3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers.
For LVA T-type Ca2+ channel blockers, 3,4-dihydroquinazoline derivatives as new scaffolds were prepared and evaluated for the inhibitory activity against two members of the recombinant T-type Ca2+ channel family. Among them, 8a (KYS05001, IC50=0.9 microM) was nearly equipotent with mibefradil (IC50=0.84 microM) and inhibited LVA T-type Ca2+ channel with greater efficacy than HVA Ca2+ channel.
Lee
Yong Sup
YS
Life Sciences Division, Korea Institute of Science & Technology, PO Box 131, Cheongryang, Seoul 130-650, South Korea.
Lee
Bum Hoon
BH
Park
Seong Jun
SJ
Kang
Soon Bang
SB
Rhim
Hyewhon
H
Park
Jin-Yong
JY
Lee
Jung-Ha
JH
Jeong
Seong-Woo
SW
Lee
Jae Yeol
JY
D000818:Animals; D002121:Calcium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D020747:Calcium Channels, T-Type / Q000187:drug effects / Q000378:metabolism*; D002460:Cell Line; D020128:Inhibitory Concentration 50; D020748:Mibefradil; D015394:Molecular Structure; D009865:Oocytes / Q000187:drug effects; D018408:Patch-Clamp Techniques; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology
D002121:Calcium Channel Blockers; D020747:Calcium Channels, T-Type; D011799:Quinazolines; D020748:Mibefradil