Description
Diltiazem is a benzothiazepine-type compound that acts as an inhibitor of L-type Ca2+ channels. Diltiazem exhibits anti-arrhythmic, anti-anginal, anti-inflammatory, and cardioprotective activities. In animal models, diltiazem inhibits expression of IL-1β and CCL-12 and prevents formation of aortic aneurysms. In animal models of ischemia/reperfusion, diltiazem prevents dephosphorylation of connexin43 gap junction proteins. This compound may also inhibit cyclic nucleotide-gated (CNG) channels, which play a role in motor neuron excitability.
References
Mieth A, Revermann M, Babelova A, et al. L-type calcium channel inhibitor diltiazem prevents aneurysm formation by blood pressure-independent anti-inflammatory effects. Hypertension. 2013 Dec;62(6):1098-104. PMID: 24082061.
Matsushita S, Kurihara H, Watanabe M, et al. Inhibition of connexin43 dephosphorylation is involved in protective effects of diltiazem on cardiac function during hypoxic injury. Histol Histopathol. 2011 Mar;26(3):315-22. PMID: 21210344.
Podda MV, D'Ascenzo M, Leone L, et al. Functional role of cyclic nucleotide-gated channels in rat medial vestibular nucleus neurons. J Physiol. 2008 Feb 1;586(3):803-15. PMID: 18048449.
Joyal M, Cremer K, Pieper J, et al. Effects of diltiazem during tachycardia-induced angina pectoris. Am J Cardiol. 1986 Jan 1;57(1):10-4. PMID: 3942050.
