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.

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Liu D, Dijkstra D, de Vries JB, Wikstrom HV

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.

Bioorg Med Chem. 2008 Mar 15;16(6):3438-44. doi: 10.1016/j.bmc.2007.06.036. Epub 2007 Jun 23.

PubMed ID
18313303 [ View in PubMed
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Abstract

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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ApomorphineDopamine D1 receptorEC 50 (nM)52N/AN/ADetails
ApomorphineDopamine D2 receptorEC 50 (nM)4N/AN/ADetails
DopamineDopamine D1 receptorEC 50 (nM)35N/AN/ADetails
DopamineDopamine D2 receptorEC 50 (nM)43N/AN/ADetails
PramipexoleDopamine D2 receptorEC 50 (nM)5N/AN/ADetails