Target intelligence / Profile preview

Dopamine receptor D1 (DRD1) (DRD1)

Target
DRD1
Molecular classification
G protein-coupled receptor, Receptor, D1-like dopamine receptor family, Class A GPCR
01

Overview

The Dopamine receptor D1 (DRD1) is the most abundant dopamine receptor in the central nervous system, primarily located in the striatum, nucleus accumbens, and cerebral cortex [UniProt: P21728]. As a member of the D1-like receptor family, it is a G protein-coupled receptor that typically couples to Gs or Golf to stimulate adenylate cyclase activity and increase cyclic AMP production [StatPearls: NBK538242]. It plays a fundamental role in regulating motor control, executive functions like working memory, and the brain's reward system [NCBI Gene: 1812]. In the periphery, DRD1 is involved in renal vasodilation and the regulation of blood pressure [PubMed: 16507349]. Pathological changes in D1 signaling are linked to neurological and psychiatric disorders such as Parkinson's disease, schizophrenia, and addiction [PubMed: 21945130]. Therapeutic strategies targeting DRD1 include agonists like fenoldopam for hypertension and various agents for Parkinson's motor symptoms [PubChem: CID 3342]. Conversely, many antipsychotic drugs act as antagonists at this receptor to manage symptoms of psychosis [PubMed: 11518473]. Research continues into selective D1 modulators to improve cognitive deficits in neuropsychiatric conditions without the side effects of non-selective dopaminergic drugs.

Other names
D1RD1 receptorDopamine D1 receptorDRD1DADR1
02

Mechanism of action

Agonism of the D1 receptor stimulates Gs or Golf proteins, activating adenylate cyclase and increasing intracellular cAMP levels, which modulates neuronal excitability and synaptic plasticity; antagonism blocks endogenous dopamine binding to inhibit these pathways [UniProt: P21728, StatPearls: NBK538242].

03

Biological functions

Signal transductionMotor controlCognitive functionReward processingRegulation of blood pressureSynaptic plasticity
04

Disease associations

Parkinson's diseaseSchizophreniaAttention deficit hyperactivity disorderHypertensionSubstance use disorderBipolar disorder
05

Safety considerations

Hypotension (due to peripheral vasodilation) [PubChem: CID 3342]TachycardiaDyskinesiaHallucinationsNauseaPotential for abuse/addiction
06

Interacting drugs

Fenoldopam

8 more in the full profile.

07

Biomarkers

Striatal D1 receptor density via PET imaging with [11C]SCH23390 [PubMed: 25635995]DRD1 gene polymorphisms (e.g., rs4532) [PubMed: 12662360]

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