Article
Inverse agonist activity at the alpha(2A)-adrenergic receptor.
Molecular pharmacology - 1 Mar 2001
Wade S M, Lan K, Moore D J, Neubig R R
Abstract excerpt
Constitutive activation of G protein-coupled receptors (GPCRs) is now well recognized and many classical GPCR antagonists have been found to be inverse agonists. For the alpha(2A)-adrenergic receptor (AR) we determine the relative inverse efficacies of a series of antagonists and utilize the extended ternary complex model to estimate the fraction of constitutively active mutant (CAM) receptors in the active...
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