Song Cai, Peter Tuohy, Chunlong Ma, Naoya Kitamura, Kimberly Gomez, Yuan Zhou, Dongzhi Ran, Shreya Sai Bellampalli, Jie Yu, Shizhen Luo, Angie Dorame, Nancy Yen Ngan Pham, Gabriella Molnar, John M Streicher, Marcel Patek, Samantha Perez-Miller, Aubin Moutal, Jun Wang, Rajesh Khanna
The voltage-gated calcium channels CaV3.1-3.3 constitute the T-type subfamily, whose dysfunctions are associated with epilepsy, psychiatric disorders, and chronic pain. The unique properties of low voltage-activation, faster inactivation, and slower deactivation of these channels support their role in modulation of cellular excitability and low-threshold firing. Thus, selective T-type calcium channel antagonists are highly sought after. Here, we explored Ugi-azide multicomponent reaction (MCR) products to identify compounds targeting T-type calcium channel...
June 10, 2020: Pain