Author/Authors :
Ja Youn Choi، نويسنده , , Han Na Seo، نويسنده , , Min Joo Lee، نويسنده , , Seong Jun Park، نويسنده , , Sung-Jun Park، نويسنده , , Ji Young Jeon، نويسنده , , Joo Hi Kang، نويسنده , , Ae Nim Pae، نويسنده , , Hyewhon Rhim، نويسنده , , Jae Yeol Lee، نويسنده ,
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 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).
Keywords :
Channel blockers , 3 , 4-Dihydroquinazoline , Regioisomers , T-type calcium channel
