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].
Références:
- [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 Activators
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D1 Receptor Modulators
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D1 Receptor Control
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D1 Receptor Ligands
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D1 Receptor Produits associés (105)
Produits associés (105)
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Adrogolide
0 ImagesCat. No.: HY-160718CAS No.: 171752-56-0Synonyms: ABT-431; DAS-431Adrogolide is an A-86929 (HY-171472) prodrug and dopamine D1 receptor agonist. Adrogolide is converted rapidly in plasma to A-86929. Adrogolide improves behavioral disability and locomotor activity scores. Adrogolide can also attenuate the ability of Cocaine to induce Cocaine-seeking behavior. Adrogolide can be used in the research of Parkinson's disease.
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SKF 38393 hydrobromide
0 ImagesCat. No.: HY-12237CAS No.: 20012-10-6Synonyms: (±)-SKF-38393 hydrobromideSKF 38393 ((±)-SKF-38393) hydrobromide is a selective agonist of the dopamine D1 receptor (D1DR) with an IC50 of 110 nM.
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A-77636
0 ImagesCat. No.: HY-141496CAS No.: 778546-51-3A-77636 is an orally active, potent, selective and long-acting dopamine D1 receptor agonist (pEC50 = 8.13; EC50 = 1.1 nM). A-77636 shows the highest affinity (pKi = 7.40 ± 0.09; Ki = 39.8 nM) for the dopamine D1 receptor. A-77636 shows antiparkinsonian activity.
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A-69024
0 ImagesCat. No.: HY-116773CAS No.: 58939-37-0A-69024 is a selectivity dopamine D-1 receptor antagonist with the Ki values of 12.6 nM and 1290 nM for dopamine D-1 receptor and dopamine D-2 receptor, respectively.
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PF-4211
0 ImagesCat. No.: HY-149168CAS No.: 2292115-41-2PF-4211 is a selective non-catechol D1R agonist with a Ki value of 2.2 μM.. PF-4211 activates adenylate cyclase by binding to D1R, thereby increasing intracellular cAMP levels. PF-4211 can be used in research related to Parkinson's disease and schizophrenia.
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(Rac)-Rotigotine-d7 (hydrochloride)
0 ImagesCat. No.: HY-15394SCAS No.: 3026226-88-7Synonyms: N-0437-d7 (hydrochloride)(Rac)-Rotigotine-d7 (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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SKF 38393
0 ImagesCat. No.: HY-12520CAS No.: 67287-49-4SKF 38393 is a selective dopamine D1 receptor agonist. SKF 38393 activates the cAMP signaling pathway and promotes dopamine release in the developing rat striatum. SKF 38393 inhibits MCF-7 breast cancer cell proliferation (IC50=0.1 μM). SKF 38393 is promising for research of neurodevelopmental disorders, dopamine-related diseases (e.g., Parkinson’s, dopamine deficiency), and cancers.
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SKF83822 hydrobromide
0 ImagesCat. No.: HY-103411CAS No.: 74115-10-9SKF83822 hydrobromide is a potent dopamine D1 receptor agonist. SKF83822 hydrobromide activates Gs/olf/adenylyl cyclase (AC)-coupled D1 receptors, but not phospholipase C (PLC)-coupled D1-like receptors.
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A 80426
0 ImagesCat. No.: HY-120037CAS No.: 152148-63-5A 80426 is an orally active serotonin (5-HT uptake) inhibitor (IC50 = 13 nM; Ki = 3.8 nM) and α2-Adrenoceptor receptor antagonist (Ki = 2 nM). A 80426 shows weak antagonistic effect to dopamine D1 receptor (Ki = 744 nM) and D2 receptor (Ki = 52 nM). A 80426 upregulates the expression and activity of TRPV1, activates the NF-κB and PI3K pathways, and reduces the levels of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α. A 80426 can be used in research related to inflammatory pain and depression.
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(+)-Razpipadon
0 ImagesCat. No.: HY-141495BCAS No.: 1643489-51-3Synonyms: (+)-PW0464(+)-Razpipadon ((+)-PW0464) is a selective D1 dopamine receptor agonist belonging to non-catechol compounds. (+)-Razpipadon activates the G protein pathway, while restricting β-arrestin coupling through the proximity effect of fluoromethyl-TM5, thereby achieving specific regulation of downstream pathways. (+)-Razpipadon can be used in studies related to Parkinson's disease.
