Atypical characteristics of the beta-adrenoceptor mediating cyclic AMP generation and lipolysis in the rat adipocyte.
The characteristics of the rat epidydimal adipocyte beta-adrenoceptor have been examined using lipolysis and cyclic AMP accumulation in adipocytes as well as adenylate cyclase activity in fat cell membranes. The pA2 values corrected for binding to bovine serum albumin of the selective antagonists betaxolol (beta 1-selective) and ICI 118.551 (beta 2-selective) against noradrenaline or fenoterol-stimulated lipolysis were indicative of an atypical beta-adrenoceptor associated with the lipolytic response. Antagonism of isoprenaline-stimulated cyclic AMP accumulation in whole cells and adenylate cyclase activity in membranes yielded pA2 values to betaxolol, ICI 118.551 and (-)-propranolol, which suggested that the atypical beta-adrenoceptor was coupled to adenylate cyclase. Comparisons of the Ki values obtained in binding studies using [125I]-cyanopindolol with pA2 values obtained in adenylate cyclase experiments suggest that the typical beta 1-receptor identified with radioligand binding studies is not the only receptor site mediating stimulation of adenylate cyclase activity and lipolysis.
Bojanic
D
D
Jansen
J D
JD
Nahorski
S R
SR
Zaagsma
J
J
D000273:Adipose Tissue / Q000166:cytology / Q000378:metabolism*; D000818:Animals; D015784:Betaxolol; D000242:Cyclic AMP / Q000096:biosynthesis / Q000378:metabolism*; D004822:Epididymis / Q000166:cytology / Q000378:metabolism*; D005280:Fenoterol / Q000494:pharmacology; D007545:Isoproterenol / Q000494:pharmacology; D008066:Lipolysis / Q000187:drug effects*; D008297:Male; D009638:Norepinephrine / Q000494:pharmacology; D011412:Propanolamines / Q000494:pharmacology; D011433:Propranolol / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011943:Receptors, Adrenergic, beta / Q000502:physiology*
D011412:Propanolamines; D011943:Receptors, Adrenergic, beta; D005280:Fenoterol; C026777:ICI 118551; D011433:Propranolol; D000242:Cyclic AMP; D007545:Isoproterenol; D015784:Betaxolol; D009638:Norepinephrine