl)-piperazine derivatives 15-21 and 23-32 has been determined. 2-(N-Methylpiperazino)-4,6-di(2-thienyl)pyrimidine 26 is a new, highly active and selective 5-HT2A receptor ligand. The topography of a molecule and the stereoelectronic effects of the thiophene rings are the major factors responsible for the high affinity and selectivity of 26 towards 5-HT2A sites.
已测定了1-(2-嘧啶基)-哌嗪衍生物15 - 21和23 - 32的5 - HT1A和5 - HT2A受体亲和力。2-(N - 甲基哌嗪基)-4,6 - 二(2 - 噻吩基)嘧啶26是一种新型、高活性且选择性的5 - HT2A受体配体。分子的拓扑结构和噻吩环的立体电子效应是导致26对5 - HT2A位点具有高亲和力和选择性的主要因素。
