Skip to main content
NCBI home page
Biochemical Journal logoLink to Biochemical Journal
. 1988 Jun 15;252(3):679–682. doi: 10.1042/bj2520679

Evidence of functional alpha 2-adrenergic receptors in adult-rat adipocytes by using the agonist UK 14304.

M C Rebourcet 1, C Carpéné 1, M Lavau 1
PMCID: PMC1149202  PMID: 2901830

Abstract

The aim of this study was to re-assess whether alpha 2-adrenergic receptors were present in rat adipocytes, by using UK 14304, a new and very selective alpha 2-agonist. The following observations demonstrate the presence of functional alpha 2-adrenoceptors in rat adipocytes. (1) Adipocyte lipolysis was dose-dependently inhibited by UK 14304 (maximal effect 80% at 1 microM-UK 14304, 45% at 10 microM-UK 14304, under basal or theophylline-stimulated conditions respectively). (2) UK 14304 bound specifically to purified plasma membranes, with Bmax. = 744 fmol/mg of protein and KD = 9 nM. (3) The effect of UK 14304 was suppressed by alpha 2-antagonists. (4) Adrenaline inhibited lipolysis upon beta-adrenergic blockade (propranolol). (5) The anti-lipolytic effect of UK 14304 was modulated by the age of the rats.

