Gu Y G, Bayburt E K, Michaelides M R, Lin C W, Shiosaki K
Neuroscience Research, Pharmaceutical Discovery, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
Bioorg Med Chem Lett. 1999 May 17;9(10):1341-6. doi: 10.1016/s0960-894x(99)00214-0.
The title compounds were synthesized by replacing the thiophene moiety of A-86929(2a) with variously substituted pyridines. Dopamine D-1 and D-2 binding and adenylate cyclase assays indicate that 4,6-diaza compounds 15 are potent and selective full D1 agonists when R1 is H or a small substituent and R2 = H, with D1 binding affinity and adenylate cyclase functional potency equivalent to that of A-86929(2a).
通过用各种取代的吡啶取代A-86929(2a)的噻吩部分合成了标题化合物。多巴胺D-1和D-2结合以及腺苷酸环化酶测定表明,当R1为H或小取代基且R2 = H时,4,6-二氮杂化合物15是强效且选择性的完全D1激动剂,其D1结合亲和力和腺苷酸环化酶功能效力与A-86929(2a)相当。