当5-HT3B亚基与5-HT3A受体共表达时，它会使对印防己毒素的敏感性降低。

The 5-HT3B subunit confers reduced sensitivity to picrotoxin when co-expressed with the 5-HT3A receptor.

作者信息

Das Paromita, Dillon Glenn H

机构信息

Department of Pharmacology and Neuroscience, University of North Texas Health Science Center, 3500 Camp Bowie Boulevard, Fort Worth, TX 76107, USA.

出版信息

Brain Res Mol Brain Res. 2003 Nov 26;119(2):207-12. doi: 10.1016/j.molbrainres.2003.09.003.

DOI:10.1016/j.molbrainres.2003.09.003

PMID:14625088

Abstract

There are currently no known agents that display selectivity between homomeric 5-hydroxytryptamine type 3A (5-HT3A) and heteromeric 5-HT3A/3B receptors. In the present study, we show that the CNS convulsant picrotoxin selectively interacts with 5-HT3A receptors. In whole-cell patch clamp recordings, the inhibitory effect of PTX was reduced 100-fold in heteromeric mouse 5-HT3A/3B receptors, compared to homomeric 5-HT3A receptors. Picrotoxin should prove to be a useful probe for determining the presence of homomeric vs. heteromeric 5-HT3 receptors in both native tissue and recombinant receptor preparations.

摘要

目前尚无已知药物能在同聚体5-羟色胺3A型（5-HT3A）受体和异聚体5-HT3A/3B受体之间表现出选择性。在本研究中，我们表明中枢神经系统惊厥剂印防己毒素能选择性地与5-HT3A受体相互作用。在全细胞膜片钳记录中，与同聚体5-HT3A受体相比，印防己毒素对异聚体小鼠5-HT3A/3B受体的抑制作用降低了100倍。印防己毒素应可证明是一种用于确定天然组织和重组受体制剂中同聚体与异聚体5-HT3受体存在情况的有用探针。