Differential regulation of human cardiac beta-adrenergic and muscarinic receptors by chronic beta-adrenoceptor antagonist treatment.
In patients undergoing coronary artery bypass grafting chronic beta 1-adrenoceptor antagonist treatment increased right atrial beta 1-adrenoceptor number, did not affect beta 2-adrenoceptor number and decreased muscarinic M2-receptor number. Concomitantly, the M2-receptor-mediated negative inotropic effect of carbachol was reduced, while the beta 1-adrenoceptor-mediated positive inotropic effect of noradrenaline was not altered. The beta 2- adrenoceptor mediated positive inotropic effect of procaterol, however, was markedly enhanced. We conclude that chronic beta 1-adrenoceptor antagonist treatment increases beta 1-adrenoceptor number, sensitizes beta 2-adrenoceptor function and desensitizes M2-receptor function in the human heart.
Motomura
S
S
Biochemical Research Laboratories, University of Essen, FRG.
Deighton
N M
NM
Zerkowski
H R
HR
Khamssi
M
M
Brodde
O E
OE
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000328:Adult; D000368:Aged; D001262:Atenolol / Q000494:pharmacology; D017298:Bisoprolol; D004558:Electric Stimulation; D006801:Humans; D066298:In Vitro Techniques; D020120:Iodocyanopindolol; D008790:Metoprolol / Q000494:pharmacology; D008875:Middle Aged; D009200:Myocardial Contraction / Q000187:drug effects; D009206:Myocardium / Q000378:metabolism*; D019832:N-Methylscopolamine; D010276:Parasympatholytics; D010869:Pindolol / Q000031:analogs & derivatives; D011412:Propanolamines / Q000494:pharmacology; D011943:Receptors, Adrenergic, beta / Q000187:drug effects / Q000378:metabolism*; D011976:Receptors, Muscarinic / Q000187:drug effects / Q000378:metabolism*; D012602:Scopolamine Derivatives
D000319:Adrenergic beta-Antagonists; D010276:Parasympatholytics; D011412:Propanolamines; D011943:Receptors, Adrenergic, beta; D011976:Receptors, Muscarinic; D012602:Scopolamine Derivatives; D001262:Atenolol; D020120:Iodocyanopindolol; D010869:Pindolol; D008790:Metoprolol; D019832:N-Methylscopolamine; D017298:Bisoprolol