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β‐Adrenoceptors of the human myocardium: determination of β 1 and β 2 subtypes by radioligand binding
Author(s) -
Heitz Alain,
Schwartz Jean,
Velly Jeanne
Publication year - 1983
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1983.tb10062.x
Subject(s) - iodocyanopindolol , ventricle , radioligand , pindolol , antagonist , medicine , atrium (architecture) , betaxolol , chemistry , left atrium , endocrinology , biophysics , binding site , receptor , biology , intrinsic activity , timolol , biochemistry , agonist , neuroscience , glaucoma , atrial fibrillation
1 β‐Adrenoceptors of the human myocardium were investigated with binding studies using 125 iodocyanopindolol (ICYP) as ligand. 2 Inhibition of ICYP‐binding by betaxolol (a selective β 1 ‐antagonist) and ICI 118551 (a selective β 2 ‐blocking drug) resulted in non‐linear Scatchard‐plots suggesting that both β‐adrenoceptor subtypes are present in human left atrium and left ventricle. 3 Computer analysis of the data gave a β 1 /β 2 ‐adrenoceptor ratio of approximately 65:35 both for left atrium and for left ventricle.