Capsazepine

• CAT Number: I001495
• CAS Number: 138977-28-3
• Molecular Formula: C19H21ClN2O2S
• Molecular Weight: 376.9
• Purity: ≥95%
• Target: TRPV1
• Solubility: DMSO: ≥ 50 mg/mL
• Storage: Store at -20°C
• IC50: 562 nM (Rat TRPV1) [1]
• InChIKey: DRCMAZOSEIMCHM-UHFFFAOYSA-N

Capsazepine (CAT: I001495) is a synthetic compound that acts as a selective antagonist of the transient receptor potential vanilloid 1 (TRPV1) channel. It inhibits the activation of TRPV1, a receptor involved in pain perception and the sensation of heat. Capsazepine blocks the binding of capsaicin, the compound responsible for the hot and spicy sensation of chili peppers, to the TRPV1 channel. It has been used as a pharmacological tool to study the role of TRPV1 in various physiological and pathological processes, including pain, inflammation, and thermoregulation.

Reference

1:Identification of capsazepine as a novel inhibitor of system xc- and cancer-induced bone pain. Fazzari J, Balenko MD, Zacal N, Singh G.J Pain Res. 2017 Apr 18;10:915-925. doi: 10.2147/JPR.S125045. eCollection 2017. PMID: 28458574 Free PMC Article2:Capsazepine inhibits JAK/STAT3 signaling, tumor growth, and cell survival in prostate cancer. Lee JH, Kim C, Baek SH, Ko JH, Lee SG, Yang WM, Um JY, Sethi G, Ahn KS.Oncotarget. 2017 Mar 14;8(11):17700-17711. doi: 10.18632/oncotarget.10775. PMID: 27458171 Free PMC Article3:Co-administration of cannabidiol and capsazepine reduces L-DOPA-induced dyskinesia in mice: Possible mechanism of action. Dos-Santos-Pereira M, da-Silva CA, Guimarães FS, Del-Bel E.Neurobiol Dis. 2016 Oct;94:179-95. doi: 10.1016/j.nbd.2016.06.013. Epub 2016 Jun 29. No abstract available. PMID: 27373843 4:Systemic desensitization through TRPA1 channels by capsazepine and mustard oil – a novel strategy against inflammation and pain. Kistner K, Siklosi N, Babes A, Khalil M, Selescu T, Zimmermann K, Wirtz S, Becker C, Neurath MF, Reeh PW, Engel MA.Sci Rep. 2016 Jun 30;6:28621. doi: 10.1038/srep28621. PMID: 27356469 Free PMC Article5:The Transient Receptor Potential Vanilloid 1 Antagonist Capsazepine Improves the Impaired Lung Mechanics during Endotoxemia. Cabral LD, Giusti-Paiva A.Basic Clin Pharmacol Toxicol. 2016 Nov;119(5):421-427. doi: 10.1111/bcpt.12605. Epub 2016 May 24. PMID: 27090778 6:Interaction between Cannabinoid Compounds and Capsazepine in Protection against Acute Pentylenetetrazole-induced Seizure in Mice. Naderi N, Shafieirad E, Lakpoor D, Rahimi A, Mousavi Z.Iran J Pharm Res. 2015 Winter;14(Suppl):115-20. PMID: 26185513 Free PMC Article7:TRPV1 antagonism by capsazepine modulates innate immune response in mice infected with Plasmodium berghei ANKA. Fernandes ES, Brito CX, Teixeira SA, Barboza R, dos Reis AS, Azevedo-Santos AP, Muscará M, Costa SK, Marinho CR, Brain SD, Grisotto MA.Mediators Inflamm. 2014;2014:506450. doi: 10.1155/2014/506450. Epub 2014 Aug 24. PMID: 25242870 Free PMC Article8:QSAR and docking studies on capsazepine derivatives for immunomodulatory and anti-inflammatory activity. Shukla A, Sharma P, Prakash O, Singh M, Kalani K, Khan F, Bawankule DU, Luqman S, Srivastava SK.PLoS One. 2014 Jul 8;9(7):e100797. doi: 10.1371/journal.pone.0100797. eCollection 2014. PMID: 25003344 Free PMC Article9:Inhibition of K+ transport through Na+, K+-ATPase by capsazepine: role of membrane span 10 of the α-subunit in the modulation of ion gating. Mahmmoud YA, Shattock M, Cornelius F, Pavlovic D.PLoS One. 2014 May 9;9(5):e96909. doi: 10.1371/journal.pone.0096909. eCollection 2014. PMID: 24816799 Free PMC Article10:TRPV1 antagonist capsazepine suppresses 4-AP-induced epileptiform activity in vitro and electrographic seizures in vivo. Gonzalez-Reyes LE, Ladas TP, Chiang CC, Durand DM.Exp Neurol. 2013 Dec;250:321-32. doi: 10.1016/j.expneurol.2013.10.010. Epub 2013 Oct 18. PMID: 24145133 Free PMC Article