Dopamine receptor D2 |
Rendering based on PDB 1I15.
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Available structures |
PDB |
Ortholog search: PDBe, RCSB |
List of PDB id codes |
1I15, 5AER
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Identifiers |
Symbols |
DRD2 ; D2DR; D2R |
External IDs |
OMIM: 126450 MGI: 94924 HomoloGene: 22561 IUPHAR: 215 ChEMBL: 217 GeneCards: DRD2 Gene |
Gene ontology |
Molecular function |
• dopamine neurotransmitter receptor activity, coupled via Gi/Go
• adrenergic receptor activity
• protein binding
• drug binding
• potassium channel regulator activity
• dopamine binding
• ionotropic glutamate receptor binding
• identical protein binding
• protein homodimerization activity
• protein heterodimerization activity
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Cellular component |
• acrosomal vesicle
• intracellular
• cytosol
• plasma membrane
• integral component of plasma membrane
• postsynaptic density
• lateral plasma membrane
• endocytic vesicle
• axon
• dendrite
• synaptic vesicle membrane
• nonmotile primary cilium
• sperm flagellum
• dendritic spine
• perikaryon
• axon terminus
• ciliary membrane
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Biological process |
• temperature homeostasis
• response to hypoxia
• synaptic transmission, dopaminergic
• response to amphetamine
• neurological system process involved in regulation of systemic arterial blood pressure
• regulation of heart rate
• regulation of sodium ion transport
• G-protein coupled receptor internalization
• positive regulation of neuroblast proliferation
• positive regulation of receptor internalization
• cellular calcium ion homeostasis
• negative regulation of adenylate cyclase activity
• adenylate cyclase-inhibiting dopamine receptor signaling pathway
• neuron-neuron synaptic transmission
• axonogenesis
• synapse assembly
• sensory perception of smell
• long-term memory
• grooming behavior
• locomotory behavior
• adult walking behavior
• feeding behavior
• protein localization
• negative regulation of cell proliferation
• associative learning
• visual learning
• response to light stimulus
• response to toxic substance
• response to iron ion
• regulation of dopamine secretion
• response to inactivity
• Wnt signaling pathway
• striatum development
• orbitofrontal cortex development
• cerebral cortex GABAergic interneuron migration
• adenohypophysis development
• negative regulation of cell migration
• peristalsis
• regulation of cAMP metabolic process
• auditory behavior
• activation of protein kinase activity
• regulation of synaptic transmission, GABAergic
• positive regulation of cytokinesis
• circadian regulation of gene expression
• negative regulation of dopamine secretion
• response to histamine
• response to nicotine
• intracellular signal transduction
• positive regulation of urine volume
• positive regulation of renal sodium excretion
• positive regulation of multicellular organism growth
• response to cocaine
• negative regulation of circadian sleep/wake cycle, sleep
• dopamine metabolic process
• response to drug
• regulation of potassium ion transport
• response to morphine
• pigmentation
• regulation of phosphoprotein phosphatase activity
• positive regulation of G-protein coupled receptor protein signaling pathway
• negative regulation of blood pressure
• negative regulation of innate immune response
• positive regulation of transcription from RNA polymerase II promoter
• phosphatidylinositol metabolic process
• negative regulation of insulin secretion
• behavioral response to cocaine
• behavioral response to ethanol
• regulation of long-term neuronal synaptic plasticity
• response to axon injury
• branching morphogenesis of a nerve
• arachidonic acid secretion
• negative regulation of protein secretion
• release of sequestered calcium ion into cytosol
• negative regulation of cytosolic calcium ion concentration
• positive regulation of cytosolic calcium ion concentration involved in phospholipase C-activating G-protein coupled signaling pathway
• regulation of dopamine uptake involved in synaptic transmission
• positive regulation of dopamine uptake involved in synaptic transmission
• regulation of synapse structural plasticity
• negative regulation of protein kinase B signaling
• negative regulation of synaptic transmission, glutamatergic
• positive regulation of growth hormone secretion
• prepulse inhibition
• phospholipase C-activating dopamine receptor signaling pathway
• negative regulation of dopamine receptor signaling pathway
• positive regulation of ERK1 and ERK2 cascade
• adenylate cyclase-activating adrenergic receptor signaling pathway
• regulation of locomotion involved in locomotory behavior
• positive regulation of glial cell-derived neurotrophic factor secretion
• positive regulation of long-term synaptic potentiation
• negative regulation of voltage-gated calcium channel activity
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Sources: Amigo / QuickGO |
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RNA expression pattern |
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More reference expression data |
Orthologs |
Species |
Human |
Mouse |
Entrez |
1813 |
13489 |
Ensembl |
ENSG00000149295 |
ENSMUSG00000032259 |
UniProt |
P14416 |
P61168 |
RefSeq (mRNA) |
NM_000795 |
NM_010077 |
RefSeq (protein) |
NP_000786 |
NP_034207 |
Location (UCSC) |
Chr 11:
113.41 – 113.48 Mb |
Chr 9:
49.34 – 49.41 Mb |
PubMed search |
[1] |
[2] |
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Dopamine receptor D2, also known as D2R, is a protein that, in humans, is encoded by the DRD2 gene.
