XB-ART-35705
Bioorg Med Chem Lett
2007 Jan 15;172:471-5. doi: 10.1016/j.bmcl.2006.10.024.
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Synthesis and biological evaluation of novel T-type calcium channel blockers.
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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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