2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.

Selective bradykinin (BK) B 1 receptor antagonists could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure activity relationships of the structurally novel HTS lead compound 1 provided potent hBK B 1 receptor antagonists with excellent receptor occupancy in the CNS of hBK B 1 transgenic rats.

[1]  M. Bock,et al.  Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes. , 2007, Bioorganic & medicinal chemistry letters.

[2]  M. Bock,et al.  Development of orally bioavailable and CNS penetrant biphenylaminocyclopropane carboxamide bradykinin B1 receptor antagonists. , 2007, Journal of medicinal chemistry.

[3]  M. Mori,et al.  Reduced Nerve Injury-Induced Neuropathic Pain in Kinin B1 Receptor Knock-Out Mice , 2005, The Journal of Neuroscience.

[4]  M. Bock,et al.  Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies. , 2004, Bioorganic & Medicinal Chemistry Letters.

[5]  M. Bock,et al.  2,3-diaminopyridine bradykinin B1 receptor antagonists. , 2004, Journal of medicinal chemistry.

[6]  M. Bock,et al.  Pharmacological characterization and radioligand binding properties of a high-affinity, nonpeptide, bradykinin B1 receptor antagonist. , 2004, European journal of pharmacology.

[7]  M. Bock,et al.  Generation and Characterization of a Human Bradykinin Receptor B1 Transgenic Rat as a Pharmacodynamic Model , 2004, Journal of Pharmacology and Experimental Therapeutics.

[8]  W. Xie,et al.  Orphan nuclear receptor-mediated xenobiotic regulation in drug metabolism. , 2004, Drug discovery today.

[9]  M. Bock,et al.  Discovery of a potent, non-peptide bradykinin B1 receptor antagonist. , 2003, Journal of the American Chemical Society.

[10]  J. Calixto,et al.  The use of kinin B1 and B2 receptor knockout mice and selective antagonists to characterize the nociceptive responses caused by kinins at the spinal level , 2002, Neuropharmacology.

[11]  J. Hochman,et al.  Evaluation of drug interactions with P-glycoprotein in drug discovery: in vitro assessment of the potential for drug-drug interactions with P-glycoprotein. , 2002, Current drug metabolism.

[12]  T. Willson,et al.  Pxr, car and drug metabolism , 2002, Nature Reviews Drug Discovery.

[13]  R. Couture,et al.  Kinin receptors in pain and inflammation. , 2001, European journal of pharmacology.

[14]  Q. Ma,et al.  Basal expression of bradykinin B1 receptor in peripheral sensory ganglia in the rat , 2000, Neuroreport.

[15]  J. Winter,et al.  Bradykinin B1 receptor is constitutively expressed in the rat sensory nervous system , 2000, Neuroscience Letters.

[16]  M. Bock,et al.  Bradykinin antagonists: new opportunities. , 2000, Current opinion in chemical biology.

[17]  T. Walther,et al.  Hypoalgesia and altered inflammatory responses in mice lacking kinin B1 receptors. , 2000, Proceedings of the National Academy of Sciences of the United States of America.

[18]  A. Pike,et al.  Fluorination of 3-(3-(piperidin-1-yl)propyl)indoles and 3-(3-(piperazin-1-yl)propyl)indoles gives selective human 5-HT1D receptor ligands with improved pharmacokinetic profiles. , 1999, Journal of medicinal chemistry.

[19]  D. Regoli,et al.  Pharmacology of bradykinin and related kinins. , 1980, Advances in experimental medicine and biology.