RGNCY-0076 (10 T-type channel inhibitor)
Compound 10 is a potent T-type calcium channel inhibitor. This compound exhibits a significant pain-alleviating effect in STZ-induced peripheral diabetic neuropathy rat models and has favorable pharmakokinetic properties. This compound demonstrates a rapid onset of activity against mechanical allodynia. In addition, co-administration of compound 10 with gabapentin at low doses results in a positive synergistic effect in a in vivo diabetic neuropathic pain model. These data demonstrate the importance of α-1H T-type calcium channels in the treatment of diabetic neuropathic pain. α-1H T-type calcium channels IC50 = 2.52 + 0.83 μM.
Systematic Name: 2-((1-(4-fluorophenyl)-5-isopropyl-1H-pyrazol-3-yl)methyl)-2,3-dihydrobenzo[d]isothiazole 1,1-dioxide
Molecular Weight: 385.46
Tags: Diabetes, RGNCY-0076, compound 10, 10, DNP, neuropathic pain, neuropathy, calcium channel, T-type