L-type Ca++ CP γ6 Inhibitors

The inhibitors listed above are all small molecules that can bind to L-type calcium channels and prevent the influx of calcium ions into cells. This inhibition can alter the function of cells in many ways, as calcium signals are essential for a broad range of cellular processes, including muscle contraction, neurotransmitter release, and gene expression. L-type calcium channel inhibitors are a diverse group of molecules that share the ability to bind to and block the L-type calcium channels. They are characterized by different chemical structures, including dihydropyridines (e.g., nifedipine, amlodipine, nimodipine), benzothiazepines (e.g., diltiazem), and phenylalkylamines (e.g., verapamil). These classes of molecules interact with different parts of the L-type calcium channel, which can result in varying degrees of selectivity and duration of action.

Dihydropyridine inhibitors, such as nifedipine, mainly act on the voltage-sensitive L-type channels found in the vascular smooth muscle, causing vasodilation. Benzothiazepine and phenylalkylamine inhibitors, like diltiazem and verapamil, respectively, have additional effects on the heart, reducing heart rate and contractility. The action of these inhibitors is based on their ability to fit into the L-type channel's drug-binding domains, stabilizing the inactive state of the channel and thus reducing the probability of channel opening in response to depolarization. This leads to a decrease in intracellular calcium concentration, which in turn affects cellular processes that are dependent on calcium as a second messenger.