Devapamil Explained

Devapamil is a calcium channel blocker. It is also known as desmethoxyverapamil, which is a phenylalkylamine (PAA) derivative.^[1] Devapamil not only inhibits by blocking the calcium gated channels, but also by depolarizing the membrane during the sodium-potassium exchanges.^[2]

Structure

Devapamil consists of two aromatic rings with methoxy substituents connected by an alkylamine chain increasing flexibility and overall potency.^[3]

Animal studies

Devapamil in rats can be used to decrease glutathione levels and increase oxidation of lipids, which makes it effective in preclusion of ulcers caused by stress.^{[4] [5]} The medical characteristics of this drug, and other phenylalkylamines, depends greatly on the state of the calcium channels being targeted which results in a greater affinity and drug efficiency. ^[6]

Notes and References

1. Erdmann R, Lüttgau HC . The effect of the phenylalkylamine D888 (devapamil) on force and Ca2+ current in isolated frog skeletal muscle fibres . The Journal of Physiology . 413 . 1 . 521–41 . June 1989 . 2557440 . 10.1113/jphysiol.1989.sp017667 . 1189114 .
2. Dierkes PW, Wende V, Hochstrate P, Schlue WR . L-type Ca2+ channel antagonists block voltage-dependent Ca2+ channels in identified leech neurons . Brain Research . 1013 . 2 . 159–67 . July 2004 . 15193524 . 10.1016/j.brainres.2004.03.038 . 22004238 .
3. Cheng RC, Tikhonov DB, Zhorov BS . Structural model for phenylalkylamine binding to L-type calcium channels . The Journal of Biological Chemistry . 284 . 41 . 28332–42 . October 2009 . 19700404 . 2788883 . 10.1074/jbc.M109.027326 . free .
4. Alican I, Toker F, Arbak S, Yegen BC, Yalçin AS, Oktay S . Gastric lipid peroxidation, glutathione and calcium channel blockers in the stress-induced ulcer model in rats . Pharmacological Research . 30 . 2 . 123–35 . August 1994 . 7816741 . 10.1016/1043-6618(94)80004-9 .
5. Hung CR . Protective effects of lysozyme chloride and reduced glutathione on betel quid chewing-produced gastric oxidative stress and haemorrhagic ulcer in rats . Inflammopharmacology . 12 . 2 . 115–29 . May 2004 . 15265315 . 10.1163/1568560041352284 . 860321 .
6. Cheng RC, Tikhonov DB, Zhorov BS . Structural model for phenylalkylamine binding to L-type calcium channels . The Journal of Biological Chemistry . 284 . 41 . 28332–42 . October 2009 . 19700404 . 2788883 . 10.1074/jbc.M109.027326 . free .