强效T型钙通道阻滞剂的发现。
Discovery of potent T-type calcium channel blocker.
作者信息
Seo Han Na, Choi Ja Youn, Choe Yun Jeong, Kim Yoonjee, Rhim Hyewhon, Lee So Ha, Kim Jungahn, Joo Dong Jun, Lee Jae Yeol
机构信息
Research Institute for Basic Sciences and Department of Chemistry, Kyung Hee University, Seoul 130-701, Republic of Korea.
出版信息
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5740-3. doi: 10.1016/j.bmcl.2007.08.070. Epub 2007 Sep 1.
The intensive SAR study of 3,4-dihydroquinazoline series led to the most potent compound 10 (KYS05090: IC(50)=41+/-1 nM) against T-type calcium channel and its potency is nearly comparable to that of Kurtoxin. As a small organic molecule, this compound showed the highest blocking activity reported to date.
对3,4-二氢喹唑啉系列的深入SAR研究产生了针对T型钙通道的最有效化合物10（KYS05090：IC(50)=41±1 nM），其效力与Kurtoxin几乎相当。作为一种小分子有机化合物，该化合物展现出了迄今为止报道的最高阻断活性。
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