Contents
- 1 Function
- 2 Isoforms
- 3 Genetics
- 4 Ligands
- 4.1 Agonists
- 4.2 Partial agonists
- 4.3 Antagonists
- 4.4 Allosteric modulators
- 4.5 Functionally selective ligands
- 5 Protein-protein interactions
- 6 See also
- 7 References
- 8 External links
Function
This gene encodes the D2 subtype of the dopamine receptor, which is coupled to Gi subtype of G protein-coupled receptor. This G protein-coupled receptor inhibits adenylyl cyclase activity.[1]
In mice, regulation of D2R surface expression by the calcium sensor NCS-1 in the dentate gyrus is involved in exploration, synaptic plasticity and memory formation.[2]
In flies, activation of the D2 autoreceptor protected dopamine neurons from cell death induced by a toxin mimicking Parkinson's disease pathology.[3]
Isoforms
Alternative splicing of this gene results in three transcript variants encoding different isoforms.[4]
The long form (D2Lh) has the "canonical" sequence and functions as a classic post-synaptic receptor.[5] The short form (D2Sh) is pre-synaptic and functions as an autoreceptor and regulates the levels of dopamine in the synaptic cleft.[5] Agonism of D2sh receptors inhibits dopamine release; antagonism increases dopaminergic release.[5] A third D2(Longer) form differs from the canonical sequence where 270V is replaced by VVQ.[6]
Genetics
Allelic variants:
- A-241G
- C132T, G423A, T765C, C939T, C957T, and G1101A[7]
- Cys311Ser
- -141C insertion/deletion[8] The polymorphisms have been investigated with respect to association with schizophrenia.[9]
Some researchers have previously associated the polymorphism Taq 1A (rs1800497) to the DRD2 gene. However, the polymorphism resides in exon 8 of the ANKK1 gene.[10] DRD2 TaqIA polymorphism has been reported to be associated with an increased risk for developing motor fluctuations in Parkinson's disease.[11]
Ligands
Most of the older antipsychotic drugs such as chlorpromazine and haloperidol are antagonists for the dopamine D2 receptor, but are, in general, very unselective, at best selective only for the "D2-like family" receptors and so binding to D2, D3 and D4, and often also to many other receptors such as those for serotonin and histamine, resulting in a range of side-effects and making them poor agents for scientific research. In similar manner, older dopamine agonists used for Parkinson's disease such as bromocriptine and cabergoline are poorly selective for one dopamine receptor over another, and, although most of these agents do act as D2 agonists, they affect other subtypes as well. Several selective D2 ligands are, however, now available, and this number is likely to increase as further research progresses.
Agonists
- N,N-Propyldihydrexidine - analogue of the D1/D5 agonist dihydrexidine; Selective for postsynaptic D2 receptor over the presynaptic D2 autoreceptor.
- Cabergoline (Caberl)
- Talipexole - selective for D2 over other dopamine receptors, but also acts as α2-adrenoceptor agonist and 5-HT3 antagonist.
- Piribedil - also D3 receptor agonist and α2-adrenergic antagonist
- Pramipexole - also D3, D4 receptor agonist
- Quinpirole - also D3 receptor agonist
- Quinelorane - affinity for D2 > D3
- Bromocriptine - full agonist
- Ropinirole - full agonist
- Sumanirole - full agonist; highly selective
Partial agonists
- Aplindore
- Aripiprazole (Abilify in USA)[12]
- Brexpiprazole/OPC-34712
- Cariprazine
- RP5063
- GSK-789,472 - Also D3 antagonist, with good selectivity over other receptors [13]
- Ketamine (also NMDA antagonist)
- LSD - in vitro, LSD was found to be a partial agonist and potentiates dopamine-mediated prolactin secretion in lactotrophs.[14] LSD is also a 5-HT2A agonist.
