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]
All Product Categories
-
D1 Receptor Inhibitors
(7)
View all products
-
D1 Receptor Agonists
(38)
View all products
-
D1 Receptor Antagonists
(43)
View all products
-
D1 Receptor Activators
(3)
View all products
-
D1 Receptor Modulators
(4)
View all products
-
D1 Receptor Control
(1)
View all products
-
D1 Receptor Ligands
(3)
View all products
-
D1 Receptor Related Products (105)
Related Products (105)
-
PF-06256142
0 ImagesPF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson's disease.
-
Perospirone hydrochloride
0 ImagesSynonyms: SM-9018Perospirone hydrochloride (SM-9018) is an orally active antagonist of 5-HT2A receptor (Ki of 0.6 nM) and dopamine D2 receptor (Ki of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT1A receptor (Ki of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
-
(Rac)-PF-06256142
0 Images(Rac)-PF-06256142 is the less effective enantiomer of PF-06256142 (HY-119943). (Rac)-PF-06256142 is an agonist of D1 receptor, with an EC50 of 107 nM. (Rac)-PF-06256142 can be used for the research of schizophrenia and Parkinson's disease.
-
SKF 83959 hydrobromide
0 ImagesSKF83959 hydrobromide is a potent and selective dopamine D1-like receptor partial agonist. SKF83959 hydrobromide Ki values for rat D1, D5, D2 and D3 receptors are 1.18, 7.56, 920 and 399 nM, respectively. SKF83959 hydrobromide is a potent allosteric modulator of sigma (σ)-1 receptor. SKF83959 hydrobromide belongs to benzazepine family and has improvements on cognitive dysfunction. SKF83959 hydrobromide can be used for the research of Alzheimer's disease and depression.
-
Ecopipam hydrobromide
0 ImagesSynonyms: SCH 39166 hydrobromideEcopipam (SCH 39166) hydrobromide 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 hydrobromide 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 hydrobromide can be used for the research of schizophrenia and obesity.
-
MLS6357
0 ImagesMLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder.
-
Iloperidone carboxylic acid
0 ImagesSynonyms: P95-12113Iloperidone carboxylic acid (P95-12113) is the metabolite of Iloperidone (HY-17410). Iloperidone carboxylic acid exhibits good affinity for 5-HT2A receptor with pKi of 8.15, and moderate affinity for adrenergic receptor α1/α2B/α2C.
-
RB 101
0 ImagesCat. No.: HY-117702CAS No.: 135949-60-9RB 101 is a blood-brain barrier-crossing prodrug as well as aminopeptidase N and neutral endopeptidase-24.11 inhibitor. RB 101 blocks enkephalin breakdown, elevates extracellular enkephalin levels and activate δ-opioid receptor and dopamine D1 receptor. RB 101 can be used for the research of pain, depressive syndromes, and diabetic neuropathy.
-
DETQ
0 ImagesCat. No.: HY-115553CAS No.: 1638667-81-8DETQ is a selective, allosteric and orally active dopamine D1 receptor (Dopamine Receptor) potentiator. In HEK293 cells expressing the human D1 receptor, DETQ increases cAMP with an EC50 of 5.8 nM and a Kb of 26 nM. DETQ shows ~30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor.
-
Razpipadon
0 ImagesSynonyms: (-)-PW0464Razpipadon ((-)-PW0464) is an isomer of (Rac)-Razpipadon (HY-141495).
-
MLS1082
0 ImagesMLS1082 is a pyrimidone-based D1-like dopamine receptor positive allosteric modulator, with an EC50 of 123 nM for DA-stimulated G protein signaling.
-
D3/5-HT receptor modulator-1
0 ImagesD3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and 5-HT2A receptor antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile.
-
SKF-75670 hydrobromide
0 ImagesSKF-75670 hydrochloride is a Dopamine D1 receptor partial agonist. SKF-75670 hydrochloride is also a Cocaine antagonist.
-
(-)-Isocorypalmine
0 ImagesSynonyms: Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine(-)-Isocorypalmine (Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine) is a dopamine receptor ligand and modulator capable of crossing the blood-brain barrier. (-)-Isocorypalmine exhibits receptor selectivity, acting as a partial agonist of dopamine D1 and D5 receptors (coupled via Gs proteins), as well as an antagonist of D2, D3 and D4 receptors (by blocking Gi protein-mediated signaling). (-)-Isocorypalmine shows no significant binding to various non-dopamine receptors, ion channels and transporters. (-)-Isocorypalmine is metabolically stable in vivo, effectively inhibits spontaneous and cocaine-induced hyperlocomotion, sensitization and conditioned place preference in mice, and does not induce addictive place preference when administered alone. (-)-Isocorypalmine can be used in addiction research.
-
Spiramide
0 ImagesSpiramide (AMI-193) is a potent and selective antagonist of 5-HT2 and dopamine D2 receptor, with Kis of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT2 versus 5-HT1C (Ki=4300 nM) receptors. Spiramide exhibits antipsychotic activity.
-
(Rac)-Rotigotine hydrochloride
0 ImagesSynonyms: N-0437 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.
-
Blonanserin dihydrochloride
0 ImagesCat. No.: HY-13575ACAS No.: 132812-45-4Synonyms: AD-5423 dihydrochlorideBlonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.
-
D1/D5 Receptor agonist-1
0 ImagesCat. No.: HY-175001D1/D5 Receptor agonist-1 is a highly brain-penetrant and orally active D1/D5 receptor agonist. D1/D5 Receptor agonist-1 maintains considerable efficacy in the cAMP pathway and in β-arrestin recruitment, with EC50s of 3.7 nM (D1R cAMP), 91 nM (D1R β-arrestin), 129 nM (D1R internalization) and a Ki of 111 nM (D1R binding affinity). D1/D5 Receptor agonist-1 inhibits β-arrestin signaling in a rat with L-DOPA (HY-N0304) induced dyskinesias. D1/D5 Receptor agonist-1 can be used for the study of Parkinson’s disease.
-
Docarpamine
0 ImagesCat. No.: HY-W752502CAS No.: 74639-40-0Docarpamine is an orally active dopamine prodrug that can be hydroxylated in the small intestine and liver to form active dopamine. Docarpamine mainly activates D1-like receptors in peripheral blood vessels to lower blood pressure and heart rate in a state of spontaneous hypertension. Docarpamine exerts a pressor and tachycardic effect by activating D1-like receptors, vasopressin V1 receptors, and α-adrenergic receptors in normal blood pressure conditions. Docarpamine can be used for research on renal vascular dilation and diuresis.
-
A68930
0 ImagesCat. No.: HY-120687CAS No.: 130465-45-1A68930, as a dopamine D1 receptor agonist, can be used for the research of bronchiectasis.
