INHIBITION OF DIPTERAN LARVAL NEUROMUSCULAR SYNAPTIC TRANSMISSION BY ANALOGS OF PHILANTHOTOXIN-4.3.3 - A STRUCTURE ACTIVITY STUDY

被引：17

作者：

BENSON, JA

SCHURMANN, F

KAUFMANN, L

GSELL, L

PIEK, T

机构：

[1] CIBA GEIGY AG, DIV PLANT PROTECT, CH-4002 BASEL, SWITZERLAND

[2] UNIV AMSTERDAM, DEPT PHARMACOL, 1105 AZ AMSTERDAM, NETHERLANDS

来源：

COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY C-TOXICOLOGY & PHARMACOLOGY | 1992年 / 102卷 / 02期

关键词：

D O I：

10.1016/0742-8413(92)90110-S

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 wasp toxin composed of a polyamine chain, an aromatic amino acid (tyrosyl) nucleus and an aliphatic (butanoic) acid was studied, together with 33 structural analogues, at the glutamatergic neuromuscular synapse in larvae of the house fly, Musca domestica. 2. Shortening of the polyamine or the aliphatic acid chain, or removing the aromatic nucleus caused a decrease in potency. 3. An increase in potency was obtained by elongating the molecule in any of several directions: elongation of the polyamine chain with amine containing groups, by iodination of the aromatic moiety and by aliphatic or aromatic elongation of the butanoic acid.

引用

页码：267 / 272

页数：6

共 34 条

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[2]

BENSON JA, 1991, IN PRESS PHYSL ACTIO

[3]

BLAGBROUGH IS, 1989, J PHARM PHARMACOL, V41, P95

[4] STRUCTURE-ACTIVITY-RELATIONSHIPS OF ANALOGS OF THE WASP TOXIN PHILANTHOTOXIN - NONCOMPETITIVE ANTAGONISTS OF QUISQUALATE RECEPTORS [J].