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  • A synthetic form of the naturally occurring, endogenous opioid peptide, metenkephalin, and agonist of the zeta- and delta-opioid receptor and, to a lesser extent the mu-opioid receptor, with potential analgesic, neuromodulatory, immunomodulatory, anti-inflammatory, antinociceptive/analgesic, antidepressant, and gastrointestinal (GI) motility modulating activities. Upon administration, metenkefalin mimics its endogenous ligand and targets, binds to and activates the opioid receptors. This leads to an analgesic effect, inhibits neuropathic pain, and inhibits GI muscle contractility. Binding to the opioid growth factor receptor (OGFR; zeta-opioid receptor), enhances tissue growth and regeneration. In addition, activation of delta-opioid receptors located on a variety of immune cells may modulate the inflammatory immune response. This may inhibit the secretion of pro-inflammatory cytokines and the proliferation of leukocytes.
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