Title : Creating a functional opioid alkaloid binding site in the orphanin FQ receptor through site-directed mutagenesis.

Pub. Date : 1998 Apr

PMID : 9547370






4 Functional Relationships(s)
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1 Furthermore, the orphanin FQ receptor mutant that has the best affinities toward the opioid alkaloids shows, in the presence of GTP and high salt concentration, an affinity-shift profile similar to that of the delta receptor. Alkaloids opioid related nociceptin receptor 1 Homo sapiens
2 Our results indicate that 1) several residues in the orphanin FQ receptor are critical to its selectivity against the opiate alkaloids, particularly antagonists; and 2) mutating these residues to those of the opioid receptor at the corresponding position preserves the agonist/antagonist nature of opiate alkaloids as they interact with the mutant receptor. Alkaloids opioid related nociceptin receptor 1 Homo sapiens
3 Our results indicate that 1) several residues in the orphanin FQ receptor are critical to its selectivity against the opiate alkaloids, particularly antagonists; and 2) mutating these residues to those of the opioid receptor at the corresponding position preserves the agonist/antagonist nature of opiate alkaloids as they interact with the mutant receptor. Alkaloids opioid related nociceptin receptor 1 Homo sapiens
4 These findings may be helpful to medicinal chemists in designing ligands for the orphanin FQ receptor based on the structure of the opiate alkaloids. Alkaloids opioid related nociceptin receptor 1 Homo sapiens