Capsazepine - CAS 138977-28-3
Catalog number: 138977-28-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C19H21ClN2O2S
Molecular Weight:
376.91
COA:
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Targets:
TRP Channel
Description:
Capsazepine, a benzazepine derivative, has been found to be a sensory neurone excitotoxin that could be used against hyperalgesic responses. IC50: 562 nM (Rat TRPV1).
Purity:
> 95%
Appearance:
White to Light Yellow Solid
Synonyms:
N-[2-(4-Chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide
Solubility:
DMSO: ≥ 50 mg/mL
Storage:
-20ºC Freeze
MSDS:
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Application:
Capsazepine has been found to be a sensory neurone excitotoxin that could be used against hyperalgesic responses.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
Melting Point:
155-161°C
InChIKey:
DRCMAZOSEIMCHM-UHFFFAOYSA-N
InChI:
InChI=1S/C19H21ClN2O2S/c20-16-5-3-13(4-6-16)7-8-21-19(25)22-9-1-2-14-10-17(23)18(24)11-15(14)12-22/h3-6,10-11,23-24H,1-2,7-9,12H2,(H,21,25)
Canonical SMILES:
C1CC2=CC(=C(C=C2CN(C1)C(=S)NCCC3=CC=C(C=C3)Cl)O)O
1.Protective role of cannabinoid CB1 receptors and vascular effects of chronic administration of FAAH inhibitor URB597 in DOCA-salt hypertensive rats.
Baranowska-Kuczko M1, Kozłowska H2, Kloza M2, Karpińska O2, Toczek M2, Harasim E3, Kasacka I4, Malinowska B2. Life Sci. 2016 Mar 9. pii: S0024-3205(16)30164-3. doi: 10.1016/j.lfs.2016.03.014. [Epub ahead of print]
AIMS: This study examined whether the fall in blood pressure (BP) induced by the chronic inhibition of fatty acid amide hydrolase (FAAH) by URB597 in deoxycorticosterone acetate (DOCA-salt) hypertensive rats correlates with endocannabinoid-mediated vascular changes.
2.Involvement of TRPV1 in the Olfactory Bulb in Rimonabant-Induced Olfactory Discrimination Deficit.
Hu SS1. Chin J Physiol. 2016 Feb 29;59(1):21-32. doi: 10.4077/CJP.2016.BAE366.
Rimonabant is well recognized as a cannabinoid CB₁ receptor antagonist/inverse agonist. Rimonabant not only antagonizes the effects induced by exogenous cannabinoids and endocannabinoids at CB₁ receptors, it also exerts several pharmacological and behavioral effects independent of CB₁ receptor inactivation. For example, rimonabant can function as a low-potency mixed agonist/antagonist of the transient receptor potential vanilloid receptor 1 (TRPV1). Hence, it is important to explain the underlying mechanisms of the diverse physiological effects induced by rimonabant with caution. Interestingly, CB₁ receptor has recently been suggested to play a role in olfactory functions. Olfaction not only is involved in food intake, visual perception and social interaction, but also is proposed as a putative marker for schizophrenia and autism. Therefore, the present study aimed to investigate whether CB₁ receptor and TRPV1 played a role in olfactory functions.
3.The Transient Receptor Potential Vanilloid 1 (TRPV1) Antagonist Capsazepine Improves the Impaired Lung Mechanics during Endotoxemia.
Cabral LD1,2, Giusti-Paiva A1,2. Basic Clin Pharmacol Toxicol. 2016 Apr 19. doi: 10.1111/bcpt.12605. [Epub ahead of print]
Acute lung injury (ALI) caused by systemic inflammatory response remains a leading cause of morbidity and mortality in critically ill patients. Management of patients with sepsis is largely limited to supportive therapies, reflecting an incomplete understanding of the underlying pathophysiology. Furthermore, there have been limited advances in the treatments for ALI. In the present study, lung function and a histological analysis were performed to evaluate the impact of transient receptor potential vanilloid-1 receptor (TRPV1) antagonist (capsazepine; CPZ) on the lipopolysaccharide (LPS)-induced lung injury in mice. For this, adult mice pre-treated with CPZ or vehicle received intraperitoneal injections of LPS or saline and 24 hr after, the mice were anaesthetized, and lung mechanics was evaluated. The LPS-challenged mice exhibited substantial mechanical impairment, characterized by increases in respiratory system resistance, respiratory system elastance, tissue damping and tissue elastance.
4.Inflammatory stimuli acutely modulate peripheral taste function.
Kumarhia D1, He L1, McCluskey LP2. J Neurophysiol. 2016 Mar 23:jn.01104.2015. doi: 10.1152/jn.01104.2015. [Epub ahead of print]
Inflammation-mediated changes in taste perception can affect health outcomes in patients, but little is known about underlying mechanisms. In the current work, we hypothesized that proinflammatory cytokines directly modulate Na+transport in taste buds. To test this, we measured acute changes in Na+flux in polarized fungiform taste buds loaded with a Na+indicator dye. IL-1β elicited an amiloride-sensitive increase in Na+transport in taste buds. In contrast, TNF-α dramatically and reversibly decreased Na+flux in polarized taste buds via amiloride-sensitive and amiloride-insensitive Na+transport systems. The speed and partial amiloride-sensitivity of these changes in Na+flux indicate that IL-1β and TNF-α modulate epithelial Na+channel (ENaC) function. A portion of the TNF-mediated decrease in Na+flux is also blocked by the TRPV1 antagonist, capsazepine, though TNF-α further reduced Na+transport independently of both amiloride and capsazepine.
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Chemical Structure

CAS 138977-28-3 Capsazepine

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