trans-2,6-, 3,6- and 4,6-Diaza-5,6,6a,7,8,12b-hexahydrobenzo[C]phenanthrene-10,11-diols as dopamine agonists

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).