10007518  Capsazepine

(CAS 138977-28-3)

Click image to enlarge

• See below for pricing and ordering
• See analysis tools
• See more Receptor Biochemistry; Receptor Antagonist; Neuroscience; Signal Transduction

Chemical structure definitions are available for many Cayman products. See Chemical Structure Database for details.

Transient receptor potential vanilloid type 1 (TRPV1) is a member of the transient receptor potential (TRP) family that is activated or sensitized by a variety of endogenous stimuli as a result of tissue injury and inflammation. TRPV1 is upregulated during inflammation and plays a role in the perception of pain.1,2 Capsazepine is a competitive antagonist of TRPV1 which blocks the capsaicin-induced uptake of Ca2+ in neonatal rat dorsal root ganglia with an IC50 of 0.42 µM and Chinese hamster ovary cells with an IC50 of 17 nM.1,3 It does not block acid- or heat-induced activation of TRPV1 and may block receptors other than TRPV1.4,5
1  Doherty, E.M., Fotsch, C., Bo, Y., et al. Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides. J Med Chem 48 71-90 (2005).
2  Walker, K.M., Urban, L., Medhurst, S.J., et al. The VR1 antagonist capsazepine reverses mechanical hyperalgesia in models of inflammatory and neuropathic pain. J Pharmacol Exp Ther 304(1) 56-60 (2003).
3  Walpole, S.J., Bevan, S., Bovermann, G., et al. The discovery of capsazepine, the first competitive antagonist of the sensory neuron excitants capsaicin and resiniferatoxin. J Med Chem 37 1942-1954 (1994 Feb 2).
4  Liu, L., Simon, S.A. Capsazepine, a vanilloid receptor antagonist, inhibits nicotinic acetylcholine receptors in rat trigeminal ganglia. Neurosci Lett 228 29-32 (1997).
5  Docherty, R.J., Yeats, J.C., Piper, A.S. Capsazepine block of voltage-activated calcium channels in adult rat dorsal root ganglion neurones in culture. Br J Pharmacol 121 1461-1467 (1997).


Purchase 10007518 Capsazepine

Pricing is for North America only. Other customers should contact a distributor in their region.

This product is also available to buy in bulk quantities. Please contact our Sales Department for a quote or to purchase.

Cayman strives to be a reliable biochemical reagent vendor by providing the best possible products and services. To ask for assistance with one of our products please contact our Technical Help staff.

Warning This product is not for human or veterinary use.

Pricing updated 2010-02-09.
Prices are subject to change without notice.

Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.

  email: password: hide x LOGIN | REGISTER
Cayman Chemical
Topical Catalogs
Packed with articles, the latest products, and much more.

New
Eicosanoid

Allergy, Asthma, & Inflammation

Cancer

More...
Helping to make your research possible by providing quality biochemicals and assays for research in and much more.
toll free 800.364.9897
direct dial 734.971.3335
1180 East Ellsworth Road
Ann Arbor, Michigan 48108
USA
All contact info
© 2002-2010
Cayman Chemical