SINGLE AMINO-ACID SUBSTITUTION AFFECTS DESENSITIZATION OF THE 5-HYDROXYTRYPTAMINE TYPE-3 RECEPTOR EXPRESSED IN XENOPUS-OOCYTES

被引：120
作者：
YAKEL, JL
LAGRUTTA, A
ADELMAN, JP
NORTH, RA
机构：
[1] Vollum Institute, Oregon Health Sciences University, Portland
来源：
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA | 1993年 / 90卷 / 11期
关键词：
SITE-DIRECTED MUTAGENESIS; LIGAND-GATED ION CHANNEL;
D O I：
10.1073/pnas.90.11.5030
中图分类号：
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号：
07 ; 0710 ; 09 ;
摘要：
5-Hydroxytryptamine type 3 receptors were expressed in Xenopus oocytes from a cloned cDNA. The peak inward current evoked by 5-hydroxytryptamine (30 muM) was linearly related to the holding potential (-100 to +20 mV) and reversed near 0 mV. The inward current (at -60 mV) declined during the continued presence of 5-hydroxytryptamine with a half-time of about 2 s; this desensitization was 20 times slower in calcium-free solution. Desensitization was markedly different in channels in which Leu286 was changed by site-directed mutagenesis; this residue is thought to lie near the middle of the M2 segment. Desensitization was faster with Phe, Tyr, or Ala in this position and slower with Thr. Phe and Thr substitutions in the equivalent position of the nicotinic acetylcholine receptor have similar effects on desensitization, suggesting that the underlying conformational change might be common to ligand-gated channels.
引用
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页码：5030 / 5033
页数：4
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