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TRIMU-5 is a selective agonist of the μ2-opioid receptor and antagonist of the μ1-opioid receptor.[1][2] It produces analgesia in animals that differs from that of conventional μ-opioid receptor agonists but that can still be blocked by μ-opioid receptor antagonists.[1] TRIMU-5 can also block the analgesic effects of μ-opioid receptor agonists like morphine.[1] In addition to analgesia, TRIMU-5 inhibits gastrointestinal transit, a known effect of μ2-opioid receptor activation.[1]

References

  1. ^ a b c d Tive LA, Pick CG, Paul D, Roques BP, Gacel GA, Pasternak GW (June 1992). "Analgesic potency of TRIMU-5: a mixed mu 2 opioid receptor agonist/mu 1 opioid receptor antagonist". Eur J Pharmacol. 216 (2): 249–55. doi:10.1016/0014-2999(92)90367-d. PMID 1327812.
  2. ^ Eisenberg RM (1994). "TRIMU-5, a mu 2-opioid receptor agonist, stimulates the hypothalamo-pituitary-adrenal axis". Pharmacol. Biochem. Behav. 47 (4): 943–6. doi:10.1016/0091-3057(94)90300-X. PMID 8029266. S2CID 54354971.


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