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 (538)
Related Products (538)
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Alizapride hydrochloride
0 ImagesAlizapride is a potent antiemetic, acting as a dopamine receptor antagonist. Alizapride also used in human digestive disorders.
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9-Fluorenol
0 ImagesSynonyms: 9-Hydroxyfluorene9-Fluorenol (9-Hydroxyfluorene; compound 3) is a dopamine (DAT) inhibitor with IC50 value of 9 µM. 9-Fluorenol is a major metabolite of compound developed as a wake promoting agent. 9-Fluorenol shows wake promotion activity in vivo.
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Ralmitaront
0 ImagesSynonyms: RO6889450Ralmitaront (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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Clozapine-d4
0 ImagesSynonyms: HF 1854-d4Clozapine-d4 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors.
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Clebopride malate
0 ImagesClebopride malate is an orally active dopamine Receptor antagonist. Clebopride malate acts on dopamine D2 receptors and has antiemetic and prokinetic effects. Clebopride malate can be used in the study of functional gastrointestinal disorders.
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Aripiprazole Lauroxil
0 ImagesAripiprazole lauroxil, an N-acyloxymethyl proagent of Aripiprazole (HY-14546), is a Long-acting injectable (LAI) typical antipsychotic for schizophrenia and a ligand of dopamine receptor D2R/D4R. Aripiprazole lauroxil is cleaved by body’s enzyme esterase to N-hydroxymethyl aripiprazole (plus lauric acid) and then to aripiprazole (plus formaldehyde), no toxicity.
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L-DOPA-13C
0 ImagesL-DOPA-13C is the 13C labeled L-DOPA. 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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L-DOPA-d6
0 ImagesSynonyms: Levodopa-d6; 3,4-Dihydroxyphenylalanine-d6L-DOPA-d6 is the deuterium labeled L-DOPA. 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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Clopenthixol
0 ImagesClopenthixol is a thiaquinoline compound with inhibitory effects similar to those of phenothiazine antipsychotics. Clopenthixol is an antagonist of D1 and D2 dopamine receptors. Clopenthixol is mainly used to suppress schizophrenia and other mental disorders.
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GBR 12783 dihydrochloride
0 ImagesGBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats.
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MIF-1 TFA
0 ImagesSynonyms: Pro-Leu-Gly-NH2 TFA; Melanostatin TFAMIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).
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SKF 77434 hydrobromide
0 ImagesSKF 77434 hydrobromide is a selective dopamine D1 receptor partial agonist. SKF 77434 hydrobromide has the potential to study cocaine addiction.
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SB269652
0 ImagesSB269652 is the first drug-like allosteric modulator of the dopamine D2 receptor (D2R); a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
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Lenperone
0 ImagesSynonyms: AHR 2277 free baseLenperone (AHR 2277 free base) has antipsychotic effect. Lenperone improves depressive symptoms.
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Chlorpromazine-d6 hydrochloride
0 ImagesChlorpromazine-d6 (hydrochloride) is the deuterium labeled Chlorpromazine. Chlorpromazine is an inhibitor of dopamine receptor, 5-HT receptor, potassium channel, sodium channel.
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L-DOPA-13C6
0 ImagesSynonyms: Levodopa-13C6; 3,4-Dihydroxyphenylalanine-13C6L-DOPA-13C6 is the 13C-labled L-DOPA. 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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Domperidone monomaleate
0 ImagesSynonyms: R33812 monomaleateDomperidone (R33812) monomaleate is an orally active and selective dopamine-2 receptor antagonist. Domperidone monomaleate acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine.
