D1 Receptor
Dopamine D1 receptor regulates motor function, reward processing, cognition, and brain gene-expression programs through D1-like dopaminergic signaling[1][2]. Mechanistically, D1 receptor activation stimulates adenylyl cyclase signaling, engages PKA-linked pathways, and can drive ERK1/2 phosphorylation in dopamine-denervated striatum[3][4]. In Parkinsonian models, D1 receptor agonists restore motor behavior, while abnormal D1-mediated signaling contributes to L-Dopa-related rewarding effects and dyskinetic molecular responses[5][6]. Compared with related dopamine receptor isoforms, D1 and D2 receptors act in separate basal-ganglia neuronal populations, and D1 receptor effects can differ from D2-linked modulation in cannabinoid, sensorimotor-gating, and antiparkinsonian assays[1][7][8]. For experimental applications, selective agonists and antagonists such as SKF81297, SCH23390, adrogolide, and non-catechol D1 agonists help define receptor selectivity, signaling bias, β-arrestin recruitment, receptor internalization, and disease-model efficacy[5][9][10][11].
References:
- [1]. Cadet JL, et al. Dopamine D1 receptors, regulation of gene expression in the brain, and neurodegeneration. CNS Neurol Disord Drug Targets. 2010 Nov;9(5):526-38. [Content Brief]
- [2]. Kimura Y, et al. Ultra-high-field pharmacological functional MRI of dopamine D1 receptor-related interventions in anesthetized rats. Pharmacol Res Perspect. 2023 Apr;11(2):e01055. [Content Brief]
- [3]. Fieblinger T, et al. Mechanisms of dopamine D1 receptor-mediated ERK1/2 activation in the parkinsonian striatum and their modulation by metabotropic glutamate receptor type 5. J Neurosci. 2014 Mar 26;34(13):4728-40. [Content Brief]
- [4]. Hao JR, et al. L-Stepholidine rescues memory deficit and synaptic plasticity in models of Alzheimer's disease via activating dopamine D1 receptor/PKA signaling pathway. Cell Death Dis. 2015 Nov 5;6(11):e1965. [Content Brief]
- [5]. Vermeulen RJ, et al. The selective dopamine D1 receptor agonist, SKF 81297, stimulates motor behaviour of MPTP-lesioned monkeys. Eur J Pharmacol. 1993 Apr 22;235(1):143-7. [Content Brief]
- [6]. Plewnia C, et al. Rewarding properties of L-Dopa in experimental parkinsonism are mediated by sensitized dopamine D1 receptors in the dorsal striatum. Mol Psychiatry. 2025 Mar;30(3):976-985. [Content Brief]
- [7]. Daigle TL, et al. Opposite function of dopamine D1 and N-methyl-D-aspartate receptors in striatal cannabinoid-mediated signaling. Eur J Neurosci. 2011 Nov;34(9):1378-89. [Content Brief]
- [8]. Gresack JE, et al. Inhibition of phosphodiesterase 10A has differential effects on dopamine D1 and D2 receptor modulation of sensorimotor gating. Psychopharmacology (Berl). 2014 May;231(10):2189-97. [Content Brief]
- [9]. Giardina WJ, et al. Adrogolide HCl (ABT-431; DAS-431), a prodrug of the dopamine D1 receptor agonist, A-86929: preclinical pharmacology and clinical data. CNS Drug Rev. 2001 Fall;7(3):305-16. [Content Brief]
- [10]. Gray DL, et al. Impaired β-arrestin recruitment and reduced desensitization by non-catechol agonists of the D1 dopamine receptor. Nat Commun. 2018 Feb 14;9(1):674. [Content Brief]
- [11]. Sahlholm K, et al. Estimation of Dopamine D1 Receptor Agonist Binding Kinetics Using Time-Resolved Functional Assays: Relation to Agonist-Induced Receptor Internalization by Investigational Antiparkinsonian Therapeutics. ACS Chem Neurosci. 2025 Jul 2;16(13):2502-2512. [Content Brief]
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D1 Receptor Inhibitors
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D1 Receptor Agonists
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D1 Receptor Antagonists
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D1 Receptor Ligands
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D1 Receptor Related Products (107)
Related Products (107)
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Loxapine
0 ImagesLoxapine is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
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A68930 hydrochloride
0 ImagesA68930 hydrochloride, as a dopamine D1 receptor agonist, can be used for the research of bronchiectasis.
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Iloperidone
0 ImagesSynonyms: HP 873Iloperidone (HP 873) is a D2/5-HT2 receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms.
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UNC9994 hydrochloride
0 ImagesUNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.
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Asenapine
0 ImagesSynonyms: Org 5222Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.
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Lumateperone tosylate
0 ImagesSynonyms: ITI-007 tosylateLumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.
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Spiperone hydrochloride
0 ImagesSpiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities.
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SKF 83959
0 ImagesSKF83959 is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 can be used for the research of Alzheimer's disease and depression.
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Ecopipam
0 ImagesSynonyms: SCH 39166Ecopipam (SCH 39166) is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam can be used for the research of schizophrenia and obesity.
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D-Tetrahydropalmatine
0 ImagesD-Tetrahydropalmatine is an isoquinoline alkaloid, mainly in the genus Corydalis. D-Tetrahydropalmatine is a dopamine (DA) receptor antagonist with preferential affinity toward the D1 receptors. D-Tetrahydropalmatine is a potent organic cation transporter 1 (OCT1) inhibitor.
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Halopemide
0 ImagesHalopemide is a potent phospholipase D (PLD) inhibitor, with IC50s of 220 and 310 nM for human PLD1 and PLD2, respectively. Halopemid is a dopamine receptors antagonist, and acts a psychotropic agent.
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Bacopaside X
0 ImagesSynonyms: Bacopaside VIIBacopaside X is found in Bacopa monnieri, and shows a binding affinity toward the D1 receptor.
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L-Stepholidine
0 ImagesSynonyms: Stepholidine; (-)-Stepholidine; L-SPDL-Stepholidine (Stepholidine) is an alkaloid. L-Stepholidine exhibits mixed dopamine D1 receptor agonist and D2 antagonist properties. L-Stepholidine has neuroprotective effect. L-Stepholidine can be used for the researches of neurological disease, such as Parkinson disease, Alzheimer's disease and opiate addiction.
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SKF 83822
0 ImagesSKF 83822 is an atypical agonist of dopamine D1 receptor. SKF 83822 activates adenylyl cyclase (AC), but not phospholipase C (PLC). SKF 83822 is also proved to stimulate AC via cAMP production. SKF 83822 can be used for research of schizophrenia.
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Pergolide
0 ImagesSynonyms: LY127809 free basePergolide (LY127809 free base), an Ergoline derivative, is a potent and orally active dopamine D1 and D2 receptor agonist. Pergolide can be used for Parkinson's disease and hyperprolactinaemia research.
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CY 208-243
0 ImagesCY 208-243 is a selective dopamine D1 receptor agonist which exhibits antiparkinsonian activity.
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(Rac)-Tavapadon
0 ImagesSynonyms: (Rac)-PF-06649751; (Rac)-CVL-751(Rac)-Tavapadon ((Rac)-PF-06649751) is a potent and selective noncatechol dopamine D1 receptor agonist. (Rac)-Tavapadon displays potent full agonism in the GS activation assay as well as partial agonism in the β-arrestin2 recruitment assay (GS-cAMP, EC50=0.8 nM; β-arrestin2, EC50=68 nM). (Rac)-Tavapadon has antiparkinsonian activity.
