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Binding of {H}-dihydroalprenolol and {H}-acetobutolol to human blood platelets is not related to occupancy of β-adrenoceptors
Authors:Roger Kerry  Michael C Scrutton
Abstract:Binding of {3H}-dihydroalprenolol to human platelet lysates is inhibited by (±)-propranolol and (±)-butoxamine, but less effectively by (±) practolol. (−)-Isoprenaline causes no significant inhibition of binding where stimulation of adenylate cyclase can be shown. Binding of {3H}-acetobutolol is also inhibited by (±)-propranolol. “Specific” binding of {3H}-dihydroalprenolol and {3H}-acetobutolol defined by (±) propranolol shows a non-classical saturation curve. 50% maximal binding is observed in the range 15 – 25 mM. The extent of “specific” binding is 2-fold greater for {3H}-dihydroalprenolol. Similar and rapid rates of binding of {3H}-dihydroalprenolol are observed at 4°C and 20°C. No stereoselectivity is observed for inhibition of {3H}-dihydroalprenolol binding by (+) and (−)-propranolol. Binding of {3H}-dihydroalprenolol and {3H}-acetobutolol may relate to the lipophilic character of these radioligands and does not represent interaction with β-adrenoceptors.
Keywords:Platelets   β  -Adrenoceptors   Radioligand Binding
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