Localization and characterization of two propranolol resistant (-) [125I]cyanopindolol binding sites in rat skeletal muscle.
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 microM) to block beta 1- and beta 2-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 by (+/-)-, (-)- and (+)-alprenolol (20 microM), tertatolol (1 microM), BRL 37344 (2-20 microM), (-)-isoprenaline (100 microM), phentolamine (10 microM) and haloperidol (250 microM) but not ICI 118,551 (70 nM), CGP 20712A (100 nM), (+)-isoprenaline (100 microM), pindolol (2 microM), cimaterol (100 microM) or serotonin (10 microM). Stereoselectivity for the optical isomers of alprenolol was displayed in the soleus muscle only. Highly localized binding was inhibited by serotonin (10 microM), (-)- and (+)-isoprenaline (100 microM) and phentolamine (10 microM).
Molenaar
P
P
Department of Pharmacology, University of Melbourne, Victoria, Australia.
Roberts
S J
SJ
Kim
Y S
YS
Pak
H S
HS
Sainz
R D
RD
Summers
R J
RJ
D000818:Animals; D001345:Autoradiography; D004351:Drug Resistance; D005260:Female; D066298:In Vitro Techniques; D020120:Iodocyanopindolol; D008297:Male; D009132:Muscles / Q000033:anatomy & histology / Q000187:drug effects / Q000378:metabolism*; D009210:Myofibrils / Q000187:drug effects / Q000201:enzymology; D010869:Pindolol / Q000031:analogs & derivatives* / Q000494:pharmacology; D011433:Propranolol / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects / Q000378:metabolism; D011943:Receptors, Adrenergic, beta / Q000187:drug effects*; D011954:Receptors, Dopamine / Q000187:drug effects / Q000378:metabolism; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism
D011942:Receptors, Adrenergic, alpha; D011943:Receptors, Adrenergic, beta; D011954:Receptors, Dopamine; D011985:Receptors, Serotonin; D020120:Iodocyanopindolol; D011433:Propranolol; D010869:Pindolol