Localization and characterization of two propranolol resistant (-) [125I]cyanopindolol binding sites in rat skeletal muscle

Peter Molenaar, Susan J. Roberts, Yong S. Kim, Helen S. Pak, Robert D. Sainz, Roger J. Summers

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Abstract

Autoradiographic studies were performed in sections of rat gastrocnemius, plantaris and soleus muscle bundles with (-)-[125I]cyanopindolol (59-69 pM) in the presence of (-)-propranolol (1 μM) to block β1- and β2-adrenoceptors. Two distinct populations of binding sites remained, one evenly distributed over the muscle bundles and the other localized in discrete patches. Evenly distributed binding was highest in the soleus muscle and inhibited (±), (-)- and (+)-alprenolol (20 μM), tertatolol (1 μM), BRL 37344 (2-20 μM), (-)-isoprenaline (100 μM), phentolamine (10 μM) and haloperidol (250 μM) but not ICI 118,551 (70 nM), CGP 20712A (100 nM), (+)-isoprenaline (100 μM), pindolol (2 μM), cimaterol (100 μM) or serotonin (10 μM). Stereoselectivity for the optical isomers of alprenolol was displayed in the soleus muscle only. Highly localized binding was inhibited by serotonin (10 μM), (-)- and (+)-isoprenaline (100 μM) and phentolamine (10 μM).

Original languageEnglish
Pages (from-to)257-262
Number of pages6
JournalEuropean Journal of Pharmacology
Volume209
Issue number3
DOIs
Publication statusPublished - 17 Dec 1991

Keywords

  • (-)-[I]cyanopindolol
  • 5-HT (5-hydroxytryptamine, serotonin)
  • Alprenolol
  • BRL 37344
  • Skeletal muscle
  • β-Adrenoceptors (atypical)

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