CAS:1933528-96-11-((2-(tert-Butyl)-4-(3-chlorophenyl)thiazol-5-yl)methyl)-3-(3-fluoro-4-(hydroxymethyl)phenyl)urea

MDR-652 is a high-affinity TRPV1 agonist with Ki value of 11.4nM.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

1933528-96-1

储存条件

分子式

C22H23ClFN3O2S

运输

蓝冰

分子量

447.95

别名

溶解度

动物实验配方

生物活性

描述The transient receptor potential vanilloid 1 (TRPV1) is aligand-gated and nonselective cation channel. Activation of TRPV1 triggers an influx of calcium and sodium, which initiates a cascade of events associated with pain transmission, including membrane depolarization, neuronal firing, and release of pain transmitters. MDR-652 is a highly specific and efficacious agonist of TRPV1. MDR-652 shows high affinity for human and rat TRPV1 with K_is of 11.4 and 23.8 nM, respectively. Also, it displays highly potent agonism in hTRPV1 with EC₅₀ of 5.05 nM. In ICR mouse, the coadministration of 3 mg/kg capsaicin with 0.5 mg/kg MDR-652 caused a further decrease in body temperature compared with that of 3 mg/kg capsaicin alone. In addition, MDR-652 displayed a dose-dependent decrease of body temperature, supporting that MDR-652 displayed TRPV1 agonism in the intact animal. The ip administration of MDR-652 exhibited an excellent and dose dependent analgesic profile with ED₅₀ of 0.5−2 mg/kg. The 5−10 mg/kg dose of MDR-652 blocked the neuropathic pain completely, indicating 100% maximum possible effect (MPE)^[1].