TTA-A2 was found to inhibit all three subtypes of low-voltage-gated T-type channels (CaV3.1, CaV3.2, and CaV3.3) with comparable potencies. Changing membrane resting potentials from −100 to −80 mV enhanced compound potency by ∼40-fold, from an IC50 of ∼4 μM to 0.1 μM, respectively, indicating state dependence of inhibition. in vivo studies have demonstrated that TTA-A2 reduces absence epilepsy seizures, pain perception, nicotine self-administration and weight gain. It also improves the quality of sleep and displays antipsychotic properties.
产品描述
A Blocker of T-type CaV Channels
产品形式
Low-voltage-activated (T-type/Cav3) Ca2+ channels are a subclass of voltage-dependent Ca2+ channels allowing Ca2+ entry near the resting potential of most cells. Various synthetic T-channel blockers have been described in the past few years including TTA-A2, a potent and state-dependent, and highly selective T-type CaV antagonist.