Synthesis and biological evaluation of novel T-type calcium channel blockers |
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| Authors: | Choi Ja Youn Seo Han Na Lee Min Joo Park Seong Jun Park Sung Jun Jeon Ji Young Kang Joo Hi Pae Ae Nim Rhim Hyewhon Lee Jae Yeol |
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| Institution: | Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, 1 Hoegi-Dong, Seoul 130-701, Republic of Korea. |
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| Abstract: | 3,4-Dihydroquinazoline analogues substituted by N-methyl-N-(5-pyrrolidinopentyl)amine at the 2-position were synthesized and their blocking effects were evaluated for T- and N-type calcium channels. Compound 11b (KYS05080), compared to mibefradil (IC50=1.34+/-0.49 microM), was about 5-fold potent (IC50=0.26+/-0.01 microM) for T-type calcium channel (alpha1G) blocking and its selectivity of T/N-type was also improved (7.5 versus 1.4 of mibefradil). |
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