- Roxindole (only at the D2 autoreceptors)
- OSU-6162 - Also 5-HT2A partial agonist, acts as "dopamine stabilizer"
- Salvinorin A - Also κ-opioid agonist.
Antagonists
- Atypical antipsychotics
- Domperidone - D2 and D3 antagonist; does not cross the blood-brain barrier
- Eticlopride
- Fallypride
- Desmethoxyfallypride
- L-741,626 (3-[4-(4-Chlorophenyl)-4-hydroxypiperidin-l-yl]methyl-1H-indole) - highly selective D2 antagonist
- Raclopride - Radiolabled C11 Raclopride is commonly employed in Positron emission tomography studies[15]
- Hydroxyzine (Vistaril, Atarax)
- Itopride
- SV 293[16]
- Typical antipsychotics
- Yohimbine
- D2Sh selective (presynaptic autoreceptors)
- Amisulpride (low doses)
- UH-232
Allosteric modulators
- Homocysteine - allosteric antagonist[17]
- PAOPA[18]
- SB-269,652 [19][20][21]
Functionally selective ligands
Protein-protein interactions
The dopamine receptor D2 has been shown to interact with EPB41L1,[23] PPP1R9B[24] and NCS-1.[25]
Receptor oligomers
The D2 receptor forms receptor heterodimers in vivo (in living animals) with other G protein-coupled receptors; these include:[26]
- D1–D2 dopamine receptor heteromer
- D2–adenosine A2A
- D2–ghrelin receptor
- D2sh–TAAR1 (a presynaptic heterodimer)
The D2 receptor has been shown to form hetorodimers in vitro (and possibly in vivo) with DRD3,[27] DRD5,[28] and 5-HT2A.[29]
See also
References
- ^ Usiello A, Baik JH, Rougé-Pont F, Picetti R, Dierich A, LeMeur M, Piazza PV, Borrelli E (2000). "Distinct functions of the two isoforms of dopamine D2 receptors.". Nature 9 (408): 199–203. PMID 11089973.
- ^ Saab BJ, Georgiou J, Nath A, Lee FJ, Wang M, Michalon A, Liu F, Mansuy IM, Roder JC (2009). "NCS-1 in the dentate gyrus promotes exploration, synaptic plasticity, and rapid acquisition of spatial memory.". Neuron 63 (5): 643–56. doi:10.1016/j.neuron.2009.08.014. PMID 19755107.
- ^ Wiemerslage L, Schultz BJ, Ganguly A, Lee D (2013). "Selective degeneration of dopaminergic neurons by MPP(+) and its rescue by D2 autoreceptors in Drosophila primary culture.". J Neurochem 126 (4): 529–40. doi:10.1111/jnc.12228. PMID 23452092.
- ^ "Entrez Gene: DRD2 dopamine receptor D2".
- ^ a b c Beaulieu JM, Gainetdinov RR (March 2011). "The physiology, signaling, and pharmacology of dopamine receptors". Pharmacol. Rev. 63 (1): 182–217. doi:10.1124/pr.110.002642. PMID 21303898.
- ^ UniProt P14416
- ^ Duan J, Wainwright MS, Comeron JM, Saitou N, Sanders AR, Gelernter J, Gejman PV (February 2003). "Synonymous mutations in the human dopamine receptor D2 (DRD2) affect mRNA stability and synthesis of the receptor". Hum. Mol. Genet. 12 (3): 205–16. doi:10.1093/hmg/ddg055. PMID 12554675.
- ^ Arinami T, Gao M, Hamaguchi H, Toru M (April 1997). "A functional polymorphism in the promoter region of the dopamine D2 receptor gene is associated with schizophrenia". Hum. Mol. Genet. 6 (4): 577–82. doi:10.1093/hmg/6.4.577. PMID 9097961.
- ^ Glatt SJ, Faraone SV, Tsuang MT (July 2004). "DRD2 -141C insertion/deletion polymorphism is not associated with schizophrenia: results of a meta-analysis". Am. J. Med. Genet. B Neuropsychiatr. Genet. 128B (1): 21–3. doi:10.1002/ajmg.b.30007. PMID 15211624.
- ^ Lucht M, Rosskopf D (July 2008). "Comment on "Genetically determined differences in learning from errors"". Science 321 (5886): 200; author reply 200. doi:10.1126/science.1155372. PMID 18621654.
