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Hepatic alpha-adrenergic receptors. Identification and subcellular localization using [3H]dihydroergocryptine.

Publication ,  Journal Article
Clarke, WR; Jones, LR; Lefkowitz, RJ
Published in: J Biol Chem
September 10, 1978

Recently, several workers have shown that adrenergic control of hepatic carbohydrate metabolism has the characteristics of an alpha-receptor-mediated process. Using the rat liver membrane preparation of Neville (Neville, D. (1968) Biochim. Biophys. Acta 154, 540-552), alpha-adrenergic receptors have been identified using the ligand [3H]dihydroergocryptine. The receptors are saturable and of high affinity. Scatchard analysis yields a KD of 1.8 nM with 1.7 +/- 0.55 pmol of sites/mg of protein. Competition of dihydroergocryptine binding with various pharmacologic agents yields the typical (alpha-adrenergic potency series: (-)-epinephrine greater than (-)-norepinephrine greater than (-)-isoproterenol. (-)-Isomers are more potent than (+)-isomers. The alpha-blocker phentolamine is 3.4 orders of magnitude more potent than the beta-blocker propranolol. To determine subcellular localization of alpha-adrenergic receptors, livers were fractionated into a crude homogenate, a 1500 X g pellet, and the purified membrane preparation used previously for binding. Specific dihydroergocryptine binding, ouabain-inhibitable (Na,K)-ATPase, and F--stimulated adenylate cyclase activities, were followed in these fractions. Specific binding was enriched, relative to that in the crude homogenate, 2.88-fold in the pellet and 6.28-fold in the membranes. Similarly, (Na,K)-ATPase acticity was enriched 2.6-fold in the pellet and 7.1-fold in the membranes while adenylate cyclase activity was enriched 2.9-fold in the pellet and 3.5-fold in the membranes. It is concluded that hepatic alpha-adrenergic receptors are likely concentrated in the plasma membranes.

Duke Scholars

Published In

J Biol Chem

ISSN

0021-9258

Publication Date

September 10, 1978

Volume

253

Issue

17

Start / End Page

5975 / 5979

Location

United States

Related Subject Headings

  • Subcellular Fractions
  • Receptors, Adrenergic, alpha
  • Receptors, Adrenergic
  • Rats
  • Liver
  • Kinetics
  • Dihydroergotoxine
  • Cell Membrane
  • Biochemistry & Molecular Biology
  • Binding, Competitive
 

Citation

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Clarke, W. R., Jones, L. R., & Lefkowitz, R. J. (1978). Hepatic alpha-adrenergic receptors. Identification and subcellular localization using [3H]dihydroergocryptine. J Biol Chem, 253(17), 5975–5979.
Clarke, W. R., L. R. Jones, and R. J. Lefkowitz. “Hepatic alpha-adrenergic receptors. Identification and subcellular localization using [3H]dihydroergocryptine.J Biol Chem 253, no. 17 (September 10, 1978): 5975–79.
Clarke WR, Jones LR, Lefkowitz RJ. Hepatic alpha-adrenergic receptors. Identification and subcellular localization using [3H]dihydroergocryptine. J Biol Chem. 1978 Sep 10;253(17):5975–9.
Clarke, W. R., et al. “Hepatic alpha-adrenergic receptors. Identification and subcellular localization using [3H]dihydroergocryptine.J Biol Chem, vol. 253, no. 17, Sept. 1978, pp. 5975–79.
Clarke WR, Jones LR, Lefkowitz RJ. Hepatic alpha-adrenergic receptors. Identification and subcellular localization using [3H]dihydroergocryptine. J Biol Chem. 1978 Sep 10;253(17):5975–5979.

Published In

J Biol Chem

ISSN

0021-9258

Publication Date

September 10, 1978

Volume

253

Issue

17

Start / End Page

5975 / 5979

Location

United States

Related Subject Headings

  • Subcellular Fractions
  • Receptors, Adrenergic, alpha
  • Receptors, Adrenergic
  • Rats
  • Liver
  • Kinetics
  • Dihydroergotoxine
  • Cell Membrane
  • Biochemistry & Molecular Biology
  • Binding, Competitive