Beta-adrenoceptors and human skeletal muscle characterisation of receptor subtype and effect of age.
1. Rectus abdominis muscle biopsies were obtained from 28 patients undergoing abdominal surgery. In membranes prepared from these biopsies beta-adrenoceptor binding was examined. The apparent affinity (KD) and the density (Bmax) of the receptors for the radioligand (-)-[125I]cyanopindolol were 28.5 +/- 2.7 (pM) and 25.9 +/- 2.1 (fmol mg-1 protein) (mean +/- s.e. mean) respectively. In forceps biopsies from vastus lateralis muscle from four healthy volunteers the values for KD and Bmax were 22.5 +/- 4.4 (pM) and 16.4 +/- 2.2 (fmol mg-1 protein). The binding characteristics for the radioligand were similar in the biopsies from the two muscle sites. 2. Inhibition of the radioligand binding by the selective beta 2-adrenoceptor antagonist ICI 118551 (KI = 117 +/- 45 nM) and selective beta 1-adrenoceptor antagonist metoprolol (KI = 15229 +/- 5046 nM) suggests the dominance of beta 2-adrenoceptor subtype in human skeletal muscle. 3. There were no significant differences in the skeletal muscle beta-adrenoceptor densities or affinities between the young and older patients.
Elfellah
M S
MS
Department of Materia Medica, University of Glasgow.
Dalling
R
R
Kantola
I M
IM
Reid
J L
JL
D000293:Adolescent; D000319:Adrenergic beta-Antagonists / Q000494:pharmacology; D000328:Adult; D000368:Aged; D000375:Aging / Q000378:metabolism*; D001667:Binding, Competitive / Q000187:drug effects; D005260:Female; D006801:Humans; D008297:Male; D008790:Metoprolol / Q000494:pharmacology; D008875:Middle Aged; D009132:Muscles / Q000378:metabolism*; D011412:Propanolamines / Q000494:pharmacology; D011869:Radioligand Assay; D011943:Receptors, Adrenergic, beta / Q000032:analysis / Q000378:metabolism*
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; D011943:Receptors, Adrenergic, beta; C026777:ICI 118551; D008790:Metoprolol