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 (537)
Related Products (537)
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Amitifadine
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L-745870 hydrochloride (Standard)
0 ImagesCat. No.: HY-14325BRCAS No.: 1173023-36-3L-745870 (hydrochloride) (Standard) is the analytical standard of L-745870 (hydrochloride). This product is intended for research and analytical applications. L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
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A68930 hydrochloride (Standard)
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Thozalinone (Standard)
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Tetrabenazine (Standard)
0 ImagesTetrabenazine (Standard) is the analytical standard of Tetrabenazine (HY-B0590). This product is intended for research and analytical applications. Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome.
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9-Fluorenol (Standard)
0 ImagesSynonyms: 9-Hydroxyfluorene (Standard)9-Fluorenol (Standard) is the analytical standard of 9-Fluorenol. This product is intended for research and analytical applications. 9-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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(R)-Preclamol hydrochloride (Standard)
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7-Hydroxychlorpromazine hydrochloride
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Itopride hydrochloride (Standard)
0 ImagesSynonyms: HSR803 (Standard)Itopride (hydrochloride) (Standard) is the analytical standard of Itopride (hydrochloride). This product is intended for research and analytical applications. Itopride (HSR803) hydrochloride is a potent dopamine-2 antagonist and an acetylcholine esterase (AChE) inhibitor. Itopride hydrochloride enhances gastric motility through both antidopaminergic and anti-acetylcholinesterasic actions, can be used as a gastrointestinal prokinetic agent. Itopride can be used for researching gastro-esophageal reflux disease (GERD).
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PD 118440
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Piribedil (Standard)
0 ImagesPiribedil (Standard) is the analytical standard of Piribedil. This product is intended for research and analytical applications. Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers.
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Iloperidone-13C,d3
0 ImagesCat. No.: HY-17410S2Synonyms: HP 873-13C,d3Iloperidone-13C,d3 (HP 873-13C,d3) is 13C labeled Iloperidone. Iloperidone (HP 873) is a D2/5-HT2 receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms.
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Metergoline (Standard)
0 ImagesMetergoline (Standard) is the analytical standard of Metergoline. This product is intended for research and analytical applications. Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na+ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation.
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Fluphenazine decanoate (Standard)
0 ImagesFluphenazine decanoate (Standard) is the analytical standard of Fluphenazine decanoate. This product is intended for research and analytical applications. Fluphenazine decanoate is a dopamine D2 receptor inhibitor, is a long-acting phenothiazine neuroleptic. Fluphenazine can be used for schizophrenia research.
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Bacopaside X (Standard)
0 ImagesCat. No.: HY-N5140RCAS No.: 94443-88-6Synonyms: Bacopaside VII (Standard)Bacopaside X (Standard) is the analytical standard of Bacopaside X. This product is intended for research and analytical applications. Bacopaside X is found in Bacopa monnieri, and shows a binding affinity toward the D1 receptor.
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(Rac)-Preclamol
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Lergotrile mesylate
0 ImagesCat. No.: HY-107002ACAS No.: 51473-23-5Lergotrile mesylate is a potent and orally active dopamine agonist and a prolactin secretion inhibitor. Lergotrile mesylate inhibits prolactin release from pituitaries by activating an adenohypophyseal dopamine receptor. Lergotrile mesylate has the potential for the research of Parkinson's disease.
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Disulergine
0 ImagesCat. No.: HY-119997CAS No.: 59032-40-5Synonyms: CH 29-717Disulergine (CH 29-717) is an ergot alkaloid. Disulergine is a dopamine receptor agonist. Disulergine inhibits secretion of prolactin in rats. Disulergine inhibits growth hormone (GH) release.
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Pridopidine (Standard)
0 ImagesSynonyms: ACR16 (Standard); ASP2314 (Standard); FR310826 (Standard)Pridopidine (Standard) is the analytical standard of Pridopidine. This product is intended for research and analytical applications. Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. Pridopidine exerts high affinity towards sigma 1 receptor (S1R) with Ki between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.
