In vitro selectivity of agonists and antagonists for beta 1- and beta 2-adrenoceptor subtypes in rat brain.
A radioreceptor binding assay was developed to determine the selectivity of beta-adrenoceptor agents in rat brain. This was achieved by using the highly selective unlabelled antagonists CGP 20712A and ICI 118-551 to block beta 1- or beta 2-sub-populations respectively in rat cerebral cortex membranes. This permitted the selective labelling of beta-adrenoceptors with the antagonist (-)-[125I]pindolol. Using this method, compounds could be routinely screened and selectivity profiles for binding in the CNS determined with a high degree of sensitivity and resolution.
D000318:Adrenergic beta-Agonists / Q000494:pharmacology*; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000818:Animals; D001665:Binding Sites; D001923:Brain Chemistry / Q000187:drug effects*; D002540:Cerebral Cortex / Q000378:metabolism; D002976:Clenbuterol / Q000494:pharmacology; D007093:Imidazoles / Q000494:pharmacology; D066298:In Vitro Techniques; D008297:Male; D010869:Pindolol / Q000378:metabolism; D011412:Propanolamines / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011943:Receptors, Adrenergic, beta / Q000187:drug effects* / Q000378:metabolism; D013237:Stereoisomerism
D000318:Adrenergic beta-Agonists; D000319:Adrenergic beta-Antagonists; D007093:Imidazoles; D011412:Propanolamines; D011943:Receptors, Adrenergic, beta; C026777:ICI 118551; D010869:Pindolol; C049763:CGP 20712A; D002976:Clenbuterol