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 Inhibitors
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Dopamine Receptor Ligands
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Dopamine Receptor Related Products (541)
Related Products (541)
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Fenoldopam mesylate (Standard)
0 ImagesSynonyms: Fenoldopam methanesulfonate (Standard); SKF-82526 mesylate (Standard)Fenoldopam mesylate (Standard) is the analytical standard of Fenoldopam mesylate (HY-B0735A). This product is intended for research and analytical applications. Fenoldopam (SKF-82526) mesylate is a selective dopamine D1 receptor agonist. Fenoldopam mesylate binds to rat D1B dopamine receptors (Kd = 11 nM) and human D1A receptors (Kd = 17 nM) in COS-7 cell membranes expressing the cloned receptors. Fenoldopam mesylate modulates dopamine receptor expression, induces vasorelaxation in vascular tissues, reverses glomerular hyperfiltration in rat models, increases intracellular cAMP levels, promotes DARPP-32 phosphorylation in small cell lung cancer (SCLC) cells, inhibits cytokine secretion, and downregulates T cell activation markers in activated human T cells. Fenoldopam mesylate can be used for research on hypertension, acute kidney injury, psoriasis, and small cell lung cancer.
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Ziprasidone (Standard)
0 ImagesSynonyms: CP-88059 (Standard)Ziprasidone (Standard) is the analytical standard of Ziprasidone. This product is intended for research and analytical applications. Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).
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Fananserin (Standard)
0 ImagesCat. No.: HY-103104RCAS No.: 127625-29-0Synonyms: RP 62203 (Standard)Fananserin (Standard) is the analytical standard of Fananserin (HY-103104). This product is intended for research and analytical applications. Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor.
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(±) Anabasine (Standard)
0 Images(±) Anabasine (Standard) is the analytical standard of (±) Anabasine (HY-W052144). This product is intended for research and analytical applications. (±) Anabasine is the racemic form of Anabasine (HY-B1532). (±) Anabasine stimulates the release of [3H]-Dopamine from mouse striatal synaptosomes. (±) Anabasine inhibits the high-affinity binding of [3H]-S-(-)-Nicotine to the striatal membrane. Anabasine is an agonist of α7nAChR and possesses anti-inflammatory and insecticidal activities.
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S3608
0 ImagesCat. No.: HY-123440CAS No.: 57359-17-8S3608 is an atypical dopamine agonist. S3608 dose dependently increase locomotor activity (LA) in rats.
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ST-836
0 ImagesCat. No.: HY-15238CAS No.: 1148156-63-1ST-836 is a dopamine receptor ligand; Antiparkinsonian agent.
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Sonepiprazole mesylate
0 ImagesCat. No.: HY-123676CAS No.: 170858-34-1Synonyms: PNU-101387G mesylate; U-101387G mesylateSonepiprazole mesylate is a selective D4 dopamine antagonist with Kis of 3.6, 10.1, 5147, and 7430 nM for rD4-Dopamine, hD4.2-Dopamine, rD2-Dopamine, and Histamine-H1 receptors, respectively.
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A31472
0 ImagesCat. No.: HY-119076CAS No.: 69319-52-4A31472 is a dopamine D-2 receptors antagonist that is promising for research of antipsychotic agents.
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Org-10490
0 ImagesCat. No.: HY-U00077CAS No.: 83507-02-2Org-10490 is an antagonist of dopamine D1 receptor and dopamine D2 receptor, used for the treatment for psychiatric disease.
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Lensiprazine
0 ImagesCat. No.: HY-14793CAS No.: 327026-93-7Lensiprazine is a potent dopamine D2 receptor (D2R) antagonist that acts as a serotonin reuptake inhibitor. Lensiprazine can be used to study bipolar disorder and schizophrenia.
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NMI 8739 (Standard)
0 ImagesCat. No.: HY-101540RCAS No.: 129024-87-9
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Haloperidol decanoate (Standard)
0 ImagesCat. No.: HY-107969RCAS No.: 74050-97-8Haloperidol decanoate (Standard) is the analytical standard of Haloperidol decanoate. This product is intended for research and analytical applications. Haloperidol decanoate is a depot preparation of haloperidol, a commonly used butyrophenone derivative with antipsychotic activity. Haloperidol decanoate can increase the striatal D2 receptor in rat. Haloperidol decanoate can improve conditions of psychoses (mainly schizophrenia). Haloperidol decanoate can lead to increased accumulation of the dopamine metabolites homo-vanillic acid. Haloperidol decanoate can reduce intestinal transport, increase gastric emptying and reduce acid output in rat model.
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Fluphenazine-d6 hydrochloride
0 ImagesCat. No.: HY-119980BSFluphenazine-d6 (hydrochloride) is deuterium labeled Fluphenazine (hydrochloride). Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride 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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Savoxepin mesylate
0 ImagesCat. No.: HY-119385CAS No.: 79262-47-8Savoxepin mesylate is a D2 dopamine receptor (D2 Dopamine Receptor) antagonist with antipsychotic activity. Savoxepin mesylate selectively blocks dopamine D2 receptors in the hippocampus while having no significant effect on D2 receptors in the striatum. This selective blockade helps reduce the risk of extrapyramidal side effects (EPS).
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Olanzapine ketolactam
0 ImagesCat. No.: HY-Z4466CAS No.: 1017241-34-7Olanzapine ketolactam (compound 1) is the impurity of Olanzapine (HY-14541). Olanzapine is a selective, orally active monoaminergic antagonist.
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UNC9994 hydrochloride (Standard)
0 ImagesCat. No.: HY-111385RCAS No.: 2108826-33-9UNC9994 hydrochloride (Standard) is the analytical standard of UNC9994 (hydrochloride) (HY-111385). This product is intended for research and analytical applications. UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.
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Milenperone
0 ImagesCat. No.: HY-121898CAS No.: 59831-64-0Milenperone (R 34009) is a dopamine atagonist. Milenperone can be used in the study for neurological disease.
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Talipexole dihydrochloride (Standard)
0 ImagesSynonyms: B-HT 920 dihydrochloride (Standard)Talipexole (dihydrochloride) (Standard) is the analytical standard of Talipexole (dihydrochloride). This product is intended for research and analytical applications. Talipexole dihydrochloride (B-HT 920 dihydrochloride) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.
