666256-06-0

NGD9002 is a new generation, topology 2 selective corticotropin releasing factor-1 (CRF-1) receptor antagonist.

NGD9002 free base is a new generation of selective corticotropin-releasing factor-1 (CRF-1) receptor antagonist with inhibitory activity on CRF-induced colonic function stimulation. NGD9002 free base can reduce CRF-induced fecal output response and show an inhibitory IC50 value of 4.3 mg/kg. NGD9002 free base can effectively block CRF-induced colonic secretory motility stimulation at the highest dose and reduce acute water avoidance-induced defecation. NGD9002 free base can also prevent the occurrence of pain hypersensitivity reactions to repeated colonic distension[1].

[1] The newly developed CRF1-receptor antagonists, NGD 98-2 and NGD 9002, suppress acute stress-induced stimulation of colonic motor function and visceral hypersensitivity in rats DOI:10.1371/journal.pone.0073749