BMS-192364 is targeting the Gα-RGS interaction to produce an inactive Gα-RGS complex. BMS-192364 reduces urinary bladder contraction and exert RGS-agonist properties by increasing the action of GAPs on Gq proteins. BMS-192364 inhibits calcium flux.
References:
[1]. Kevin Fitzgerald, et al. Chemical genetics reveals an RGS/G-protein role in the action of a compound. PLoS Genet. 2006 Apr;2(4):e57.
[2]. Maciej Salaga, et al. RGS proteins as targets in the treatment of intestinal inflammation and visceral pain: New insights and future perspectives. Bioessays. 2016 Apr;38(4):344-54.
[3]. David P Basile, et al. A GAP in our knowledge of vascular signaling in acute kidney injury. Kidney Int. 2011 Aug;80(3):233-5.
















