3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers.

Article Details

Citation

Lee YS, Lee BH, Park SJ, Kang SB, Rhim H, Park JY, Lee JH, Jeong SW, Lee JY

3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers.

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3379-84.

PubMed ID
15177437 [ View in PubMed
]
Abstract

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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
MibefradilVoltage-dependent T-type calcium channel subunit alpha-1GIC 50 (nM)840N/AN/ADetails