- ^ Wang J, Liu ZL, Chen B. (June 2001). "Association study of dopamine D2, D3 receptor gene polymorphisms with motor fluctuations in PD". Neurology. 56 (12): 1757–9. doi:10.1212/WNL.56.12.1757. PMID 11425949.
- ^ "Clinical Pharmacology for Abilify". RxList.com. 2010-01-21. Retrieved 2010-01-21.
- ^ Holmes IP, Blunt RJ, Lorthioir OE, Blowers SM, Gribble A, Payne AH, Stansfield IG, Wood M, Woollard PM, Reavill C, Howes CM, Micheli F, Di Fabio R, Donati D, Terreni S, Hamprecht D, Arista L, Worby A, Watson SP (March 2010). "The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure". Bioorganic & Medicinal Chemistry Letters 20 (6): 2013–6. doi:10.1016/j.bmcl.2010.01.090. PMID 20153647.
- ^ Giacomelli S, Palmery M, Romanelli L, Cheng CY, Silvestrini B (1998). "Lysergic acid diethylamide (LSD) is a partial agonist of D2 dopaminergic receptors and it potentiates dopamine-mediated prolactin secretion in lactotrophs in vitro". Life Sci. 63 (3): 215–22. doi:10.1016/S0024-3205(98)00262-8. PMID 9698051.
- ^ Wang GJ, Volkow ND, Thanos PK, Fowler JS (2004). "Similarity between obesity and drug addiction as assessed by neurofunctional imaging: a concept review". J Addict Dis 23 (3): 39–53. doi:10.1300/J069v23n03_04. PMID 15256343.
- ^ Huang R, Griffin SA, Taylor M, Vangveravong S, Mach RH, Dillon GH, Luedtke RR (2013). "The effect of SV 293, a D2 dopamine receptor-selective antagonist, on D2 receptor-mediated GIRK channel activation and adenylyl cyclase inhibition.". Pharmacology 92 (1-2): 84–9. doi:10.1159/000351971. PMID 23942137.
- ^ Agnati LF, Ferré S, Genedani S, Leo G, Guidolin D, Filaferro M, Carriba P, Casadó V, Lluis C, Franco R, Woods AS, Fuxe K (Nov 2006). "Allosteric modulation of dopamine D2 receptors by homocysteine.". Journal of proteome research 5 (11): 3077–83. doi:10.1021/pr0601382. PMID 17081059.
- ^ Beyaert MG, Daya RP, Dyck BA, Johnson RL, Mishra RK (2012). "PAOPA, a potent dopamine D2 receptor allosteric modulator, prevents and reverses behavioral and biochemical abnormalities in an amphetamine-sensitized preclinical animal model of schizophrenia". Eur Neuropsychopharmacol 23 (3): 253–62. doi:10.1016/j.euroneuro.2012.04.010. PMID 22658400.
- ^ Lane JR, Donthamsetti P, Shonberg J, Draper-Joyce CJ, Dentry S, Michino M, Shi L, López L, Scammells PJ, Capuano B, Sexton PM, Javitch JA, Christopoulos A (2014). "A new mechanism of allostery in a G protein-coupled receptor dimer". Nat. Chem. Biol. 10 (9): 745–52. doi:10.1038/nchembio.1593. PMID 25108820.
- ^ Maggio R, Scarselli M, Capannolo M, Millan MJ (2014). "Novel dimensions of D3 receptor function: Focus on heterodimerisation, transactivation and allosteric modulation". Eur Neuropsychopharmacol. doi:10.1016/j.euroneuro.2014.09.016. PMID 25453482.
- ^ Silvano E, Millan MJ, Mannoury la Cour C, Han Y, Duan L, Griffin SA, Luedtke RR, Aloisi G, Rossi M, Zazzeroni F, Javitch JA, Maggio R (2010). "The tetrahydroisoquinoline derivative SB269,652 is an allosteric antagonist at dopamine D3 and D2 receptors". Mol. Pharmacol. 78 (5): 925–34. doi:10.1124/mol.110.065755. PMC 2981362. PMID 20702763.
- ^ Möller D, Kling RC, Skultety M, Leuner K, Hübner H, Gmeiner P (2014). "Functionally selective dopamine D₂, D₃ receptor partial agonists". J. Med. Chem. 57 (11): 4861–75. doi:10.1021/jm5004039. PMID 24831693.
