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Summary
Novelty: A combination of a μ-opioid agonist (opiate) and a δ-opioid agonist (enkephalin derivative) is disclosed, which shows potentiation of the analgesic, sedative, antitussive, and gastrointestinal motility modalities of opiate action, with a claimed reduction of tolerance and dependence.
Biology: Dose-response data for antinociceptive activity (hot plate trial) for the opiate/enkephalin combination are presented showing a significant and useful leftward shift in the presence of the enkephalin. For example, the ED50 for morphine alone was 1.0 nmol upon intracerebroventricular (KK) administration and was 0.2 nmol in combination with 1.5 nmol DPDPE. Naloxone-precipitated dependence symptoms are not potentiated, though still present.
Chemistry: Preferred opiates are morphine, oxymorphine, codeine, methadone etc. Preferred enkephalins are [D-Pen2, D-Pen5] enkephalin (DPDPE) and [D-Pen2, L-Pen5] enkephalin (DPLPE).