Dopamine Receptor
Dopamine receptors are GPCRs through which dopamine regulates motor function, motivation, drive, cognition, and peripheral physiology[1][2]. Mechanistically, dopamine receptor signaling is organized into D1-like receptors (D1, D5) and D2-like receptors (D2S, D2L, D3, D4), enabling subtype-specific control of cAMP-mediated and non-canonical signaling[1][3]. In disease-oriented research, dopamine-glutamate-NMDA interactions and dopamine receptor ligands provide experimental frameworks for schizophrenia, Parkinson’s disease, depression, bipolar disorder, and addiction models[1][3]. Compared with related isoforms, D1-D2 receptor heteromers form a pharmacologically distinct signaling complex coupled to Gq/11, requiring agonist binding to both receptors for G protein activation and intracellular calcium release[4]. This calcium pathway links D1-D2 receptor heteromer activation to CaMKIIα, BDNF production, and neuronal growth in striatal models[5]. Compared with D1, D5 shows high agonist affinity and constitutive activity shaped by carboxyl-terminal tail sequence and intracellular loop determinants[6][7]. Therefore, subtype-selective agonists, antagonists, partial agonists, and heteromer-directed ligands remain practical tools for dissecting dopamine receptor pharmacology, signaling bias, and disease-relevant neurocircuit mechanisms[1][3][4].
References:
- [1]. Martel JC, et al. Dopamine Receptor Subtypes, Physiology and Pharmacology: New Ligands and Concepts in Schizophrenia. Front Pharmacol. 2020 Jul 14;11:1003. [Content Brief]
- [2]. Beaulieu JM, et al. The physiology, signaling, and pharmacology of dopamine receptors. Pharmacol Rev. 2011 Mar;63(1):182-217. [Content Brief]
- [3]. Beaulieu JM, et al. Dopamine receptors - IUPHAR Review 13. Br J Pharmacol. 2015 Jan;172(1):1-23. [Content Brief]
- [4]. Rashid AJ, et al. D1-D2 dopamine receptor heterooligomers with unique pharmacology are coupled to rapid activation of Gq/11 in the striatum. Proc Natl Acad Sci U S A. 2007 Jan 9;104(2):654-9. [Content Brief]
- [5]. Hasbi A, et al. Calcium signaling cascade links dopamine D1-D2 receptor heteromer to striatal BDNF production and neuronal growth. Proc Natl Acad Sci U S A. 2009 Dec 15;106(50):21377-82. [Content Brief]
- [6]. Demchyshyn LL, et al. Dopamine D5 receptor agonist high affinity and constitutive activity profile conferred by carboxyl-terminal tail sequence. J Biol Chem. 2000 Aug 4;275(31):23446-55. [Content Brief]
- [7]. Tumova K, et al. Role of the fourth intracellular loop of D1-like dopaminergic receptors in conferring subtype-specific signaling properties. FEBS Lett. 2004 Oct 22;576(3):461-7. [Content Brief]
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Dopamine Receptor Related Products (533)
Related Products (533)
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Olanzapine
0 ImagesSynonyms: LY170053Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
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Quinpirole hydrochloride
0 ImagesSynonyms: LY 171555 hydrochloride; (-)-LY 141865 hydrochlorideQuinpirole hydrochloride (LY 171555 hydrochloride) is a high-affinity agonist of dopamine D2/D3 receptor.
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Ansofaxine hydrochloride
0 ImagesSynonyms: LY03005; LPM570065Ansofaxine hydrochloride (LY03005; LPM570065) is a triple reuptake inhibitor; inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively.
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Asimilobine
0 ImagesAsimilobine is an aporphine isoquinoline alkaloid isolated from plant species of Magnolia obobata Thun. Asimilobine is a dopamine biosynthesis inhibitor and a serotonergic receptor antagonist. Asimilobine shows an antimalarial and anti-cancer activity.
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Trifluoperazine dihydrochloride
0 ImagesTrifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.
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Fluphenazine dihydrochloride
0 ImagesFluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2.
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Trifluoperazine
0 ImagesTrifluoperazine, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine is a potent α1-adrenergic receptor antagonist. Trifluoperazine is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine can be used for the research of schizophrenia. Trifluoperazine acts as a reversible inhibitor of influenza virus morphogenesis.
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L-DOPA (Standard)
0 ImagesSynonyms: Levodopa (Standard); 3,4-Dihydroxyphenylalanine (Standard)L-DOPA (Standard) is the analytical standard of L-DOPA. This product is intended for research and analytical applications. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease.
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Levomepromazine
0 ImagesLevomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca2+ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting.
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Quinagolide hydrochloride
0 ImagesSynonyms: CV205-502 hydrochlorideQuinagolide hydrochloride (CV205-502 hydrochloride) is a selective and orally active dopamine D2 receptor agonist. Quinagolide hydrochloride is an inhibitor of prolactin. Quinagolide hydrochloride down-regulates AKT levels and its phosphorylation. Quinagolide hydrochloride shows antitumor effects, it can be used for the research of cancer.
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Dopamine hydrochloride (Standard)
0 ImagesSynonyms: ASL279 (Standard)Dopamine (hydrochloride) (Standard) is the analytical standard of Dopamine (hydrochloride). This product is intended for research and analytical applications. Dopamine hydrochloride (ASL279) is a catecholamine neurotransmitter that is produced in the substantia nigra, ventral tegmental area, and hypothalamus of the brain. Dopamine hydrochloride (ASL279) plays several important roles in the brain and body. Dopamine hydrochloride (ASL279) acts through D2 dopamine receptors to induce endocytosis of VEGFR2, which is critical for promoting angiogenesis.
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Tavapadon
0 ImagesSynonyms: PF-06649751; CVL-751Tavapadon (PF-06649751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist. Tavapadon is effective in enabling movement and reducing disability and has the potential for Parkinson's disease.
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Thioridazine
0 ImagesThioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
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Piperacetazine
0 ImagesPiperacetazine is an orally active dopamine receptor antagonist and phenothiazine antipsychotic. Piperacetazine can directly bind to the PAX3::FOXO1 fusion protein and inhibit its transcriptional activity. Piperacetazine also exhibits antitumor activity with an IC50 of 7.627 μM against PANC-1 cells. Piperacetazine can be used for the research of diseases such as schizophrenia and pancreatic cancer and other tumors.
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BRL-44408 maleate
0 ImagesBRL-44408 maleate is a selective, blood-brain barrier-permeable α2A-adrenergic receptor antagonist with a Ki value of 8.56 nM against human targets. BRL-44408 maleate exhibits activities such as antidepressant, analgesic effects and attenuation of sepsis-induced acute lung injury by regulating the release of neurotransmitters such as norepinephrine and dopamine, or inhibiting signaling pathways including ERK1/2, p38MAPK and p65. BRL-44408 maleate can be used in studies related to acute respiratory distress syndrome, depression and visceral pain.
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Dopamine-d3 hydrochloride
0 ImagesSynonyms: ASL279-d3Dopamine-d3 (hydrochloride) is the deuterium labeled Dopamine hydrochloride (ASL279)-.
