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In the guinea pig isolated terminal ileum the opioid pentapeptides, methionine-enkephalin and leucine-enkephalin, dose-dependently inhibit contractile responses induced by electrical field stimulation releasing endogenous acetylcholine, and by specific noncholinergic compounds including histamine, barium chloride, and beta-acetyl-digoxin. Tissue levels of cAMP and cGMP remain unchanged. We conclude that enkephalins exert their effects by a direct action at or within the muscle cell and may play a physiological role in the local control of the gut smooth muscle motility.
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