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
Interaction of beta-adrenergic antagonists with local anaesthetic acceptor sites / G.Bruschi ; M.Spaggiari; L.Tacinelli; ME.Bruschi ;M. Caroppo ; S.Gandolfi;A. Cavatorta. - In: ARCHIVES INTERNATIONALES DE PHARMACODYNAMIE ET DE THERAPIE. - ISSN 0003-9780. - 282(1986), pp. 5-15.
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