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 Ligands
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Dopamine Receptor Related Products (537)
Related Products (537)
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Preclamol hydrochloride (Standard)
0 ImagesCat. No.: HY-108698RCAS No.: 88768-67-6Synonyms: (-)-3-PPP hydrochloride (Standard)Preclamol hydrochloride (Standard) is the analytical standard of Preclamol (hydrochloride) (HY-108698). This product is intended for research and analytical applications. Preclamol hydrochloride ((-)-3-PPP hydrochloride) is a selective dopamine autoreceptor agonist. Preclamol hydrochloride has the potential for the research of schizophrenia.
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Brl 20596
0 ImagesCat. No.: HY-121008CAS No.: 69082-47-9Brl 20596 (compound 4a) is a potent central dopamine receptor antagonist and can be used in antipsychotic research.
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7-Hydroxy ropinirole bromide
0 ImagesCat. No.: HY-167636CAS No.: 81654-57-1Synonyms: SK&F 89124 bromide7-Hydroxy ropinirole (SK&F 89124) bromide is a potent and highly selective DA2 receptor agonist, and a derivative of N,N-di-n-propyldopamine (DPDA). In isolated perfused rabbit ear artery models, 7-Hydroxy ropinirole (bromide) exerts its DA2 agonist effects by inhibiting neurotransmitter release or sympathetic nerve-induced responses. It shows potential for research in the fields of cardiovascular and neurological diseases.
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TAT-D1 peptide
0 ImagesCat. No.: HY-P10405TAT-D1 peptide is a dopamine D1-D2 receptor heterodimer inhibitor. TAT-D1 peptide disrupts the function of dopamine D1-D2 receptor heteromers, enhances subchronic amphetamine-induced locomotor activity, and exacerbates the expression of amphetamine-induced locomotor sensitization. TAT-D1 peptide produces rapid anxiolytic and antidepressant-like effects in rat models of depression and anxiety, and inhibits c-fos expression in the nucleus accumbens of rats. TAT-D1 peptide can be used in the research of psychostimulant addiction, depression and anxiety disorders.
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Chlorpromazine (Standard)
0 ImagesChlorpromazine (Standard) is the analytical standard of Chlorpromazine (HY-12708). This product is intended for research and analytical applications. Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis.
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Teniloxazine free base
0 ImagesCat. No.: HY-164009CAS No.: 62473-79-4Synonyms: Sufoxazinefree base; Y-8894free baseTeniloxazine free base is an inhibitor for norepinephrine neuronal reuptake and an weak inhibitor for reuptake of Serotonin (HY-B1473A) and Dopamine (HY-B0451). Teniloxazine free base exhibits antidepressant, antihypoxic and anti-amnestic properties without anticholinergic, sedative, and cardiovascular adverse effects.
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GBR-13119
0 ImagesCat. No.: HY-183665CAS No.: 76778-24-0GBR-13119 is a blood-brain barrier-permeable inhibitor of the presynaptic dopamine uptake system. GBR-13119 binds to dopamine uptake sites with high selectivity, without being affected by other neurotransmitter reuptake inhibitors. GBR-13119 exhibits a lipophilic systemic distribution profile with extremely low defluorination in rats, while it shows a differential characteristic of slow striatal washout in the brain of primates. GBR-13119 can serve as a PET tracer to achieve visualized imaging of the striatum in primates, and can reflect MPTP-induced dopaminergic neuron degeneration through reduced uptake. GBR-13119 can be widely applied to studies related to Parkinson's disease and dopaminergic neuron degeneration.
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Aramisulpride (Standard)
0 ImagesCat. No.: HY-109167RCAS No.: 71675-90-6Synonyms: (R)-Amisulpride (Standard); (R)-Esamisulpride (Standard); (R)-DAN 2163 (Standard)Aramisulpride (Standard) is the analytical standard of Aramisulpride (HY-109167). This product is intended for research and analytical applications. Aramisulpride (R-(+)-Amisulpride) is the R-isomer of Amisulpride (HY-14545). Aramisulpride is a 5-HT7 receptor antagonist with a Ki value of 22 nM. Aramisulpride is a D2/D3 receptor antagonist with a Ki value of 140 nM for D2R and a Ki value of 13.9 nM for D3R. Aramisulpride can be used in psychiatric research.
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PD-147693
0 ImagesCat. No.: HY-169837CAS No.: 163239-24-5PD-147693 (compound II) is an active metabolite of the presynaptic dopamine autoreceptor agonist CI-1007 and has antipsychotic activity similar to CI-1007.
