Inhibition of human N- and T-type calcium channels by an ortho -phenoxyanilide derivative, MONIRO-1

What is it about?

Neuropathic pain affects more than 3% of the population and existing therapies only provide relief in 50% of patients. One way of treating neuropathic pain is to block the transmission of pain signals. N-type calcium channels and more recently T-type calcium channels have been implicated in pain transmission. Herein, we describe the synthesis and testing of a non-peptidic small molecule that exhibits 10-fold higher affinity for the T-type (Cav3.1, Cav3.2 and Cav3.3) calcium channel over the N-type (Cav2.2) calcium channel and is 100-fold more active at T-type calcium channels, than other ion channels examined. These rarely seen properties are of considerable interest from the viewpoint of developing improved treatments for a debilitating disorder.

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