Molecular structure of Capsazepine, CAS Number: 138977-28-3
Capsazepine (CAS 138977-28-3)
See product citations (11)
Alternate Names:
N-[2-(4-Chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide
Application:
Capsazepine is an antagonist of TRPV1 and activator of ENaC
CAS Number:
138977-28-3
Purity:
≥97%
Molecular Weight:
376.90
Molecular Formula:
C19H21ClN2O2S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Capsazepine is a competitive antagonist of the VR1 (TRPV1, also transient receptor potential vanilloid type 1), antagonizing the effects produced by Capsaicin at this receptor (sc-3577). The VR1 (TRPV1 receptor) is a non-selective ligand-gated cation channel that responds to noxious heat, protons, and Capsaicin, producing nociception signals. Capsazepine also activates ENaCdelta (amiloride-sensitive epithelial Na+ channel). Capsazepine is shown to inhibit the development of mechanical hyperalgesia induced by intraplanar capsaicin injection. Capsazepine is described to block Resiniferatoxin (sc-24015)- and Capsaicin-induced contractions of guinea pig treacheal smooth muscle. Studies investigating the function of the VR1 (TRPV1 receptor) have employed Capsazepine as a tool for perturbing systemic neuronal response to Capsaicin.
Capsazepine (CAS 138977-28-3) References
- The VR1 antagonist capsazepine reverses mechanical hyperalgesia in models of inflammatory and neuropathic pain. | Walker, KM., et al. 2003. J Pharmacol Exp Ther. 304: 56-62. PMID: 12490575
- Capsazepine: a competitive antagonist of the sensory neurone excitant capsaicin. | Bevan, S., et al. 1992. Br J Pharmacol. 107: 544-52. PMID: 1422598
- Current perspectives on the therapeutic utility of VR1 antagonists. | Valenzano, KJ. and Sun, Q. 2004. Curr Med Chem. 11: 3185-202. PMID: 15579007
- Capsazepine, a novel capsaicin antagonist, selectively antagonises the effects of capsaicin in the mouse spinal cord in vitro. | Urban, L. and Dray, A. 1991. Neurosci Lett. 134: 9-11. PMID: 1726117
- Selective antagonism of capsaicin by capsazepine: evidence for a spinal receptor site in capsaicin-induced antinociception. | Dickenson, AH. and Dray, A. 1991. Br J Pharmacol. 104: 1045-9. PMID: 1810591
- Capsazepine inhibits JAK/STAT3 signaling, tumor growth, and cell survival in prostate cancer. | Lee, JH., et al. 2017. Oncotarget. 8: 17700-17711. PMID: 27458171
- A comparison of capsazepine and ruthenium red as capsaicin antagonists in the rat isolated urinary bladder and vas deferens. | Maggi, CA., et al. 1993. Br J Pharmacol. 108: 801-5. PMID: 7682139
- The discovery of capsazepine, the first competitive antagonist of the sensory neuron excitants capsaicin and resiniferatoxin. | Walpole, CS., et al. 1994. J Med Chem. 37: 1942-54. PMID: 8027976
- Inhibition by capsazepine of resiniferatoxin- and capsaicin-induced contractions of guinea pig trachea. | Ellis, JL. and Undem, BJ. 1994. J Pharmacol Exp Ther. 268: 85-9. PMID: 8301598
- Capsazepine, a vanilloid receptor antagonist, inhibits nicotinic acetylcholine receptors in rat trigeminal ganglia. | Liu, L. and Simon, SA. 1997. Neurosci Lett. 228: 29-32. PMID: 9197280
- Capsazepine block of voltage-activated calcium channels in adult rat dorsal root ganglion neurones in culture. | Docherty, RJ., et al. 1997. Br J Pharmacol. 121: 1461-7. PMID: 9257928
- Ruthenium red and capsazepine antinociceptive effect in formalin and capsaicin models of pain in mice. | Santos, AR. and Calixto, JB. 1997. Neurosci Lett. 235: 73-6. PMID: 9389599
Inhibitor of:
6330403A02Rik, ACCN5, ANKRD10, ANKTM1, ASIC1, BSPII, CARD 8, CGRP1, CNOX, CYB5R2, EG328644, HRC, HVCN1, LYSMD4, Mas 7, Mimitin, MrgA1, MrgA3, MrgA4, MrgA8, MrgA9, MrgB2, MrgB4, MrgH, NAIP7, NALP1B, NALP5, NALP9, NDUFB2, NDUFB8, Olfr1166, Olfr31, Olfr315, Olfr331, Olfr347, Olfr350, Olfr374, Olfr376, Olfr378, Olfr38, Olfr536, Olfr544, Olfr551, Olfr722, Olfr860, Olfr862, Olfr866, Olfr867, Olfr868, OR10AG1, OR10H5, OR10K2, OR2T34, OR2W3, OR4K15, OR51I, OR5H15, OR5K2, OR5K4, P2RY8, PIRT, PTα, QCR10, RFESD, TASK-3, THC, THEM92, TMC6, TMEM143, TMEM34, TMEM63B, TMEM87B, Trk1, TRP14, TRPM8, TRPV6, UQCRC2, V3R 8, Vmn2r106, Vmn2r21, Vmn2r80, Vmn2r94, Vmn2r95, and VR1.Activator of:
ASIC-β, ASIC4, CNRIP1, CYLD, delta ENaC, LALP70, MrgB4, MrgB5, MrgB8, MrgH, Mrgprh, NALP11, Olfr466, Olfr512, and VRL-1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Capsazepine, 5 mg | sc-201098 | 5 mg | $148.00 | |||
Capsazepine, 25 mg | sc-201098A | 25 mg | $459.00 |