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 Antagonists
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D1 Receptor Ligands
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D1 Receptor Related Products (105)
Related Products (105)
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UNC10062
0 ImagesCat. No.: HY-179241UNC10062 is a dopamine D1 receptor (D1R) positive allosteric modulator. UNC10062 specifically binds to the extracellular allosteric pocket (upper pocket) at the interface of transmembrane helices (TM) 1 and 7 of D1R. UNC10062 can increase dopamine potency and D1R-mediated cAMP production. UNC10062 can be used for the research of neurological disease, such as Parkinson's disease.
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Trepipam
0 ImagesCat. No.: HY-119463CAS No.: 20012-08-2Synonyms: Trimopam; SCH-12679Trepipam (Trimopam; SCH-12679) is a D1-dopamine receptor antagonist. Trepipam can reduce the self-injurious behavior in 6-OHDA-lesioned rats. Trepipam can be used in the research of epilepsy and anxiety neurosis.
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(S)-SKF-77434
0 ImagesCat. No.: HY-116430CAS No.: 139689-10-4Synonyms: (S)-APB(S)-SKF-77434 (Compound 11) ((S)-APB) is an enantiomer of SKF-77434 (HY-103417). (S)-SKF-77434 shows an affinity for the D1 receptor with an IC50 of 2800 nM. (S)-SKF-77434 can be used in the research of neuropsychiatric disorders.
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(S)-Remoxipride
0 ImagesCat. No.: HY-101313CAS No.: 80125-14-0Synonyms: (-)-Remoxipride(S)-Remoxipride ((-)-Remoxipride) is a selective dopamine D2-receptor antagonist with an IC50 value of 1.57 μM. (S)-Remoxipride can be used for the research of psychotic disorder.
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(Z)-Flupenthixol decanoate
0 ImagesCat. No.: HY-105657ACAS No.: 69079-98-7(Z)-Flupenthixol decanoate is the cis form of Flupenthixol decanoate. (Z)-Flupenthixol decanoate is a potent dopamine D1/D2 receptor antagonist. (Z)-Flupenthixol decanoate shows antipsychotic effect.
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Dihydrexidine
0 ImagesCat. No.: HY-101299ACAS No.: 123039-93-0Synonyms: DAR-0100Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity. Dihydrexidine can stimulate YAP phosphorylation.
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SCH-23390 maleate
0 ImagesCat. No.: HY-108400CAS No.: 87134-87-0Synonyms: R-(+)-SCH-23390 maleateSCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
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Raclopride tartrate
0 ImagesCat. No.: HY-108976CAS No.: 98185-20-7Raclopride tartrate is a selective dopamine D2/D3 receptor antagonist with potential antipsychotic effects. Raclopride tartrate binds to D2 and D3 receptors with Kis of 1.8 nM and 3.5 nM, respectively.
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UNC9815
0 ImagesCat. No.: HY-179240UNC9815 is a D1 dopamine receptor (D1R) orthosteric allosteric modulator (PAM). UNC9815 can dose-dependently enhance the functional efficacy of dopamine in β-inhibitory protein recruitment experiments and cAMP accumulation experiments. When used in combination with other PAMs, UNC9815 exhibits a significant synergistic enhancement effect. UNC9815 can be used to study neurological and psychiatric diseases such as Parkinson's disease and schizophrenia.
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SKF-83566 hydrochloride
0 ImagesCat. No.: HY-103430BCAS No.: 164265-49-0SKF-83566 hydrochloride is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM. SKF-83566 hydrochloride modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway. SKF-83566 hydrochloride acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2). SKF-83566 hydrochloride competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation. SKF-83566 hydrochloride is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect").
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Berupipam
0 ImagesCat. No.: HY-182585CAS No.: 150490-85-0Berupipam is a benzazepine-selective dopamine D1 receptor antagonist. Berupipam is used in the research of mental disorders.
