Chemistry:Fendiline
Fendiline is a nonselective calcium channel blocker and coronary vasodilator, originally developed for its anti-anginal and antiarrhythmic properties in the management of coronary heart disease.[1][2][3]
By inhibiting the influx of calcium ions into cardiac and vascular smooth muscle cells, fendiline promotes vasodilation, particularly of the coronary arteries, thereby increasing blood flow to the heart muscle, alleviating ischemia, and reducing chest pain associated with angina.[2] Although its clinical use has become limited due to the availability of alternative treatments and its relatively slow onset of action, fendiline remains notable for its long half-life, lack of tolerance development, and demonstrated efficacy in improving exercise tolerance and reducing the frequency of angina attacks in placebo-controlled trials.[2]
References
- ↑ "Fendiline". DrugBank. https://go.drugbank.com/drugs/DB08980.
- ↑ 2.0 2.1 2.2 "Fendiline: a review of its basic pharmacological and clinical properties.". Pharmatherapeutica 5 (2): 103–136. 1987. OCLC 115670794. PMID 3310016.
- ↑ "Effect of Ca2+ antagonists on isolated rabbit detrusor muscle". Acta Physiologica Hungarica 77 (3–4): 269–278. 1991. PMID 1755331.
Further reading
- "Fendiline-evoked [Ca2+]i rises and non-Ca2+-triggered cell death in human oral cancer cells". Human & Experimental Toxicology 28 (1): 41–48. January 2009. doi:10.1177/0960327108097436. PMID 19411560. Bibcode: 2009HETox..28...41H.
- "Fendiline, an anti-anginal drug, increases intracellular Ca2+ in PC3 human prostate cancer cells". Cancer Chemotherapy and Pharmacology 48 (1): 37–41. July 2001. doi:10.1007/s002800000262. PMID 11488522.
- "Single dose pharmacokinetics of fendiline in humans". European Journal of Drug Metabolism and Pharmacokinetics 7 (2): 105–110. April 1982. doi:10.1007/BF03188726. PMID 7117293.
- "The anti-anginal drug fendiline elevates cytosolic Ca2+ in rabbit corneal epithelial cells". Life Sciences 71 (9): 1071–1079. July 2002. doi:10.1016/S0024-3205(02)01797-6. PMID 12088766.
- "Fendiline Inhibits K-Ras Plasma Membrane Localization and Blocks K-Ras Signal Transmission". Molecular and Cellular Biology 33 (2): 237–251. 2013. doi:10.1128/MCB.00884-12. PMID 23129805.
- "Fendiline inhibits proliferation and invasion of pancreatic cancer cells by interfering with ADAM10 activation and β-catenin signaling". Oncotarget 6 (34): 35931–35948. 3 November 2015. doi:10.18632/oncotarget.5933. PMID 26440150.
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