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. 1980 Aug;77(8):4569–4573. doi: 10.1073/pnas.77.8.4569

Agonist versus antagonist binding to alpha-adrenergic receptors.

B B Hoffman, T Michel, D M Kilpatrick, R J Lefkowitz, M E Tolbert, H Gilman, J N Fain
PMCID: PMC349885  PMID: 6107908

Abstract

The binding properties of two alpha-adrenergic radioligands, [3H]epinephrine (an agonist) and [3H]dihydroergocryptine (an antagonist), were compared in two model systems--membranes derived from human platelets and membranes from rat liver. The platelet contains exclusively alpha 2 and the liver mostly (approximately 80%) alpha 1 receptors. Agonists induce the formation of a guanine nucleotide-sensitive high-affinity state of alpha 2 but not alpha 1 receptors. [3H]Dihydroergocryptine labels all the alpha receptors, whereas [3H]epinephrine at low concentrations labels predominantly the high-affinity form of the alpha 2 receptor in both platelet and liver. However, in the liver, alpha-adrenergic effects such as glycogen phosphorylase activation are shown to be mediated via alpha 1 receptors. Thus, in liver membranes the endogenous "physiological" agonist may not label the physiologically relevant alpha 1 receptors in typical radioligand binding assays using low concentrations of [3H]epinephrine.

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Selected References

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

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