The rat lipolytic β-adrenoceptor: Studies using novel β-adrenoceptor agonists

Wilson, Campbell; Wilson, Shelagh; Piercy, Valerie; Sennitt, Matthew V.; Arch, Jonathan R.S.

doi:10.1016/0014-2999(84)90007-4

Cited by 155 publications

(89 citation statements)

References 20 publications

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“…These ratios suggested either a better coupling efficiency of the murine P3-adrenoceptor to adenylyl cyclase or a better intrinsic activity for isoprenaline at the murine P3 site. We therefore evaluated the stoichiometry of receptor-Gs-adenylyl cyclase interactions in transfected CHO cells, according to Alousi et al (1991) BRL 37344, the reference agonist for the atypical P-site Wilson et al, 1984), possessed a cyclase stimulation constant 38 fold higher for the murine than for the human subclone, with a BRL 37344 potency relative to (-)-isoprenaline (Kact(Iso)/K(BRL)) of 11.3 (Feve et al, 1991 -o-4t _+ +l +l +l +l +l +l +l +l +l +l +l +l +1 +1 +1 +1 +1 +1 The P3-adrenoceptor as the adipose tissue atypical P site The P3-adrenoceptor displays six pharmacological properties, strikingly different from those of the Pj-and P2-receptors, and which are shared with the atypical P-adrenoceptor of adipose tissue.…”

Section: Resultsmentioning

confidence: 99%

Mediation of most atypical effects by species homologues of the β₃‐adrenoceptor

Blin

Nahmias

Drumare

et al. 1994

British J Pharmacology

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1 A wide panel of compounds acting on 1-adrenoceptors active either in mammalian heart or in rodent digestive tract 3 This pharmacological analysis further established that the 13-adrenoceptor is the prototype of the adipose tissue atypical P-adrenoceptor, since these receptors share a number of pharmacological properties which differ strikingly from those of P13-and 132-adrenoceptors: low affinities for conventional 13-adrenoceptor agonists and antagonists, high potencies for novel compounds active in adipose tissues, partial agonistic activites for several PI/p2-antagonists. 4 Although the pharmacological profiles of the human and murine 133-receptor were very similar, some quantitative or even qualitative differences were observed for particular compounds such as propranolol, which exhibited weak and partial agonistic effects at the human 133-receptors and antagonistic effects at the murine 13-receptors. These differences may result from key amino-acid substitutions between the human and the murine P3-receptor sequences, which may alter the binding site or signal processing. 5 Compounds active on atypical P-sites of other tissues such as heart and digestive tract were also potent on the P3-adrenoceptor expressed in Chinese hamster ovary cells, suggesting that this receptor mediates most of the atypical properties described in various tissues, and that differences in ligand effects may result from tissue-related specificities.

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Section: Resultsmentioning

confidence: 99%

Mediation of most atypical effects by species homologues of the β₃‐adrenoceptor

Blin

Nahmias

Drumare

et al. 1994

British J Pharmacology

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show abstract

“…Following the discovery that functional adrenoceptors of the putative p3-sub-type are present in rat adipose tissue Wilson et al, 1984), the control of lipolysis by P-adrenoceptors has been re-examined in a number of different laboratory animal species. A few comparative studies have been conducted on human adipose tissue (Hollenga et al, 1991a;Langin et al, 1991), but to our knowledge there have been no previous studies using adipose tissue from domestic animals.…”

Section: Introductionmentioning

confidence: 99%

Classical and atypical binding sites for β‐adrenoceptor ligands and activation of adenylyl cyclase in bovine skeletal muscle and adipose tissue membranes

Sillence

Matthews

1994

British J Pharmacology

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“…When expressed in this way, high concentrations of antagonists had no effect on the increase in size of the current produced by (-)-Iso but generally depressed basal calcium current size themselves. (-)-Propranolol up to 10 JM was without significant antagonism; this drug has a high affinity for type PBand type P2-receptors, its pA2 being in the range 8-9 Wilson et al, 1984) although its affinity for P3-receptors is somewhat less, pA2 about 7 Bond & Clarke, 1988). Atenolol, a. Pi-selective antagonist with a pA2 of 6 to 7 (O'Donnell & Wanstall, 1983), the PI-selective antagonst CGP 20712A with a pA2 greater than 9 (Kaumann, 1986), and the antagonist ICI 118551 with a pA2 for P2-receptors in the range 8-10 (O'Donnell & Wanstall, 1983; in concentrations up to 10 .M did not significantly antagonize the effect of (-)-Iso or (-)-NA on ICa (Figure 3a,b,c).…”

Section: Resultsmentioning

confidence: 89%