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SKF-82958 hydrobromide (Standard)
0 ImagesSynonyms: (±)-SKF-82958 hydrobromide (Standard); Chloro-APB hydrobromide (Standard)SKF-82958 (hydrobromide) (Standard) is the analytical standard of SKF-82958 (hydrobromide). This product is intended for research and analytical applications. SKF-82958 ((±)-SKF 82958) hydrobromide is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 hydrobromide induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM).
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Pramipexole (Standard)
0 ImagesPramipexole (Standard) is the analytical standard of Pramipexole. This product is intended for research and analytical applications. Pramipexole is a selective and blood-brain barrier (BBB) penetrant dopamine D2-type receptor agonist, with Kis of 2.2 nM, 3.9 nM, 0.5 nM and 1.3 nM for D2-type receptor, D2, D3 and D4 receptors, respectively. Pramipexole can be used for the research of Parkinson's disease (PD) and restless legs syndrome (RLS).
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(Rac)-GR218231
0 ImagesCat. No.: HY-123757CAS No.: 175442-95-2(Rac)-GR218231 is a selective dopamine D3 receptor antagonist with a pKi of 8.9.
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Cinitapride-d5
0 ImagesCat. No.: HY-B2089SCAS No.: 2714421-62-0Cinitapride-d5 is the deuterium labeled Cinitapride.
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SB-277011 hydrochloride (Standard)
0 ImagesCat. No.: HY-10847BRCAS No.: 215804-67-4Synonyms: SB-277011A hydrochloride (Standard)SB-277011 hydrochloride (Standard) is the analytical standard of SB-277011 (hydrochloride) (HY-10847B). This product is intended for research and analytical applications. SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
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A 23887
0 ImagesCat. No.: HY-119183CAS No.: 61955-05-3A 23887 is a semirigid antipsychotic compound with considerable affinity for dopamine D2 receptor.
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Promazine-d6 hydrochloride
0 ImagesCat. No.: HY-B1225SCAS No.: 1246819-33-9Synonyms: Romtiazin-d6 hydrochloride; Ampazine-d6 hydrochloridePromazine-d6 (hydrochloride) (Romtiazin-d6 (hydrochloride)) is deuterium labeled Promazine (hydrochloride). Promazine (Romtiazin) hydrochloride is an antipsychotic and a dopamine receptor D2 antagonist. Promazine hydrochloride inhibits dopaminergic neurotransmission.
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Nomifensine maleate (Standard)
0 ImagesCat. No.: HY-B1110ARCAS No.: 32795-47-4Synonyms: (±)-Nomifensine maleate (Standard); Nomifensin maleate (Standard)Nomifensine (maleate) (Standard) is the analytical standard of Nomifensine (maleate). This product is intended for research and analytical applications. Nomifensine ((±)-Nomifensine) maleate is a potent norepinephrine (NE) and dopamine (DA) reuptake inhibitor. Nomifensine maleate inhibits uptake of NE, DA and 5-HT in rat brain synaptosomes, with IC50 values of 6.6 nM, 48 nM and 830 nM, and Ki values of 4.7 nM, 26 nM and 4000 nM, respectively. Nomifensine maleate has antidepressant and analgesic effects. Nomifensine maleate is used in neurodegenerative diseases, compound addiction, and pain research.
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Ralmitaront (Standard)
0 ImagesCat. No.: HY-109157RCAS No.: 2133417-13-5Synonyms: RO6889450 (Standard)Ralmitaront (Standard) is the analytical standard of Ralmitaront (HY-109157). This product is intended for research and analytical applications. Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC50 value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder.
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Halopemide (Standard)
0 ImagesHalopemide (Standard) is the analytical standard of Halopemide. This product is intended for research and analytical applications. Halopemide 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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Ocaperidone (Standard)
0 ImagesCat. No.: HY-101094RCAS No.: 129029-23-8Synonyms: R79598 (Standard)Ocaperidone (Standard) is the analytical standard of Ocaperidone (HY-101094). This product is intended for research and analytical applications. Ocaperidone is an effective antipsychotic agent, acting as a potent 5-HT2 and dopamine D2 antagonist, and a 5-HT1A agonist, with Kis of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT2, a1-adrenergic receptor, dopamine D2, histamine H1 and a2-adrenergic receptor, respectively, and a pEC50 and pKi of 7.60 and 8.08 for h5-HT1A.
