product name
辣椒平, ≥98% (HPLC), solid
质量水平
检测方案
≥98% (HPLC)
形式
solid
颜色
off-white
溶解性
DMSO: >10 mg/mL, clear
储存温度
2-8°C
SMILES字符串
Oc1cc2CCCN(Cc2cc1O)C(=S)NCCc3ccc(Cl)cc3
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)
InChI key
DRCMAZOSEIMCHM-UHFFFAOYSA-N
基因信息
human ... TRPV1(7442) , TRPV4(59341)
rat ... Trpv1(83810)
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应用
辣椒平作为瞬时受体电位香草醛-1(TRPV1)拮抗剂的应用实例：
- 研究其对辣椒素诱导的胞外信号调节激酶(ERK)磷酸化的影响作用
- 研究TRPV1在大鼠伤害感受器中枢神经末梢的作用
- 公牛精子中TRPV1的功能表征
生化/生理作用
辣椒平(Capsazepine)是人工合成的辣椒素类似物和瞬时受体电位香草醛-1(TRPV1)拮抗剂。在多种癌症中具有抗增殖和抗癌作用，包括口腔鳞状细胞癌、非小细胞肺癌(NSCLC)、乳腺癌和前列腺癌细胞株（HSC-3、H460、MDA-231和PC-3）。辣椒平可恢复在内毒素血症中受损的肺机能，可作为急性肺损伤(ALI)的潜在治疗药物。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
S Bevan et al.
British journal of pharmacology, 107(2), 544-552 (1992-10-01)
1. Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, capsaicin. The present study shows the capsazepine acts as a competitive antagonist of capsaicin. 2. Capsazepine (10 microM) reversibly reduced or abolished the current response to capsaicin (500 nM)
Ablation and regeneration of peripheral and central TRPV1 expressing nerve terminals and the consequence of nociception
Yu SQ and Premkumar LS
Open Medicine : A Peer-Reviewed, Independent, Open-Access Journal, 8(1) (2015)
Jorge De La Chapa et al.
Bioorganic & medicinal chemistry, 27(1), 208-215 (2018-12-12)
We previously demonstrated that capsazepine (CPZ), a synthetic transient receptor potential Vanilloid subtype 1 (TRPV1) antagonist, has significant anti-cancer effects in vivo. The purpose of this study was to develop more potent analogs based upon CPZ pharmacophore and structure-activity relationships
Mustafa Nazıroğlu et al.
PloS one, 12(6), e0179950-e0179950 (2017-06-24)
There is convincing epidemiological and experimental evidence that capsaicin, a potent natural transient receptor potential cation channel vanilloid member 1 (TRPV1) agonist, has anticancer activity. However, capsaicin cannot be given systemically in large doses, because of its induction of acute
Giulia Donvito et al.
The Journal of pharmacology and experimental therapeutics, 359(2), 310-318 (2016-10-21)
Chemotherapy-induced peripheral neuropathy (CIPN) represents a serious complication associated with antineoplastic drugs. Although there are no medications available that effectively prevent CIPN, many classes of drugs have been used to treat this condition, including anticonvulsants, serotonin and noradrenaline reuptake inhibitors
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