Abstract
Bonner, G. G., P. Davis, D. Stropova, R. Ferguson, H. I. Yamamura, F. Porreca and V. J. Hruby. Opioid peptides: Simultaneous δ agonism and μ antagonism in somatostatin analogues. Peptides 18(1) 93–100, 1997.—Four isomers of the Somatostatin analogue H-D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH 2 (CTAP) were made with β-MePhe in position 1 and assayed for opioid binding in rat brain, biological activity in MVD and GPI bioassays, and antinociception in mouse warm-water tail flick assays. These analogues displayed varying potencies and biological activities including: simultaneous δ receptor agonism/ μ receptor antagonism, μ receptor antagonism, and δ receptor agonism. These analogues demonstrated that the N-terminal residue is important for receptor potency/selectivity and signal transduction. These analogues may represent leads to therapeutic agents that yield analgesia via δ agonist effects, yet lack side effects associated with μ activity.
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