RGNCY-0076 (10 T-type channel inhibitor)

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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.

SMILE:  O=S1(C2=CC=CC=C2CN1CC3=NN(C4=CC=C(F)C=C4)C(C(C)C)=C3)=O

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

Formula:  C20H20FN3O2S

PMID:  28799755