trans-2,6-,3,6- and 4,6-diaza-5,6,6a,7,8,12b-hexahydro-benzo[c]phenanthrene-10,11- diols as dopamine agonists

Y G Gu; E K Bayburt; M R Michaelides; C W Lin; K Shiosaki

doi:10.1016/s0960-894x(99)00214-0

trans-2,6-,3,6- and 4,6-diaza-5,6,6a,7,8,12b-hexahydro-benzo[c]phenanthrene-10,11- diols as dopamine agonists

Bioorg Med Chem Lett. 1999 May 17;9(10):1341-6. doi: 10.1016/s0960-894x(99)00214-0.

Authors

Y G Gu¹, E K Bayburt, M R Michaelides, C W Lin, K Shiosaki

Affiliation

¹ Neuroscience Research, Pharmaceutical Discovery, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.

PMID: 10360732
DOI: 10.1016/s0960-894x(99)00214-0

Abstract

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).

MeSH terms

Dopamine Agonists / chemical synthesis
Dopamine Agonists / chemistry*
Dopamine Agonists / metabolism*
Humans
Phenanthridines / chemical synthesis
Phenanthridines / chemistry*
Phenanthridines / metabolism*
Receptors, Dopamine D1 / metabolism
Receptors, Dopamine D2 / metabolism
Structure-Activity Relationship

Substances

Dopamine Agonists
Phenanthridines
Receptors, Dopamine D1
Receptors, Dopamine D2