Chung Jae-Uk, Kim Su Yeon, Lim Ju-Ok, Choi Hyun-Kyung, Kang Sang-Uk, Yoon Hae-Seok, Ryu Hyungchul, Kang Dong Wook, Lee Jeewoo, Kang Bomi, Choi Sun, Toth Attila, Pearce Larry V, Pavlyukovets Vladimir A, Lundberg Daniel J, Blumberg Peter M
Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea.
Bioorg Med Chem. 2007 Sep 15;15(18):6043-53. doi: 10.1016/j.bmc.2007.06.041. Epub 2007 Jun 26.
A series of alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. alpha-Methyl substituted analogues showed potent and stereospecific antagonism to the action of capsaicin on rat TRPV1 heterologously expressed in Chinese hamster ovary cells. In particular, compounds 14 and 18, which possess the R-configuration, exhibited excellent potencies (respectively, K(i)=41 and 39.2 nM and K(i(ant))=4.5 and 37 nM).
一系列α-取代的N-(4-叔丁基苄基)-N'-[4-(甲磺酰氨基)苄基]硫脲类似物已作为瞬时受体电位香草酸亚型1（TRPV1）受体拮抗剂进行了研究。α-甲基取代的类似物对辣椒素作用于中国仓鼠卵巢细胞中异源表达的大鼠TRPV1表现出强效且立体特异性的拮抗作用。特别是具有R-构型的化合物14和18，表现出优异的效力（分别为K(i)=41和39.2 nM以及K(i(ant))=4.5和37 nM）。
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