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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
1989-11-8
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pubmed:abstractText |
The interaction of the formamidine pesticides chlordimeform (CDM) and amitraz (AMZ) with rat brain alpha2-adrenoceptors was investigated. Both compounds inhibited the binding of 3H-clonidine and 3H-yohimbine in vitro with IC50 values of 62-68 microM (CDM) and 95-110 nM (AMZ). In vivo administration of AMZ and CDM caused a dose-dependent inhibition of 3H-clonidine binding in rat forebrain. The inhibition was short-lasting (24 hr) following CDM administration, while after AMZ recovery of 3H-clonidine binding occurred only after 72 hr. Good correlations were found between inhibition of brain 3H-clonidine binding by the formamidines and "plasma equivalents" of these compounds and/or their biologically active metabolites, as measured by a new radioreceptor assay. These results suggest that 1) formamidines can interact in vivo with brain alpha 2-adrenoceptors when administered at doses previously shown to cause toxic effects on the central nervous system: and 2) this effect is reversible, both in vivo and in vitro, and appears to be linked to the presence of the formamidines and/or their active metabolites at the receptor sites.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Amidines,
http://linkedlifedata.com/resource/pubmed/chemical/Chlorphenamidine,
http://linkedlifedata.com/resource/pubmed/chemical/Clonidine,
http://linkedlifedata.com/resource/pubmed/chemical/Insecticides,
http://linkedlifedata.com/resource/pubmed/chemical/Pesticides,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Adrenergic, alpha,
http://linkedlifedata.com/resource/pubmed/chemical/Toluidines,
http://linkedlifedata.com/resource/pubmed/chemical/Yohimbine,
http://linkedlifedata.com/resource/pubmed/chemical/amitraz
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pubmed:status |
MEDLINE
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pubmed:issn |
0892-0362
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
11
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
405-11
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pubmed:dateRevised |
2009-10-26
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pubmed:meshHeading |
pubmed-meshheading:2552275-Amidines,
pubmed-meshheading:2552275-Animals,
pubmed-meshheading:2552275-Brain Chemistry,
pubmed-meshheading:2552275-Chlorphenamidine,
pubmed-meshheading:2552275-Clonidine,
pubmed-meshheading:2552275-Dose-Response Relationship, Drug,
pubmed-meshheading:2552275-Insecticides,
pubmed-meshheading:2552275-Male,
pubmed-meshheading:2552275-Pesticides,
pubmed-meshheading:2552275-Radioligand Assay,
pubmed-meshheading:2552275-Rats,
pubmed-meshheading:2552275-Rats, Inbred Strains,
pubmed-meshheading:2552275-Receptors, Adrenergic, alpha,
pubmed-meshheading:2552275-Toluidines,
pubmed-meshheading:2552275-Yohimbine
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pubmed:articleTitle |
Formamidine pesticides and alpha 2-adrenoceptors: studies with amitraz and chlordimeform in rats and development of a radioreceptor binding assay.
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pubmed:affiliation |
Department of Environmental Health, University of Washington, Seattle 98195.
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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