Chemistry:TRIMU 5

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TRIMU 5
TRIMU 5.png
Names
IUPAC name
L-Tyrosyl-N-{[(3-methylbutyl)amino]acetyl}-D-alaninamide
Systematic IUPAC name
(2R)-2-Amino-3-(4-hydroxyphenyl)-N-[(2R)-1-{2-[(3-methylbutyl)amino]acetamido}-1-oxopropan-2-yl]propanamide
Identifiers
3D model (JSmol)
ChemSpider
Properties
C19H30N4O4
Molar mass 378.466
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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Infobox references

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. 1.0 1.1 1.2 1.3 "Analgesic potency of TRIMU-5: a mixed mu 2 opioid receptor agonist/mu 1 opioid receptor antagonist". Eur J Pharmacol 216 (2): 249–55. June 1992. 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.