TRIMU-5 is a selective agonist of the μ2-opioid receptor and antagonist of the μ1-opioid receptor. 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. TRIMU-5 can also block the analgesic effects of μ-opioid receptor agonists like morphine. In addition to analgesia, TRIMU-5 inhibits gastrointestinal transit, a known effect of μ2-opioid receptor activation.
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