Cav1.2 plays an important role in the contraction of the heart. It is particularly important and well known for its expression in the heart where it mediates L-type currents, which causes calcium-induced calcium release from the ER Stores via ryanodine receptors. The block of calcium current can lead to AV block and negative inotropy. Cav1.2 depolarizes at -30mV and helps define the shape of the action potential in cardiac and smooth muscle.
Fig. 1 AngII increases twitch Ca2+ transients and L-type Ca2+ channel currents in immature cardiomyocytes.
Testing of compounds for interactions with Cav1.2 channel in Acroscell identify potential cardiac risk in humans and can be used as a screen in development candidate selection.
Acroscell currently provide manual patch clamp assay using acutely isolated animal cardiomyocytes or HEK 293-Cav 1.2 cell line to test drug's inhibition or potentiating effect on Cav1.2 channels. This assay is one of the preclinical cardiac safety assays highly recommended in the pharmaceutical industry.
Tissue-specific Location: heart, smooth muscle, neurons and endocrine tissue.
Therapeutic Targets: cardiac arrhythmia and hypertension.