CIM-0216

Last updated
CIM-0216
CIM-0216 structure.png
Names
Preferred IUPAC name
2-(3,4-Dihydroquinolin-1(2H)-yl)-N-(5-methyl-1,2-oxazol-3-yl)-2-phenylacetamide
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
PubChem CID
  • InChI=1S/C21H21N3O2/c1-15-14-19(23-26-15)22-21(25)20(17-9-3-2-4-10-17)24-13-7-11-16-8-5-6-12-18(16)24/h2-6,8-10,12,14,20H,7,11,13H2,1H3,(H,22,23,25)
    Key: KSEXDSJYVSEVGF-UHFFFAOYSA-N
  • CC1=CC(=NO1)NC(=O)C(C2=CC=CC=C2)N3CCCC4=CC=CC=C43
Properties
C21H21N3O2
Molar mass 347.418 g·mol−1
Hazards
GHS labelling:
GHS-pictogram-exclam.svg
Warning
H302, H315, H319, H335
P261, P264, P270, P271, P280, P301+P312, P302+P352, P304+P340, P305+P351+P338, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, P501
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).

CIM-0216 is a chemical compound which acts as a potent and selective activator of the TRPM3 calcium channel. It produces nociception and inflammation and is used to study the function of the TRPM3 receptor in these processes. [1] [2] [3] [4]

References

  1. ↑ Held K, Kichko T, De Clercq K, Klaassen H, Van Bree R, Vanherck JC, et al. (March 2015). "Activation of TRPM3 by a potent synthetic ligand reveals a role in peptide release". Proceedings of the National Academy of Sciences of the United States of America. 112 (11): E1363-72. Bibcode:2015PNAS..112E1363H. doi: 10.1073/pnas.1419845112 . PMC   4371942 . PMID   25733887.
  2. ↑ Thiel G, Rubil S, Lesch A, Guethlein LA, Rössler OG (October 2017). "Transient receptor potential TRPM3 channels: Pharmacology, signaling, and biological functions". Pharmacological Research. 124: 92–99. doi:10.1016/j.phrs.2017.07.014. PMID   28720517.
  3. ↑ Kelemen B, Lisztes E, Vladár A, Hanyicska M, Almássy J, Oláh A, et al. (April 2020). "Volatile anaesthetics inhibit the thermosensitive nociceptor ion channel transient receptor potential melastatin 3 (TRPM3)". Biochemical Pharmacology. 174 113826. doi: 10.1016/j.bcp.2020.113826 . hdl: 2437/278831 . PMID   31987857.
  4. ↑ Vangeel L, Benoit M, Miron Y, Miller PE, De Clercq K, Chaltin P, et al. (June 2020). "Functional expression and pharmacological modulation of TRPM3 in human sensory neurons". British Journal of Pharmacology. 177 (12): 2683–2695. doi:10.1111/bph.14994. PMC   7236075 . PMID   31985045.
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