3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers.
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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
Drug Target Property Measurement pH Temperature (°C) Mibefradil Voltage-dependent T-type calcium channel subunit alpha-1G IC 50 (nM) 840 N/A N/A Details