THE PHYSIOLOGICAL ACTION OF ANALOGS OF PHILANTHOTOXIN-4.3.3 AT INSECT NICOTINIC ACETYLCHOLINE-RECEPTORS

被引:17
作者
BENSON, JA
KAUFMANN, L
HUE, B
PELHATE, M
SCHURMANN, F
GSELL, L
PIEK, T
机构
[1] CIBA GEIGY AG,DIV PLANT PROTECT,CH-4002 BASEL,SWITZERLAND
[2] UNIV ANGERS,NEUROPHYSIOL LAB,CNRS,URA 611,F-49045 ANGERS,FRANCE
[3] UNIV AMSTERDAM,DEPT PHARMACOL,1105 AZ AMSTERDAM,NETHERLANDS
来源
COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY C-PHARMACOLOGY TOXICOLOGY & ENDOCRINOLOGY | 1993年 / 105卷 / 02期
关键词
D O I
10.1016/0742-8413(93)90212-4
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
1. The blocking action of delta-philanthotoxin (PhTX-4.3.3), a polyamine amide wasp toxin, and 33 structural analogues was studied at the nicotinic acetylcholine receptor of isolated neuronal somata from locust thoracic ganglia and at the cockroach cercal nerve-giant interneuron nicotinic cholinergic synapse. 2. A comparison of the structure-activity relationships reported here for the locust somal and cockroach synaptic nicotinic receptors and for the glutamatergic neuromuscular synapses of housefly larvae reported previously suggests a generally similar pharmacology for the channel-blocking action at ligand-activated ion channels, but with differences that might be due to variation in accessibility between synaptic receptors and those on the neuronal somata or to genuine divergence in ligand-activated ion channel pharmacology.
引用
收藏
页码:303 / 310
页数:8
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