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Capsazepine

Cat. No. 0464

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Chemical Name: N-[2-(4-Chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide

Biological Activity

Selective vanilloid receptor antagonist (K_i = 3.2 μM). Inhibits carrageenan inflammation-induced hyperalgesic responses in the rat. Also activates amiloride-sensitive epithelial Na⁺ channel ENaCδ. Also available as part of the Vanilloid TRPV1 Receptor Tocriset™.

Technical Data

M.Wt:

376.9

Formula:

C₁₉H₂₁ClN₂O₂S

Solubility:

Soluble to 25 mM in ethanol and to 100 mM in DMSO

Purity:

>99 %

Storage:

Store at RT

CAS No:

138977-28-3

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.

Resources

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

References

Dickenson and Dray (1991) Selective antagonism of capsaicin by capsazepine: evidence for a spinal receptor site in capsaicin-induced antinociception. Br.J.Pharmacol. 104 1045. PMID: 1810591.

Kwak et al (1998) A capsaicin-receptor antagonist, capsazepine, reduces inflammation-induced hyperalgesic responses in the rat: evidence for an endogenous capsaicin-like substance. Neuroscience 86 619. PMID: 9881874.

Yamamura et al (2004) Capsazepine is a novel activator of the δ subunit of the human epithelial Na⁺ channel. J.Biol.Chem. 279 44483. PMID: 15308635.

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Keywords: Capsazepine, supplier, Vanilloid, receptor, antagonists, activators, ENaCdelta, vanilloid, Vanillioid, Receptors, VR1, TRPV, TRP, Channels, Transient, Receptor, Potential, Sodium, Epithelial, ENaC, Na+