SSR240612

SSR240612 is a potent, orally active, and selective non-peptide antagonist of the bradykinin B1 receptor. It exhibits high affinity for the B1 receptor (Kis = 0.48–0.73 nM) and much lower affinity for the B2 receptor (Kis = 358–481 nM), demonstrating strong selectivity[4][6]. Developed originally by Sanofi-Synthélabo (now Sanofi), it was investigated as an analgesic and anti-inflammatory agent targeting conditions such as neuropathic pain, inflammation, and central nervous system disorders[2][3][5]. In preclinical models, SSR240612 reversed tactile and cold allodynia in rats with insulin-induced neuropathy and reduced inflammatory pain behaviors in mice[3][8]. Its mechanism of action involves antagonism of the bradykinin B1 receptor on sensory nerves and spinal cord neurons to inhibit pain signaling pathways[8]. Despite promising preclinical results and advancement to phase II clinical trials for chronic pain indications in France, no further development has been reported since 2009[2].

Other names

SSR-240612SSR240612SSR 240612Ssr-240612 free baseSsr240612 free baseSsr 240612 free base