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Glutamate receptor inhibitors as potential insecticides
M E Eldefrawi1, N A Anis, A T Eldefrawi
1Department of Pharmacology and Experimental Therapeutics, University of Maryland, School of Medicine, Baltimore 21201.
Archives of Insect Biochemistry and Physiology
|January 1, 1993
Summary
Philanthotoxins (PhTXs) block insect glutamate receptors, but derivatives lack selectivity for insecticide development. Further structural modifications may yield effective insect control agents targeting these receptors.
Area of Science:
- Neuroscience
- Pharmacology
- Entomology
Background:
- Philanthotoxin (PhTX) from digger wasp venom targets insect glutamate receptors.
- Glutamate receptor blockers show potential for selective insect control.
Purpose of the Study:
- Synthesize and test PhTX derivatives as inhibitors of insect skeletal muscle glutamate receptors.
- Investigate structure-activity relationships for PhTX derivatives.
Main Methods:
- Structure-activity relationship (SAR) studies of synthesized PhTX derivatives.
- Testing PhTX derivatives for potency against insect glutamate receptors.
Main Results:
- Shortening polyamine chain length or nitrogen quaternization reduced PhTX potency.
- Bulky hydrophobic anchoring groups and 3,5-diiodo-tyrosyl moiety increased PhTX potency.
- PhTX derivatives inhibited various glutamate and nicotinic receptors, showing low selectivity.
Conclusions:
- Current PhTX derivatives are unsuitable as insecticides due to low selectivity and poor penetration.
- Insect skeletal muscle glutamate receptors remain a viable target for insecticide development.
- Significant structural modifications of PhTX may lead to potential insecticidal compounds.