Arvanitis Argyrios G, Rescinito Joseph T, Arnold Charles R, Wilde Richard G, Fitzgerald Lawrence W, Zaczek Robert, Hartig Paul R, Grossman Scott, Arneric Stephen P, Gilligan Paul J, Olson Richard E, Robertson David W
Discovery Chemistry-Wilmington, Bristol-Myers Squibb Company, Experimental Station, DE 19880, USA.
Bioorg Med Chem Lett. 2003 Jan 6;13(1):129-31. doi: 10.1016/s0960-894x(02)00834-x.
A series of high affinity CRF receptor ligands with an imidazo[4,5-c]pyridine core is described. Individual analogues were synthesized and tested in vitro in rat brain receptors to determine binding affinity. The best compound was further tested in the dog N-in-1 pharmacokinetic model to assess oral bioavailability at 1 mg/kg po.
描述了一系列具有咪唑并[4,5-c]吡啶核心的高亲和力促肾上腺皮质激素释放因子（CRF）受体配体。合成了各个类似物并在大鼠脑受体中进行体外测试以确定结合亲和力。对最佳化合物进一步在犬N合一药代动力学模型中进行测试，以评估口服1mg/kg时的生物利用度。
