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Research Article Free access | 10.1172/JCI110055

Pharmacological Characterizations of Adrenergic Receptors in Human Adipocytes

Thomas W. Burns, Paul E. Langley, Boyd E. Terry, David B. Bylund, Brian B. Hoffman, Michael D. Tharp, Robert J. Lefkowitz, J. Adolfo García-Saínz, and John N. Fain

Department of Medicine, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Surgery, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Pharmacology, University of Missouri School of Medicine, Columbia, Missouri 65211

Howard Hughes Medical Institute, Duke University Medical Center, Durham, North Carolina 27710

Department of Medicine (Cardiology) and Biochemistry, Duke University Medical Center, Durham, North Carolina 27710

Section of Physiological Chemistry, Brown University, Providence, Rhode Island 02912

Find articles by Burns, T. in: PubMed | Google Scholar

Department of Medicine, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Surgery, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Pharmacology, University of Missouri School of Medicine, Columbia, Missouri 65211

Howard Hughes Medical Institute, Duke University Medical Center, Durham, North Carolina 27710

Department of Medicine (Cardiology) and Biochemistry, Duke University Medical Center, Durham, North Carolina 27710

Section of Physiological Chemistry, Brown University, Providence, Rhode Island 02912

Find articles by Langley, P. in: PubMed | Google Scholar

Department of Medicine, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Surgery, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Pharmacology, University of Missouri School of Medicine, Columbia, Missouri 65211

Howard Hughes Medical Institute, Duke University Medical Center, Durham, North Carolina 27710

Department of Medicine (Cardiology) and Biochemistry, Duke University Medical Center, Durham, North Carolina 27710

Section of Physiological Chemistry, Brown University, Providence, Rhode Island 02912

Find articles by Terry, B. in: PubMed | Google Scholar

Department of Medicine, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Surgery, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Pharmacology, University of Missouri School of Medicine, Columbia, Missouri 65211

Howard Hughes Medical Institute, Duke University Medical Center, Durham, North Carolina 27710

Department of Medicine (Cardiology) and Biochemistry, Duke University Medical Center, Durham, North Carolina 27710

Section of Physiological Chemistry, Brown University, Providence, Rhode Island 02912

Find articles by Bylund, D. in: PubMed | Google Scholar

Department of Medicine, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Surgery, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Pharmacology, University of Missouri School of Medicine, Columbia, Missouri 65211

Howard Hughes Medical Institute, Duke University Medical Center, Durham, North Carolina 27710

Department of Medicine (Cardiology) and Biochemistry, Duke University Medical Center, Durham, North Carolina 27710

Section of Physiological Chemistry, Brown University, Providence, Rhode Island 02912

Find articles by Hoffman, B. in: PubMed | Google Scholar

Department of Medicine, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Surgery, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Pharmacology, University of Missouri School of Medicine, Columbia, Missouri 65211

Howard Hughes Medical Institute, Duke University Medical Center, Durham, North Carolina 27710

Department of Medicine (Cardiology) and Biochemistry, Duke University Medical Center, Durham, North Carolina 27710

Section of Physiological Chemistry, Brown University, Providence, Rhode Island 02912

Find articles by Tharp, M. in: PubMed | Google Scholar

Department of Medicine, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Surgery, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Pharmacology, University of Missouri School of Medicine, Columbia, Missouri 65211

Howard Hughes Medical Institute, Duke University Medical Center, Durham, North Carolina 27710

Department of Medicine (Cardiology) and Biochemistry, Duke University Medical Center, Durham, North Carolina 27710

Section of Physiological Chemistry, Brown University, Providence, Rhode Island 02912

Find articles by Lefkowitz, R. in: PubMed | Google Scholar

Department of Medicine, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Surgery, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Pharmacology, University of Missouri School of Medicine, Columbia, Missouri 65211

Howard Hughes Medical Institute, Duke University Medical Center, Durham, North Carolina 27710

Department of Medicine (Cardiology) and Biochemistry, Duke University Medical Center, Durham, North Carolina 27710

Section of Physiological Chemistry, Brown University, Providence, Rhode Island 02912

Find articles by García-Saínz, J. in: PubMed | Google Scholar

Department of Medicine, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Surgery, University of Missouri School of Medicine, Columbia, Missouri 65211

Department of Pharmacology, University of Missouri School of Medicine, Columbia, Missouri 65211

Howard Hughes Medical Institute, Duke University Medical Center, Durham, North Carolina 27710

Department of Medicine (Cardiology) and Biochemistry, Duke University Medical Center, Durham, North Carolina 27710

Section of Physiological Chemistry, Brown University, Providence, Rhode Island 02912

Find articles by Fain, J. in: PubMed | Google Scholar

Published February 1, 1981 - More info

Published in Volume 67, Issue 2 on February 1, 1981
J Clin Invest. 1981;67(2):467–475. https://doi.org/10.1172/JCI110055.
© 1981 The American Society for Clinical Investigation
Published February 1, 1981 - Version history
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Abstract

Three types of adrenergic receptors, beta, alpha-1, and alpha-2, were identified in human adipocytes, isolated from properitoneal adipose tissue, using both the binding of radioactive ligands and the effects of adrenergic agents on receptor-specific biochemical responses. Adrenergic binding studies showed the following results: [3H]dihydroalprenolol binding (beta adrenergic) Bmax 280 fmol/mg protein, KD 0.38 nM; [3H]para-aminoclonidine binding (alpha-2 adrenergic) Bmax 166 fmol/mg protein, KD 0.49 nM; [3H]WB 4101 binding (alpha-1 adrenergic) Bmax 303 fmol/mg protein, KD 0.86 nM. In adipocytes from subcutaneous adipose tissue, [3H]dihydroergocryptine binding indicated the presence of alpha-2 but not alpha-1 receptors.

Beta and alpha-2 adrenergic receptors appeared to be positively and negatively coupled to adenylate cyclase, respectively. Cells or cell membranes were incubated with epinephrine (10 μM) alone and in combination with the antagonists yohimbine (alpha-2) and prazosin (alpha-1). Epinephrine alone prompted a modest increase in adenylate cyclase activity, cyclic AMP, and glycerol release, an index of lipolysis. Yohimbine (0.1 μM) greatly enhanced these actions whereas prazosin was without effect. The beta agonist, isoproterenol, stimulated glycerol release, whereas the alpha-2 agonist, clonidine, inhibited lipolysis and cyclic AMP accumulation. To assess further alpha-1 receptors, cells were incubated with [32P]phosphate and epinephrine (10 μM) alone and in combination with prazosin and yohimbine. Epinephrine alone caused a three- to fourfold increase in 32P incorporation into phosphatidylinositol. Prazosin (0.1 μM) blocked this action whereas yohimbine (0.1 μM) was without effect. Thus, in a homogeneous cell preparation, the human adipocyte appears to have three different adrenergic receptors, each of which is coupled to a distinct biochemical response.

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