Linked Life Data

2552275

Source:http://linkedlifedata.com/resource/pubmed/id/2552275

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pubmed-article:2552275pubmed:abstractTextThe 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.lld:pubmed
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pubmed-article:2552275pubmed:articleTitleFormamidine pesticides and alpha 2-adrenoceptors: studies with amitraz and chlordimeform in rats and development of a radioreceptor binding assay.lld:pubmed
pubmed-article:2552275pubmed:affiliationDepartment of Environmental Health, University of Washington, Seattle 98195.lld:pubmed
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pubmed-article:2552275pubmed:publicationTypeResearch Support, U.S. Gov't, P.H.S.lld:pubmed
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