D5 Receptor
D5 receptor (DRD5) is a D1-like dopamine receptor whose cloned human form shows strong homology to D1 and higher dopamine affinity than D1[1]. Mechanistically, D5 supports dopaminergic phospholipase C-phosphoinositide signaling in mammalian brain, because this response is robust in wild-type animals but absent in D5 receptor mutants[2]. In disease models, D5-deficient mice show hypertension with increased sympathetic tone, increased renal sodium transporter expression, and oxidative-stress pathways involving NADPH oxidase and heme oxygenase-1[3][4][5]. Compared with related isoforms, D5 differs from D1 by higher dopamine affinity, high agonist-independent activity, and distinct trafficking properties[1][6][7]. For experimental applications, D1/D5 agonists and D5-selective antagonists help separate D5-linked PLC, calcium, oxidative-stress, and blood-pressure mechanisms from broader D1-like receptor signaling[2][8].
References:
- [1]. Sunahara RK, et al. Cloning of the gene for a human dopamine D5 receptor with higher affinity for dopamine than D1. Nature. 1991 Apr 18;350(6319):614-9. [Content Brief]
- [2]. Sahu A, et al. D5 dopamine receptors are required for dopaminergic activation of phospholipase C. Mol Pharmacol. 2009 Mar;75(3):447-53. [Content Brief]
- [3]. Hollon TR, et al. Mice lacking D5 dopamine receptors have increased sympathetic tone and are hypertensive. J Neurosci. 2002 Dec 15;22(24):10801-10. [Content Brief]
- [4]. Wang X, et al. Upregulation of renal sodium transporters in D5 dopamine receptor-deficient mice. Hypertension. 2010 Jun;55(6):1431-7. [Content Brief]
- [5]. Lu Q, et al. D5 dopamine receptor decreases NADPH oxidase, reactive oxygen species and blood pressure via heme oxygenase-1. Hypertens Res. 2013 Aug;36(8):684-90. [Content Brief]
- [6]. Tiberi M, et al. High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype. J Biol Chem. 1994;269:27925-27931.
- [7]. Thompson D, et al. Trafficking properties of the D5 dopamine receptor. Traffic. 2011 May;12(5):644-56. [Content Brief]
- [8]. Mohr P, et al. Dopamine/serotonin receptor ligands. 12(1): SAR studies on hexahydro-dibenz[d,g]azecines lead to 4-chloro-7-methyl-5,6,7,8,9,14-hexahydrodibenz[d,g]azecin-3-ol, the first picomolar D5-selective dopamine-receptor antagonist. J Med Chem. 2006 Mar 23;49(6):2110-6. [Content Brief]
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D5 Receptor Related Products (28)
Related Products (28)
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(-)-Isocorypalmine
0 ImagesSynonyms: Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine(-)-Isocorypalmine (Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine) is a dopamine receptor ligand and modulator capable of crossing the blood-brain barrier. (-)-Isocorypalmine exhibits receptor selectivity, acting as a partial agonist of dopamine D1 and D5 receptors (coupled via Gs proteins), as well as an antagonist of D2, D3 and D4 receptors (by blocking Gi protein-mediated signaling). (-)-Isocorypalmine shows no significant binding to various non-dopamine receptors, ion channels and transporters. (-)-Isocorypalmine is metabolically stable in vivo, effectively inhibits spontaneous and cocaine-induced hyperlocomotion, sensitization and conditioned place preference in mice, and does not induce addictive place preference when administered alone. (-)-Isocorypalmine can be used in addiction research.
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(Rac)-Rotigotine hydrochloride
0 ImagesSynonyms: N-0437 hydrochloride(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
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D1/D5 Receptor agonist-1
0 ImagesCat. No.: HY-175001D1/D5 Receptor agonist-1 is a highly brain-penetrant and orally active D1/D5 receptor agonist. D1/D5 Receptor agonist-1 maintains considerable efficacy in the cAMP pathway and in β-arrestin recruitment, with EC50s of 3.7 nM (D1R cAMP), 91 nM (D1R β-arrestin), 129 nM (D1R internalization) and a Ki of 111 nM (D1R binding affinity). D1/D5 Receptor agonist-1 inhibits β-arrestin signaling in a rat with L-DOPA (HY-N0304) induced dyskinesias. D1/D5 Receptor agonist-1 can be used for the study of Parkinson’s disease.
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SCH-23390 maleate
0 ImagesCat. No.: HY-108400CAS No.: 87134-87-0Synonyms: R-(+)-SCH-23390 maleateSCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
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Molindone hydrochloride (Standard)
0 ImagesSynonyms: EN-1733A (Standard)Molindone hydrochloride (Standard) is the analytical standard of Molindone hydrochloride (HY-B1017). This product is intended for research and analytical applications. Molindone hydrochloride (EN-1733A) is an orally active and brain-penetrant dopamine D2/D5 receptor antagonist. Molindone hydrochloride shows antipsychotic and antidepressant-like activities. Molindone hydrochloride suppresses spontaneous locomotion, and antagonizes apomorphine-induced emesis. Molindone hydrochloride can be used for the research of neurological disease.
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SKF-83566 (Standard)
0 ImagesCat. No.: HY-103430ARCAS No.: 99295-33-7SKF-83566 (Standard) is the analytical standard of SKF-83566 (HY-103430A). This product is intended for research and analytical applications. SKF-83566 is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM. SKF-83566 modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway. SKF-83566 acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2). SKF-83566 competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation. SKF-83566 is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect").
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ABT-724
0 ImagesABT-724, a chemical probe, is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile.
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Iloperidone hydrochloride
0 ImagesCat. No.: HY-17410ACAS No.: 1299470-39-5Synonyms: HP 873 hydrochlorideIloperidone hydrochloride (HP 873 hydrochloride) is a D2/5-HT2 receptor antagonist. Iloperidone hydrochloride is an atypical antipsychotic for the schizophrenia symptoms.
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