Specific labelling of postsynaptic alpha 1 adrenoceptors in rat heart ventricle by 3H-WB 4101.
The alpha-adrenoceptor ligand, 3H-WB 4101 binds to a single population of independent sites in the rat heart ventricle. These sites are not affected by chemical sympathectomy with 6-hydroxydopamine and thus appear to be located postsynaptically. The relative order of potencies for displacement of 3H-WB 4101 binding:prazosin greater than phentolamine greater than yohimbine, is characteristic of that of the alpha 1 type of adrenoceptors. In heart ventricle 3H WB-4101 thus seems to label specifically postsynaptically located alpha 1-adrenoceptors. The significance of the specificity of this ligand is discussed with relevance to its use in the central nervous system.
D000317:Adrenergic alpha-Antagonists; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D003000:Clonidine / Q000378:metabolism; D004146:Dioxanes; D004147:Dioxins; D006892:Hydroxydopamines / Q000494:pharmacology; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D009206:Myocardium / Q000378:metabolism*; D010647:Phenyl Ethers; D051381:Rats; D011941:Receptors, Adrenergic / Q000378:metabolism*; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism*
D000317:Adrenergic alpha-Antagonists; D004146:Dioxanes; D004147:Dioxins; D006892:Hydroxydopamines; D010647:Phenyl Ethers; D011941:Receptors, Adrenergic; D011942:Receptors, Adrenergic, alpha; C010654:(2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane; D003000:Clonidine