Kinetics of beta-funaltrexamine binding to wild-type and mutant mu-opioid receptors expressed in Chinese hamster ovary cells.

Abstract excerpt

The two-stage reaction whereby the antagonist beta-funaltrexamine (beta-FNA) binds covalently to micro opioid receptors makes it a highly discriminating probe into the tertiary structure of the receptor's recognition pocket. To obtain a quantitative measure of how well this pocket is preserved in a mutated form of the receptor, in which His-297 is substituted with glutamine, we employed [3H]-beta-FNA to evaluate...

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