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Binding of {3H}-dihydroalprenolol and {3H}-acetobutolol to human blood platelets is not related to occupancy of β-adrenoceptors

Authors
Journal
Thrombosis Research
0049-3848
Publisher
Elsevier
Publication Date
Volume
29
Issue
6
Identifiers
DOI: 10.1016/0049-3848(83)90213-x
Keywords
  • Platelets
  • β-Adrenoceptors
  • Radioligand Binding

Abstract

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.

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