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 Calcium channel blockers (CCBs) disrupt the movement of calcium (Ca2+) through calcium channels. They are used as antihypertensive drugs, i.e., as medications to decrease blood pressure in patients with hypertension. CCBs are particularly effective against large vessel stiffness, one of the common causes of elevated systolic blood pressure in elderly patients.
Calcium channel blockers are also frequently used to alter heart rate, to prevent cerebral vasospasm, and to reduce chest pain caused by angina pectoris. N-type, L-type, and T-type voltage-dependent calcium channels are present in the zona glomerulosa of the human adrenal, and CCBs can directly influence the biosynthesis of aldosterone in adrenocortical cells, with consequent impact on the clinical treatment of hypertension with these agents.
Our Calcium Channel Blocker library (833 compounds in total) was designed as a special screening library containing compounds with predicted calcium channels blocking activity. The compounds have been selected by pharmacophore screening of OTAVAchemicals Drug-like Green Collection against four ligand-based pharmacophore models. The models were built based on known calcium channel blockers.
This library comprises drug-like compounds only and provides an excellent basis for antihypertensive research and drug discovery projects.
All compounds are in stock, cherry-picking is available.
The library (DB, SD, XLS, PDF format) as well as the price-list is available on request. Feel free to contact us or use on-line form below to send an inquiry if you are interested to obtain this library or if you need more information.
1. Dolphin AC, A short history of voltage-gated calcium channels, Br J Pharmacol , 2006 – 147 – pp. 56–62.
2. Frank Striggow and Barbara E Ehrlich, Ligand-gated calcium channels inside and out, Curr. Opin. Cell Biol., 1996 – 8 (4) – pp. 490–495.
3. Ferri N, Corsini A, Pontremoli R, Antihypertensive treatment with calcium channel blockers and renal protection: focus on lercanidipine and lercanidipine/enalapril, Eur Rev Med Pharmacol Sci., 2022 – 26(20) – pp. 7482-7492.
4. Nelson M, Drug treatment of elevated blood pressure, Australian Prescriber, 2010 – 33 (4) – pp. 108–112.
5. Kushner J, Ferrer X, Marx SO, Roles and Regulation of Voltage-gated Calcium Channels in Arrhythmias, J Innov Card Rhythm Manag. 2019 – 10(10) – pp. 3874-3880.
6. Felizola SJA, Maekawa T, Nakamura Y, Satoh F, Ono Y, Kikuchi K, Aritomi S, Ikeda K, Yoshimura M, Tojo K, Sasano H, Voltage-gated calcium channels in the human adrenal and primary aldosteronism, J Steroid Biochem Mol Biol., 2014 – 144 (part B) – pp. 410–416.
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