当前位置：
X-MOL 学术
›
J. Med. Chem.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Discovery of Nonpungent Transient Receptor Potential Vanilloid 1 (TRPV1) Agonist as Strong Topical Analgesic.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2019-11-26 , DOI: 10.1021/acs.jmedchem.9b01046 Jihyae Ann 1 , Ho Shin Kim 1 , Shivaji A Thorat 1 , Hee Kim 2 , Hee-Jin Ha 2 , Kwanghyun Choi 2 , Young-Ho Kim 2 , Minseok Kim 3 , Sun Wook Hwang 3 , Larry V Pearce 4 , Timothy E Esch 4 , Noe A Turcios 4 , Peter M Blumberg 4 , Jeewoo Lee 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2019-11-26 , DOI: 10.1021/acs.jmedchem.9b01046 Jihyae Ann 1 , Ho Shin Kim 1 , Shivaji A Thorat 1 , Hee Kim 2 , Hee-Jin Ha 2 , Kwanghyun Choi 2 , Young-Ho Kim 2 , Minseok Kim 3 , Sun Wook Hwang 3 , Larry V Pearce 4 , Timothy E Esch 4 , Noe A Turcios 4 , Peter M Blumberg 4 , Jeewoo Lee 1
Affiliation
|
Paradoxically, some TRPV1 agonists are, at the organismal level, both nonpungent and clinically useful as topical analgesics. Here, we describe the scaled-up synthesis and characterization in mouse models of a novel, nonpungent vanilloid. Potent analgesic activity was observed in models of neuropathic pain, and the compound blocked capsaicin induced allodynia, showing dermal accumulation with little transdermal absorption. Finally, it displayed much weaker systemic toxicity compared to capsaicin and was negative in assays of genotoxicity.
中文翻译：
发现非刺激性瞬态潜在受体香草醛1（TRPV1）激动剂可作为强效局部镇痛药。
矛盾的是，某些TRPV1激动剂在机体水平上既无刺激性又在临床上可用作局部镇痛药。在这里，我们描述了一种新型的，非辛辣的类香草的小鼠模型中的按比例放大的合成和表征。在神经性疼痛模型中观察到了有效的镇痛活性，该化合物阻断了辣椒素诱导的异常性疼痛，显示出皮肤积聚而很少经皮吸收。最后，与辣椒素相比，它显示出较弱的全身毒性，并且在遗传毒性试验中呈阴性。
更新日期：2019-11-28
中文翻译：
发现非刺激性瞬态潜在受体香草醛1（TRPV1）激动剂可作为强效局部镇痛药。
矛盾的是，某些TRPV1激动剂在机体水平上既无刺激性又在临床上可用作局部镇痛药。在这里，我们描述了一种新型的，非辛辣的类香草的小鼠模型中的按比例放大的合成和表征。在神经性疼痛模型中观察到了有效的镇痛活性，该化合物阻断了辣椒素诱导的异常性疼痛，显示出皮肤积聚而很少经皮吸收。最后，与辣椒素相比，它显示出较弱的全身毒性，并且在遗传毒性试验中呈阴性。
京公网安备 11010802027423号