Synthesis and biological evaluation of novel T-type calcium channel blockers.
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Choi JY, Seo HN, Lee MJ, Park SJ, Park SJ, Jeon JY, Kang JH, Pae AN, Rhim H, Lee JY
Synthesis and biological evaluation of novel T-type calcium channel blockers.
Bioorg Med Chem Lett. 2007 Jan 15;17(2):471-5. Epub 2006 Oct 12.
- PubMed ID
- 17064894 [ View in PubMed]
- 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 microM), was about 5-fold potent (IC50=0.26+/-0.01 microM) for T-type calcium channel (alpha1G) blocking and its selectivity of T/N-type was also improved (7.5 versus 1.4 of mibefradil).
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) 1340 N/A N/A Details