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HERO ID
7572751
Reference Type
Journal Article
Title
Structure and insecticidal activity of picrotoxinin analogs
Author(s)
Miller, TA; Maynard, M; Kennedy, JM; ,
Year
1979
Is Peer Reviewed?
1
Journal
Pesticide Biochemistry and Physiology
ISSN:
0048-3575
EISSN:
1095-9939
Publisher
ACADEMIC PRESS INC JNL-COMP SUBSCRIPTIONS
Location
SAN DIEGO
Volume
10
Issue
2
Page Numbers
128-136
Language
English
DOI
10.1016/0048-3575(79)90014-2
Web of Science Id
WOS:A1979GQ38400002
URL
https://linkinghub.elsevier.com/retrieve/pii/0048357579900142
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Abstract
Picrotoxinin, a convulsant in mammals, was nontoxic when topically applied on whole house flies. When synergized with piperonyl butoxide, the topical LD50 of picrotoxinin on house flies was 6.50 μg/g or 260 times less toxic on house flies than the synergized insecticide, carbofuran, a carbamate cholinesterase inhibitor. When perfused on the isolated thoracic ganglion of house fly, picrotoxinin was less potent in producing convulsions than carbofuran; however, when assayed on the desheathed thoracic ganglion, picrotoxin was more potent than carbofuran. This suggested a substantial barrier to picrotoxinin preventing diffusion into the house fly central nervous system. Of several picrotoxinin analogs synthesized the 2-iodo,4-isopropyl, 6-methylenebromidecyclohexane-γ-lactone was the most potent convulsant. © 1979.
Keywords
carbofuran; drug; drug analog; pesticide; picrotoxin; picrotoxinin; piperonyl butoxide; animal experiment; central nervous system; convulsion; dihydropicrotoxinin; drug comparison; drug concentration; drug response; house fly; in vitro study; intoxication; invertebrate; nervous system; neurotoxicity; picrotin; picrotoxinin h 3; regional perfusion; structure activity relation; topical drug administration; toxicity
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