TRPM4-IN-5: Difference between revisions

TRPM4-IN-5
Identifiers
	IUPAC name 4-chloro-2-{[2-(2-chlorophenoxy)acetyl]amino}benzoic acid;
CAS Number	351424-20-9;
PubChem CID	2264067;
Chemical and physical data
Formula	C15H11Cl2NO4
Molar mass	340.16 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1=CC=C(C(=C1)OCC(=O)NC2=C(C=CC(=C2)Cl)C(=O)O)Cl;
	InChI InChI=1S/C15H11Cl2NO4/c16-9-5-6-10(15(20)21)12(7-9)18-14(19)8-22-13-4-2-1-3-11(13)17/h1-7H,8H2,(H,18,19)(H,20,21); Key:CVQCJPCMPGKEDH-UHFFFAOYSA-N;

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Revision as of 09:36, 14 February 2021

TRPM4-IN-5 is a drug which acts as a potent and selective blocker of the TRPM4 ion channel, with an IC₅₀ of 1.5μM.^[1] It is protective against glutamate mediated neuronal excitotoxicity.^[2]

References

^ Ozhathil LC, Delalande C, Bianchi B, Nemeth G, Kappel S, Thomet U, Ross-Kaschitza D, Simonin C, Rubin M, Gertsch J, Lochner M, Peinelt C, Reymond JL, Abriel H. Identification of potent and selective small molecule inhibitors of the cation channel TRPM4. Br J Pharmacol. 2018 Jun;175(12):2504-2519. doi:10.1111/bph.14220 PMID 29579323
^ Bianchi B, Smith PA, Abriel H. The ion channel TRPM4 in murine experimental autoimmune encephalomyelitis and in a model of glutamate-induced neuronal degeneration. Mol Brain 2018; 11: 41doi:10.1186/s13041-018-0385-4

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[1] Ozhathil LC, Delalande C, Bianchi B, Nemeth G, Kappel S, Thomet U, Ross-Kaschitza D, Simonin C, Rubin M, Gertsch J, Lochner M, Peinelt C, Reymond JL, Abriel H. Identification of potent and selective small molecule inhibitors of the cation channel TRPM4. Br J Pharmacol. 2018 Jun;175(12):2504-2519. doi:10.1111/bph.14220 PMID 29579323

[2] Bianchi B, Smith PA, Abriel H. The ion channel TRPM4 in murine experimental autoimmune encephalomyelitis and in a model of glutamate-induced neuronal degeneration. Mol Brain 2018; 11: 41doi:10.1186/s13041-018-0385-4

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-'''TRPM4-IN-5''' is a drug which acts as a potent and selective blocker of the [[TRPM4]] [[ion channel]], with an IC<sub>50</sub> of 1.5μM.<ref>Ozhathil LC, Delalande C, Bianchi B, Nemeth G, Kappel S, Thomet U, Ross-Kaschitza D, Simonin C, Rubin M, Gertsch J, Lochner M, Peinelt C, Reymond JL, Abriel H. Identification of potent and selective small molecule inhibitors of the cation channel TRPM4. ''Br J Pharmacol''. 2018 Jun;175(12):2504-2519. {{doi|10.1111/bph.14220}} {{pmid|29579323}}</ref>
+'''TRPM4-IN-5''' is a drug which acts as a potent and selective blocker of the [[TRPM4]] [[ion channel]], with an IC<sub>50</sub> of 1.5μM.<ref>Ozhathil LC, Delalande C, Bianchi B, Nemeth G, Kappel S, Thomet U, Ross-Kaschitza D, Simonin C, Rubin M, Gertsch J, Lochner M, Peinelt C, Reymond JL, Abriel H. Identification of potent and selective small molecule inhibitors of the cation channel TRPM4. ''Br J Pharmacol''. 2018 Jun;175(12):2504-2519. {{doi|10.1111/bph.14220}} {{pmid|29579323}}</ref> It is protective against glutamate mediated neuronal excitotoxicity.<ref>Bianchi B, Smith PA, Abriel H. The ion channel TRPM4 in murine experimental autoimmune encephalomyelitis and in a model of glutamate-induced neuronal degeneration. ''Mol Brain'' 2018; 11: 41{{doi|10.1186/s13041-018-0385-4}}</ref>
 == References ==