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FLA-797
0 ImagesCat. No.: HY-182381CAS No.: 84226-14-2FLA-797 is a brain-penetrant dopamine D2 receptor blocker and very low affinity for dopamine D1 receptors. FLA-797 selectively binds to and blocks postsynaptic dopamine D2 receptors. FLA-797 induces catalepsy in male rats. FLA-797 blocks dopamine agonist-induced hypothermia in male rats. FLA-797 contributes marginally to the dopamine D2 receptor-blocking activity of Remoxipride (HY-101313) in male rats. FLA-797 does not mimic the atypical antipsychotic profile of Remoxipride. FLA-797 can be used for research on mental disorders.
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SKF-83566 (Standard)
0 ImagesCat. No.: HY-103430ARCAS No.: 99295-33-7SKF-83566 (Standard) is the analytical standard of SKF-83566 (HY-103430A). This product is intended for research and analytical applications. SKF-83566 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 modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway. SKF-83566 acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2). SKF-83566 competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation. SKF-83566 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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Alentemol
0 ImagesCat. No.: HY-124524CAS No.: 112891-97-1Synonyms: U-66444B free baseAlentemol (U-66444B (free base)) is a blood-brain barrier-permeable dopamine receptor D1, D2, D3, and D4 agonist. Alentemol inhibits dopamine release, reduces dopamine synthesis, regulates dopamine metabolism, suppresses the impulse activity of dopaminergic neurons, and decreases the impulse frequency of dopaminergic neurons in the substantia nigra pars compacta and ventral tegmental area. Alentemol is applicable to research related to schizophrenia.
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Fenoldopam
0 ImagesCat. No.: HY-B0735CAS No.: 67227-56-9Synonyms: SKF 82526Fenoldopam (SKF-82526) is a selective dopamine D1 receptor agonist. Fenoldopam binds to rat D1B dopamine receptors (Kd = 11 nM) and human D1A receptors (Kd = 17 nM) in COS-7 cell membranes expressing the cloned receptors. Fenoldopam modulates dopamine receptor expression, induces vasorelaxation in vascular tissues, reverses glomerular hyperfiltration in rat models, increases intracellular cAMP levels, promotes DARPP-32 phosphorylation in small cell lung cancer (SCLC) cells, inhibits cytokine secretion, and downregulates T cell activation markers in activated human T cells. Fenoldopam can be used for research on hypertension, acute kidney injury, psoriasis, and small cell lung cancer.
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Pimozide-d5 N-Oxide
0 ImagesCat. No.: HY-12987S1CAS No.: 1794795-40-6Pimozide-d5 N-Oxide is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
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Iloperidone hydrochloride
0 ImagesCat. No.: HY-17410ACAS No.: 1299470-39-5Synonyms: HP 873 hydrochlorideIloperidone hydrochloride (HP 873 hydrochloride) is a D2/5-HT2 receptor antagonist. Iloperidone hydrochloride is an atypical antipsychotic for the schizophrenia symptoms.
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(S)-SKF 38393
0 ImagesCat. No.: HY-12520CCAS No.: 81702-43-4(S)-SKF 38393 is the S-enantiomer of SKF 38393 (HY-12520). (S)-SKF 38393 shows no activity against the D1 dopamine receptor, with an IC50 of 10700 nM. (S)-SKF 38393 can be used in the research of neurological diseases.
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ADX-10061
0 ImagesCat. No.: HY-19100CAS No.: 128022-68-4Synonyms: CEE 03-310; NNC 687ADX-10061 (compound NNC 687) is a dopamine D1 receptor antagonist with the Ki values of 9.1 nM, 5.8 nM, > 10 000 nM and 355 nM for adenylyl cyclase, D1, D2 and 5-HT2 receptor, respectively. ADX-10061 can be used for study of schizophrenia.
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Cinuperone
0 ImagesCat. No.: HY-W754019CAS No.: 82117-51-9Cinuperone is a multi-target competitive receptor ligand and σ receptor antagonist that acts on Dopamine D1, σ, Dopamine D1, and 5-HT2 receptors. Cinuperone shows significantly higher affinity for σ receptors than for Dopamine D1 receptors, and only exhibits moderate binding activity for dopamine D2 receptors. Cinuperone can be used in the research of central nervous system diseases.
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FAUC-312
0 ImagesCat. No.: HY-121740CAS No.: 562104-72-7FAUC-312, a tetrahydropyrimidine, is a strong and highly selective dopamine D4 receptor partial agonist (Ki=1.5 nM).
