Dopamine receptor D₁, also known as DRD1, is a human gene.

This gene encodes the D₁ subtype of the dopamine receptor. The D₁ subtype is the most abundant dopamine receptor in the central nervous system. This G-protein coupled receptor stimulates adenylyl cyclase and activates cyclic AMP-dependent protein kinases. D₁ receptors regulate neuronal growth and development, mediate some behavioral responses, and modulate dopamine receptor D₂-mediated events. Alternate transcription initiation sites result in two transcript variants of this gene.^[1]

Ligands

There are a number of ligands selective for D₁ over the D₂, D₃ and D₄ receptors, but note that all of the D₁-preferring ligands developed so far also bind to D₅ and so cannot be said to be truly selective.

Agonists

• (+)-trans-2,3-dihydroxy-6a,7,8,12b-tetrahydro-6H-chromeno[3,4-c]isoquinoline, a chromano (oxygen) bioisostere of dihydrexidine, potent full agonist, selective over D₂^[2]
• A-86929, full agonist^[3][4]
• SKF-81297 (6-Chloro-2,3,4,5-tetrahydro-1-phenyl-1H-3-benzazepine)
• SKF-38393 (1-Phenyl-2,3,4,5-tetrahydro-(1H)-3-benzazepine-7,8-diol) - partial agonist

Antagonists

• SCH-23390(7-chloro-3-methyl-1-phenyl-1,2,4,5-tetrahydro-3-benzazepin-8-ol)
• SCH-39166 ((6aS-trans)-11-Chloro-6,6a,7,8,9,13b-hexahydro-7-methyl-5H-benzo[d]naphth[2,1-b]azepin-12-ol)
• SKF-83566 (8-Bromo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepin-7-ol) - selective over other dopamine receptors but also blocks 5HT_2A

Chemical structures of selective D₁ receptor agonists.^[2][3]

See also

• Dopamine receptor

References

Further reading

External links