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NRA-0562
0 ImagesCat. No.: HY-182504CAS No.: 244276-65-1NRA‑0562 is a dopamine antagonist with high affinities for dopamine D1/D2/D3/D4, 5‑HT2A and α1‑adrenoceptors. NRA-0562 dose‑dependently reverses induced suppression of firing activity in rat A9 and A10 midbrain dopamine neurons, with preferential potency at A10 neurons (ED50 = 0.3 mg/kg). NRA-0562 elevates Fos-like immunoreactivity in rat nucleus accumbens and dorsolateral striatum. NRA-0562 can be used for preclinical research on schizophrenia..
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PDE1-IN-12
0 ImagesCat. No.: HY-182327CAS No.: 191982-37-3PDE1-IN-12 (P78, the first compound in 12) is a PDE1 inhibitor. PDE1-IN-12 inhibits PDEl-mediated suppression of the dopamine D1 receptor intracellular pathway and can be used for narcolepsy.
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SKF-83566-PEG1-pomalidomide
0 ImagesCat. No.: HY-180814SKF-83566-PEG1-pomalidomide is an anti-tumor agent and is formed by the covalent connection of SKF-83566 (HY-103430A) (dopamine D1 receptor antagonist) and Pomalidomide (HY-10984) (immunomodulatory agent). SKF-83566-PEG1-pomalidomide can inhibit cancer cells invasion, migration and colony formation. SKF-83566-PEG1-pomalidomide can inhibit tumor growth and angiogenesis in MDA-MB-231 cell chicken embryo chorioallantoic membrane (CAM) xenograft model. SKF-83566-PEG1-pomalidomide can be used for research of breast cancer.
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Asenapine citrate
0 ImagesCat. No.: HY-10121BCAS No.: 1411867-74-7Synonyms: Org 5222 citrateAsenapine citrate, 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 citrate can be used in the research of schizophrenia and bipolar disorder.
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Flupentixol
0 ImagesFlupentixol is an orally active D1/D2 dopamine receptor antagonist and new PI3K inhibitor (PI3Kα IC50=127 nM). Flupentixol shows anti-proliferative activity to cancer cells and induces apoptosis. Flupentixol can also be used in schizophrenia, anxiolytic and depressive research.
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D1R antagonist 2
0 ImagesCat. No.: HY-178103D1R antagonist 2 (Compound 13a) is a BBB-penetrable D1R antagonist with IC50s of 35.6 and 70 nM for cAMP-based D1R and β-arrestin-based D1R, respectively. D1R antagonist 2 effectively antagonizes D1R-mediated cAMP and β-arrestin recruitment. D1R antagonist 2 can be used for neurodegenerative and neuropsychiatric diseases such as schizophrenia, Parkinson’s disease and Alzheimer’s disease research.
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Loxapine hydrochloride
0 ImagesCat. No.: HY-17390BCAS No.: 54810-23-0Loxapine hydrochloride is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
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Agroclavine
0 ImagesAgroclavine acts as an agonist of the D1-dopamine receptor and α1-adrenergic receptor. Agroclavine enhances the sensitivity of the brain to magnetic fields; it impairs spatial memory without affecting hippocampal long-term potentiation (LTP). Agroclavine exerts bidirectional regulatory effects on immune activity: it enhances NK cell activity with low toxicity under normal conditions, while it inhibits NK cell activity and exhibits significant cardiac and hepatic toxicity under stress conditions. Agroclavine can be used for research on neuroelectrophysiology, learning and memory, and immunoregulation.
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Dopamine D3 receptor agonist-2
0 ImagesCat. No.: HY-183776CAS No.: 1000031-37-7Dopamine D3 receptor agonist-2 is a selective dopamine D3 receptor partial agonist with a Ki of 0.268 nM. Dopamine D3 receptor agonist-2 exhibits 29-fold selectivity over dopamine D2 receptor (Ki= 7.67nM).
