Add time:09/05/2019         Source:sciencedirect.com

The N-terminal tetrapeptide amide analog of enkephalin (H-Tyr-D-Ala-Gly-Phe-NH2) is approximately equipotent with highly active pentapeptide analogs of enkephalin (and with morphine) in producing analgesia after either intracerebroventricular or intravenous administration. Smaller fragments exhibited diminished potency, but even the dipeptide (H-Tyr-D-Ala-NH2) retained naloxone-reversible analgesic activity at high intraventricular doses. These findings suggest that while the dipeptide has full intrinsic activity, the tetrapeptide sequence may be a minimum structural requirement for potent analgesia.

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