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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7-Hydroxy-DPAT hydrobromide
0 Images7-Hydroxy-DPAT hydrobromide is a selective D3 dopamine receptor agonist, exhibiting significant pharmacological activity in modulating locomotor behavior and dopamine metabolism within the brain.
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Flavoxate
0 ImagesSynonyms: Rec-7-0040 free base; DW61 free baseFlavoxate (Rec-7-0040 free base; DW61 free base) is an orally active L-type Ca2+ channel inhibitor and antispasmodic. Flavoxate inhibits cyclic adenosine monophosphate production by blocking voltage-dependent inward Ba2+ currents, regulating the brainstem micturition center, and stimulating G protein-coupled receptors. Consequently, Flavoxate induces relaxation of bladder smooth muscle and inhibits isovolumetric rhythmic contractions. Flavoxate effectively increases bladder capacity and alleviates symptoms of urgent urination frequency and pollakiuria caused by overactive bladder. Flavoxate can be used in research on overactive bladder and related voiding dysfunctions.
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Mesdopetam hemitartrate
0 ImagesSynonyms: IRL790 hemitartrateMesdopetam (IRL790) hemitartrate is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam hemitartrate is used for the research of motor and psychiatric complications in Parkinson disease.
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Dopamine D2 receptor antagonist-1
0 ImagesDopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity.
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Pirepemat
0 ImagesCat. No.: HY-137447CAS No.: 1227638-29-0Synonyms: IRL752Pirepemat (IRL752) is a corticalpreferring catecholamine- and cognition-promoting agent. Pirepemat (IRL752) is used for the study of Parkinson's disease. IRL752 is a selective enhancer of cortical dopamine, acetylcholine and norepinephrine.
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Mesulergine hydrochloride
0 ImagesSynonyms: CU32-085 hydrochlorideMesulergine (CU32-085) hydrochloride is a potent 5-HT2C antagonist and dopamine (DA) agonist. Mesulergine hydrochloride presentes hyperphagia. Mesulergine hydrochloride has the potential for the research of cognitive processes.
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(R)-Preclamol hydrochloride
0 ImagesSynonyms: (+)-3-PPP hydrochloride(R)-Preclamol hydrochloride ((+)-3-PPP hydrochloride) is the R-enantiomer of Preclamol hydrochloride. (R)-Preclamol hydrochloride is a DA agonist with autoreceptor as well as postsynaptic receptor stimulatory properties.
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AJ-76 hydrochloride
0 ImagesSynonyms: (+)-AJ 76 hydrochloride; (1S,2R)-AJ 76 hydrochlorideAJ-76 hydrochloride ((+)-AJ 76 hydrochloride) is an antagonist of dopamine autoreceptor with pKi values of 6.95, 6.67, 6.37, 6.21 and 6.07 for hD3, hD4, hD2S, hD2L and rD2 receptors, respectively.
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GBR 12783
0 ImagesCat. No.: HY-W008610CAS No.: 67469-57-2GBR 12783 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 can improve memory performance and increase hippocampal acetylcholine release in rats.
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OPC 4392 hydrochloride
0 ImagesOPC 4392 hydrochloride is an agonist for presynaptic dopamine receptor and an antagonist for postsynaptic D2 receptor. OPC 4392 reverses the Reserpine (HY-N0480)-induced dopamine accumulation, inhibits Apomorphine (HY-12723)-induced stereotypic and climbing behaviors in mouse models.
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2'-O-Methylisoliquiritigenin
0 Images2'-O-Methylisoliquiritigenin, isolated from the Arachis species, up-regulates 5-HT, NE, DA and GABA pathways, but does not put a very significant effect on ne NE pathway.
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MFZ 2-13
0 ImagesCat. No.: HY-W722043CAS No.: 146725-34-0Synonyms: O-456MFZ 2-13 (O-456) is an N-demethylated intermediate and N-nor-analogue of MFD 2-12. MFZ 2-13 inhibits dopamine uptake through the human dopamine receptor with an IC50 of 1.4 nM.
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RG-15
0 ImagesCat. No.: HY-171328CAS No.: 1076189-55-3RG-15 is the orally active antagonist for dopamine receptor that exhibits goof affinity to human D2 receptor and human D3 receptor with pKi of 8.23 and 10.49. RG-15 inhibits dopamine-stimulated [35S]GTPγS binding with IC50 of 21.2 nM (rat striatal membranes), 36.7 nM (mouse A9 cells expressing human D2L receptors) and 7.2 nM (CHO cells expressing human D3 receptors). RG-15 increases the turnover and biosynthesis of dopamine in mouse striatum and olfactory bulb, exhibiting antipsychotic activity.
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Nafadotride
0 ImagesNafadotride is a dopamine D3 receptor antagonist. Nafadotrode regulates dopamine signaling primarily by antagonizing dopamine D3 receptors. The dopamine D3 receptor plays an important role in regulating emotion, motivation, reward, and certain motor functions. By blocking these receptors, Nafadotrode may affect neurotransmission processes associated with these functions. Nafadotrode can be used to explore the role of dopamine D3 receptors in various behavioral and neuropsychiatric disorders.
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Pentiapine
0 ImagesSynonyms: CGS 10746Pentiapine (CGS 10746) is a dopamine release inhibitor without binding to synaptic dopamine receptor sites.
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Trifluoperazine dihydrochloride (Standard)
0 ImagesTrifluoperazine (dihydrochloride) (Standard) is the analytical standard of Trifluoperazine (dihydrochloride). This product is intended for research and analytical applications. Trifluoperazine 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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(R)-3-O-Methyldopa-d3
0 ImagesCat. No.: HY-W401531SCAS No.: 1259947-39-1(R)-3-O-Methyldopa-d3 is a deuterium labeled (R)-3-O-Methyldopa, and (R)-3-O-Methyldopa is an R-enantiomer of 3-O-Methyldopa. 3-O-Methyldopa is a metabolite of L-DOPA which is formed by catechol-O-methyltransferase (COMT). 3-O-Methyldopa competitively inhibits the pharmacodynamics of L-DOPA and dopamine.
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(+)-Dihydrexidine hydrochloride
0 ImagesCat. No.: HY-101299CAS No.: 158704-02-0Synonyms: (+)-DAR-0100 hydrochloride(+)-Dihydrexidine hydrochloride ((+)-DAR-0100 hydrochloride) is a dopamine D1 receptor agonist with an EC50 of 72± 21 nM.
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NPEC-caged-dopamine
0 ImagesNPEC-caged-dopamine is a caged version of dopamine. NPEC-caged-Dopamine was used by applying focal photolysis with UV light (360 nm) to releases dopamine, which leads to D1 receptor activation.
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Timiperone
0 ImagesTimiperone has a strong affinity for cerebral dopamine D2 receptor. Timiperone has antipsychotic activity, and inhibits stereotyped behaviour. Timiperone can be used for research of schizophrenia.
