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Description: SSR-240612 HCl, the hydrochloride salt of SSR-240612, is a novel, potent, and orally bioactive specific non-peptide bradykinin B(1) receptor antagonist. SSR-240612 has the potential for the treatment of inflammation and chronic pain. SSR240612 acts by inhibiting the binding of (3)HLys(0)-des-Arg(9)-BK to the B(1) receptor in human fibroblast MRC5 and to recombinant human B(1) receptor expressed in human embryonic kidney cells with inhibition constants (K(i)) of 0.48 and 0.73 nM, respectively. SSR240612 inhibited Lys(0)-desAr(9)-BK (10 nM)-induced inositol monophosphate formation in human fibroblast MRC5, with an IC(50) of 1.9 nM. It also antagonized des-Arg(9)-BK-induced contractions of isolated rabbit aorta and mesenteric plexus of rat ileum with a pA(2) of 8.9 and 9.4, respectively.
References: Regul Pept. 2009 Jan 8; 152(1-3):67-72; J Pharmacol Exp Ther. 2004 May; 309(2):661-9.
Related CAS#: 465539-70-2 (free base)
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