928006-44-4Relevant articles and documents
Synthesis and biological evaluation of novel T-type calcium channel blockers
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
, p. 471 - 475 (2007)
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 μM), was about 5-fold potent (IC50 = 0.26 ± 0.01 μM) for T-type calcium channel (α1G) blocking and its selectivity of T/N-type was also improved (7.5 versus 1.4 of mibefradil).