Article
beta-Funaltrexamine, a gauge for the recognition site of wildtype and mutant H297Q mu-opioid receptors.
Synapse (New York, N.Y.) - 1 Jul 2003
Spivak Charles E, Beglan Carol L, Zöllner Christian, Surratt Christopher K
Abstract excerpt
The antagonist beta-funaltrexamine (beta-FNA), known to bind covalently to mu-opioid receptors by a two-step, doubly discriminating sequence, was used as a sensitive gauge to compare wildtype to mutant H297Q mu-opioid receptors. We addressed whether this mutation, which enhances the intrinsic activities of alkaloid mu-receptor agents, affects both the reversible and covalent phases of beta-FNA binding. Such...
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