Interaction of beta-adrenergic antagonists with local anaesthetic acceptor sites.
H3-dihydroalprenolol (H3-DHA) binding in isolated smooth muscle cells has been studied. Two different binding sites have been detected: a high affinity (highly specific) and a low affinity (nonspecific) binding site. Local anaesthetics are able to displace H3-DHA from nonspecific sites with a rank order of potency that mirrors their local anaesthetic activity. This finding correlates, at the molecular level, with the local anaesthetic properties of beta-blockers, as concluded from classical pharmacological experiments.
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000779:Anesthetics, Local / Q000378:metabolism*; D000818:Animals; D004082:Dihydroalprenolol; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains; D011955:Receptors, Drug / Q000378:metabolism*
D000319:Adrenergic beta-Antagonists; D000779:Anesthetics, Local; D011955:Receptors, Drug; D004082:Dihydroalprenolol