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Pharmacological Characterizations of Adrenergic Receptors in Human Adipocytes

1981; American Society for Clinical Investigation; Volume: 67; Issue: 2 Linguagem: Inglês

10.1172/jci110055

1558-8238

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

Receptor Mechanisms and Signaling

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.