Full text

PDF
679

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Belsham G. J., Denton R. M., Tanner M. J. Use of a novel rapid preparation of fat-cell plasma membranes employing Percoll to investigate the effects of insulin and adrenaline on membrane protein phosphorylation within intact fat-cells. Biochem J. 1980 Nov 15;192(2):457–467. doi: 10.1042/bj1920457. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Berlan M., Carpene C., Lafontan M., Dang-Tran L. Alpha-2 adrenergic antilipolytic effect in dog fat cells: incidence of obesity and adipose tissue localization. Horm Metab Res. 1982 May;14(5):257–260. doi: 10.1055/s-2007-1018986. [DOI] [PubMed] [Google Scholar]
  3. Bradford M. M. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem. 1976 May 7;72:248–254. doi: 10.1016/0003-2697(76)90527-3. [DOI] [PubMed] [Google Scholar]
  4. Burns T. W., Langley P. E., Terry B. E., Bylund D. B., Hoffman B. B., Tharp M. D., Lefkowitz R. J., García-Saínz J. A., Fain J. N. Pharmacological characterizations of adrenergic receptors in human adipocytes. J Clin Invest. 1981 Feb;67(2):467–475. doi: 10.1172/JCI110055. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Bylund D. B. Heterogeneity of alpha-2 adrenergic receptors. Pharmacol Biochem Behav. 1985 May;22(5):835–843. doi: 10.1016/0091-3057(85)90536-2. [DOI] [PubMed] [Google Scholar]
  6. Cambridge D. UK-14,304, a potent and selective alpha2-agonist for the characterisation of alpha-adrenoceptor subtypes. Eur J Pharmacol. 1981 Jul 10;72(4):413–415. doi: 10.1016/0014-2999(81)90588-4. [DOI] [PubMed] [Google Scholar]
  7. Carpene C., Berlan M., Lafontan M. Lack of functional antilipolytic alpha 2-adrenoceptor in rat fat cell:comparison with hamster adipocyte. Comp Biochem Physiol C. 1983;74(1):41–45. doi: 10.1016/0742-8413(83)90145-7. [DOI] [PubMed] [Google Scholar]
  8. Dabiré H. Idazoxan: a novel pharmacological tool for the study of alpha 2-adrenoceptors. J Pharmacol. 1986 Apr-Jun;17(2):113–118. [PubMed] [Google Scholar]
  9. García-Sínz J. A., Hoffman B. B., Li S. Y., Lefkowitz R. J., Fain J. N. Role of alpha 1 adrenoceptors in the turnover of phosphatidylinositol and of alpha 2 adrenoceptors in the regulation of cyclic AMP accumulation in hamster adipocytes. Life Sci. 1980 Sep 15;27(11):953–961. doi: 10.1016/0024-3205(80)90105-8. [DOI] [PubMed] [Google Scholar]
  10. Giudicelli Y., Agli B., Brulle D., Nordmann R. Influence of alpha-adrenergic blocking agents on cyclic AMP, cyclic GMP and lipolysis in hamster white fat cells. FEBS Lett. 1977 Nov 15;83(2):225–230. doi: 10.1016/0014-5793(77)81010-7. [DOI] [PubMed] [Google Scholar]
  11. Guerre-Millo M., Lavau M., Horne J. S., Wardzala L. J. Proposed mechanism for increased insulin-mediated glucose transport in adipose cells from young, obese Zucker rats. Large intracellular pool of glucose transporters. J Biol Chem. 1985 Feb 25;260(4):2197–2201. [PubMed] [Google Scholar]
  12. Himms-Hagen J. Adrenergic receptors for metabolic responses in adipose tissue. Fed Proc. 1970 Jul-Aug;29(4):1388–1401. [PubMed] [Google Scholar]
  13. Hittelman K. J., Butcher R. W. Effects of antilipolytic agents and alpha-adrenergic antagonists on cyclic AMP metabolism in hamster white adipocytes. Biochim Biophys Acta. 1973 Sep 25;316(3):403–410. doi: 10.1016/0005-2760(73)90079-9. [DOI] [PubMed] [Google Scholar]
  14. Kather H., Wieland E., Fischer B., Wirth A., Schlierf G. Adrenergic regulation of lipolysis in abdominal adipocytes of obese subjects during caloric restriction: reversal of catecholamine action caused by relief of endogenous inhibition. Eur J Clin Invest. 1985 Feb;15(1):30–37. doi: 10.1111/j.1365-2362.1985.tb00140.x. [DOI] [PubMed] [Google Scholar]
  15. Lafontan M. Alpha-adrenergic responses in rabbit white fat cells: the influence of obesity and food restriction. J Lipid Res. 1981 Sep;22(7):1084–1093. [PubMed] [Google Scholar]
  16. Lafontan M., Berlan M. Evidence for the alpha 2 nature of the alpha-adrenergic receptor inhibiting lipolysis in human fat cells. Eur J Pharmacol. 1980 Aug 22;66(1):87–93. doi: 10.1016/0014-2999(80)90298-8. [DOI] [PubMed] [Google Scholar]
  17. Lavau M., Fried S. K., Susini C., Freychet P. Mechanism of insulin resistance in adipocytes of rats fed a high-fat diet. J Lipid Res. 1979 Jan;20(1):8–16. [PubMed] [Google Scholar]
  18. Lawrence J. C., Jr, Larner J. Evidence for alpha adrenergic activation of phosphorylase and inactivation of glycogen synthase in rat adipocytes. Effects of alpha and beta adrenergic agonists and antagonists on glycogen synthase and phosphorylase. Mol Pharmacol. 1977 Nov;13(6):1060–1075. [PubMed] [Google Scholar]
  19. Ostman J., Efendić S. Catecholamines and metabolism of human adipose tissue. II. Effect of isoprophylnoradrenaline and adrenergic blocking agents on lipolysis in human omental adipose tissue in vitro. Acta Med Scand. 1970 Jun;187(6):471–476. [PubMed] [Google Scholar]
  20. Pecquery R., Giudicelli Y. Ontogenic development of alpha-adrenergic receptors and responsiveness in white adipocytes. Biochem J. 1980 Dec 15;192(3):947–950. doi: 10.1042/bj1920947. [DOI] [PMC free article] [PubMed] [Google Scholar]
  21. Pushpendran C. K., García-Sáinz J. A. RX781094 a potent and selective alpha 2-adrenergic antagonist. Effects in adipocytes and hepatocytes. Eur J Pharmacol. 1984 Apr 6;99(4):337–339. doi: 10.1016/0014-2999(84)90142-0. [DOI] [PubMed] [Google Scholar]
  22. RODBELL M. METABOLISM OF ISOLATED FAT CELLS. I. EFFECTS OF HORMONES ON GLUCOSE METABOLISM AND LIPOLYSIS. J Biol Chem. 1964 Feb;239:375–380. [PubMed] [Google Scholar]

Articles from Biochemical Journal are provided here courtesy of The Biochemical Society

RESOURCES