A novel synthesis and pharmacological evaluation of a potential dopamine D1/D2 agonist: 1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-6,7-diol.
Previously, we have demonstrated that enone prodrugs of dopaminergic catecholamines represent a new type of dopamine (DA) agonist. Trans-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-6,7-diol (TL-334), the active form of trans-1-propyl-2,3,4,4a,5,7,8,9,10,10a-decahydro-1H-benzo[g]quinolin-6-one (GMC-6650), in vivo showed an extremely potent dopaminergic activity. Here, we report a novel synthesis and a pharmacological evaluation of TL-334 by means of microdialysis.
Liu
Danyang
D
Department of Medicinal Chemistry, University Centre for Pharmacy, University of Groningen, Antonius Deusinglaan 1, NL-9713 AV Groningen, The Netherlands.
Dijkstra
Durk
D
de Vries
Jan B
JB
Wikström
Håkan V
HV
D000818:Animals; D001923:Brain Chemistry; D002460:Cell Line; D003956:Dialysis; D018491:Dopamine Agonists / Q000138:chemical synthesis; D006801:Humans; D008832:Microchemistry / Q000379:methods; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017447:Receptors, Dopamine D1 / Q000819:agonists*; D017448:Receptors, Dopamine D2 / Q000819:agonists*; D014162:Transfection
D018491:Dopamine Agonists; D011804:Quinolines; D017447:Receptors, Dopamine D1; D017448:Receptors, Dopamine D2