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螺[9,10-二氢蒽]-9,3'-吡咯烷（SpAMDA）对5-羟色胺（2A）受体高亲和力的结构决定因素

Structural determinants for high 5-HT(2A) receptor affinity of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (SpAMDA).

作者信息

Peddi Srinivas, Roth Bryan L, Glennon Richard A, Westkaemper Richard B

机构信息

Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, PO Box 980540, Richmond, VA 23298, USA.

出版信息

Bioorg Med Chem Lett. 2004 May 3;14(9):2279-83. doi: 10.1016/j.bmcl.2004.02.014.

DOI:10.1016/j.bmcl.2004.02.014
PMID:15081025
Abstract

The synthesis and 5-HT(2A) receptor affinities of ring altered derivatives of spiro[9,10-dihydroanthracene]-9,3(')-pyrrolidine (4), a structurally unique tetracyclic 5-HT(2A) receptor antagonist, are described. The characteristics of the parent compound prove to be necessary for optimal 5-HT(2A) receptor affinity. However, expansion of the size of the pyrrolidine and central rings produce compounds with reasonably high 5-HT(2A) receptor affinities. In addition, the parent compound is shown to have high 5-HT(2) receptor selectivity.

摘要

本文描述了螺[9,10-二氢蒽]-9,3'-吡咯烷（4）的环修饰衍生物的合成及其5-HT(2A)受体亲和力，螺[9,10-二氢蒽]-9,3'-吡咯烷是一种结构独特的四环5-HT(2A)受体拮抗剂。母体化合物的特性被证明是实现最佳5-HT(2A)受体亲和力所必需的。然而，吡咯烷环和中心环尺寸的扩大产生了具有相当高5-HT(2A)受体亲和力的化合物。此外，母体化合物显示出对5-HT(2)受体具有高选择性。

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