CYM51010

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CYM51010
Identifiers
  • ethyl 1-[(4-acetamidophenyl)methyl]-4-(2-phenylethyl)piperidine-4-carboxylate
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC25H32N2O3
Molar mass408.542 g·mol−1
3D model (JSmol)
  • CCOC(=O)C1(CCN(CC1)CC2=CC=C(C=C2)NC(=O)C)CCC3=CC=CC=C3
  • InChI=1S/C25H32N2O3/c1-3-30-24(29)25(14-13-21-7-5-4-6-8-21)15-17-27(18-16-25)19-22-9-11-23(12-10-22)26-20(2)28/h4-12H,3,13-19H2,1-2H3,(H,26,28)
  • Key:VUXRYYSKTWDPLO-UHFFFAOYSA-N

CYM51010 is an opioid drug which acts as a selective agonist for the μOR-δOR heteromer, with little affinity for the normal form of the mu opioid receptor or delta opioid receptor. It has analgesic effects but with a reduced side effect profile compared to typical mu opioid agonists.[1][2][3][4][5][6]

See also

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References

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  1. ^ Gomes I, Fujita W, Gupta A, Saldanha SA, Negri A, Pinello CE, et al. (July 2013). "Identification of a μ-δ opioid receptor heteromer-biased agonist with antinociceptive activity". Proceedings of the National Academy of Sciences of the United States of America. 110 (29): 12072–12077. Bibcode:2013PNAS..11012072G. doi:10.1073/pnas.1222044110. PMC 3718106. PMID 23818586.
  2. ^ DiCello JJ, Carbone SE, Saito A, Rajasekhar P, Ceredig RA, Pham V, et al. (2020). "Mu and Delta Opioid Receptors Are Coexpressed and Functionally Interact in the Enteric Nervous System of the Mouse Colon". Cellular and Molecular Gastroenterology and Hepatology. 9 (3): 465–483. doi:10.1016/j.jcmgh.2019.11.006. PMC 7036548. PMID 31759144.
  3. ^ Tiwari V, He SQ, Huang Q, Liang L, Yang F, Chen Z, et al. (April 2020). "Activation of µ-δ opioid receptor heteromers inhibits neuropathic pain behavior in rodents". Pain. 161 (4): 842–855. doi:10.1097/j.pain.0000000000001768. PMC 7085422. PMID 31815916.
  4. ^ Derouiche L, Pierre F, Doridot S, Ory S, Massotte D (September 2020). "Heteromerization of Endogenous Mu and Delta Opioid Receptors Induces Ligand-Selective Co-Targeting to Lysosomes". Molecules. 25 (19): 4493. doi:10.3390/molecules25194493. PMC 7583997. PMID 33007971.
  5. ^ Requana Aradas A, Djaboub Y, McCort-Tranchepain I, Hajasova Z, Clémenceau L, Canestrelli C, et al. (July 2023). "Activation of the Mu-Delta Opioid Receptor Heteromers Blocks Morphine Rewarding Effects". The International Journal of Neuropsychopharmacology. 26 (7): 513–521. doi:10.1093/ijnp/pyad032. PMC 10388387. PMID 37343217.
  6. ^ Watanabe A, Yamada S, Yoshida H, Inagaki M, Atsumi N, Matsushima A, et al. (2024). "Structure-Activity Relationship Study of CYM51010, an agonist for the µ-δ Opioid Receptor Heterodimer". Chemical & Pharmaceutical Bulletin. 72 (7) c24-00188: 711–730. doi:10.1248/cpb.c24-00188. PMID 39085079.
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