一种功能选择性D3激动剂的设计与合成及其经鼻内途径的体内递送。
Design and synthesis of a functionally selective D3 agonist and its in vivo delivery via the intranasal route.
作者信息
Blagg Julian, Allerton Charlotte M N, Batchelor David V J, Baxter Andrew D, Burring Denise J, Carr Christopher L, Cook Andrew S, Nichols Carly L, Phipps Joanne, Sanderson Vivienne G, Verrier Hugh, Wong Stephen
机构信息
Pfizer Global Research & Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
出版信息
Bioorg Med Chem Lett. 2007 Dec 15;17(24):6691-6. doi: 10.1016/j.bmcl.2007.10.059. Epub 2007 Oct 22.
This paper reports the synthesis and biological activity of a novel series of aryl-morpholine dopamine receptor agonists. Several compounds show high levels of functional selectivity for the D3 over the D2 dopamine receptor. Compound 26 has >1000-fold functional selectivity and has been successfully progressed in vivo using an intranasal delivery route.
本文报道了一系列新型芳基吗啉多巴胺受体激动剂的合成及其生物活性。几种化合物对D3多巴胺受体的功能选择性高于D2多巴胺受体。化合物26具有大于1000倍的功能选择性，并已通过鼻内给药途径在体内成功推进研究。
Zotero 插件