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CIM-0216

From Wikipedia, the free encyclopedia
CIM-0216
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
  • 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:
GHS07: Exclamation mark
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

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  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. 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.