Westkaemper R B, Runyon S P, Savage J E, Roth B L, Glennon R A
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond 23298, USA.
Bioorg Med Chem Lett. 2001 Feb 26;11(4):563-6. doi: 10.1016/s0960-894x(01)00010-5.
Comparison of the serotonin 5-HT2A receptor affinities of a parallel series of structural analogues of the novel ligand 9-aminomethyl-9,10-dihydroanthracene (AMDA) and a structurally similar prototypical tricyclic amine cyproheptadine suggests that the two agents bind to the receptor in different fashions. Examination of ligand-receptor model complexes supports the experimental data and suggests a potential origin for the differences in binding modes.
新型配体9-氨基甲基-9,10-二氢蒽(AMDA)的一系列结构类似物与结构相似的原型三环胺赛庚啶的血清素5-HT2A受体亲和力比较表明,这两种药物以不同方式与受体结合。对配体-受体模型复合物的研究支持了实验数据,并揭示了结合模式差异的潜在原因。