- ^ Binda AV, Kabbani N, Lin R, Levenson R (September 2002). "D2 and D3 dopamine receptor cell surface localization mediated by interaction with protein 4.1N". Mol. Pharmacol. 62 (3): 507–13. doi:10.1124/mol.62.3.507. PMID 12181426.
- ^ Smith FD, Oxford GS, Milgram SL (July 1999). "Association of the D2 dopamine receptor third cytoplasmic loop with spinophilin, a protein phosphatase-1-interacting protein". J. Biol. Chem. 274 (28): 19894–900. doi:10.1074/jbc.274.28.19894. PMID 10391935.
- ^ Kabbani N, Negyessy L, Lin R, Goldman-Rakic P, Levenson R (2002). "Interaction with neuronal calcium sensor NCS-1 mediates desensitization of the D2 dopamine receptor.". J. Neurosci. 22 (19): 8476–86. PMID 12351722.
- ^ Beaulieu JM, Espinoza S, Gainetdinov RR (2015). "Dopamine receptors - IUPHAR Review 13". Br. J. Pharmacol. 172 (1): 1–23. doi:10.1111/bph.12906. PMID 25671228.
- ^ Maggio R, Millan MJ (2010). "Dopamine D2-D3 receptor heteromers: pharmacological properties and therapeutic significance". Current Opinion in Pharmacology 10 (1): 100–7. doi:10.1016/j.coph.2009.10.001. PMID 19896900.
- ^ Hasbi A, O'Dowd BF, George SR (2010). "Heteromerization of dopamine D2 receptors with dopamine D1 or D5 receptors generates intracellular calcium signaling by different mechanisms". Current Opinion in Pharmacology 10 (1): 93–9. doi:10.1016/j.coph.2009.09.011. PMC 2818238. PMID 19897420.
- ^ Albizu L, Holloway T, González-Maeso J, Sealfon SC (2011). "Functional crosstalk and heteromerization of serotonin 5-HT2A and dopamine D2 receptors". Neuropharmacology 61 (4): 770–7. doi:10.1016/j.neuropharm.2011.05.023. PMC 3556730. PMID 21645528.
External links
- Receptors, Dopamine D2 at the US National Library of Medicine Medical Subject Headings (MeSH)
- Pappas, Stephanie. "Study: Genes Influence Who Your Friends Are". Imaginova Corp. LiveScience. Retrieved 20 January 2011.
This article incorporates text from the United States National Library of Medicine, which is in the public domain.
Dopaminergics
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Receptor ligands
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DR |
Agonists |
- Adamantanes
- Amantadine
- Memantine
- Rimantadine
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- Aminotetralins
- 7-OH-DPAT
- 8-OH-PBZI
- Rotigotine
- UH-232
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- Benzazepines
- 6-Br-APB
- Fenoldopam
- SKF-38,393
- SKF-77,434
- SKF-81,297
- SKF-82,958
- SKF-83,959
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- Ergolines
- Bromocriptine
- Cabergoline
- Dihydroergocryptine
- Epicriptine
- Lisuride
- LSD
- Pergolide
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- Dihydrexidine derivatives
- 2-OH-NPA
- A-86929
- Adrogolide (ABT-431, DAS-431)
- Ciladopa
- Dihydrexidine
- Dinapsoline
- Dinoxyline
- Doxanthrine
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- Others
- A-68930
- A-77636
- A-412,997
- ABT-670
- ABT-724
- Aplindore
- Apomorphine
- Aripiprazole
- Arketamine
- Bifeprunox
- BP-897
- Captodiame
- CY-208,243
- Dizocilpine
- Esketamine
- Etilevodopa
- Flibanserin
- Ketamine
- Melevodopa
- Modafinil
- Pardoprunox
- Phencyclidine
- PD-128,907
- PD-168,077
- PF-219,061
- Piribedil
- Pramipexole
- Propylnorapomorphine
- Pukateine
- Quinagolide
- Quinelorane
- Quinpirole
- RDS-127
- Ro10-5824
- Ropinirole
- Rotigotine
- Roxindole
- Salvinorin A
- SKF-89,145
- Sumanirole
- Terguride
- Umespirone
- WAY-100,635
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Antagonists |
- Typical antipsychotics
- Acepromazine
- Azaperone
- Benperidol
- Bromperidol
- Clopenthixol
- Chlorpromazine
- Chlorprothixene
- Droperidol
- Flupentixol
- Fluphenazine
- Fluspirilene
- Haloperidol
- Levomepromazine
- Levosulpiride
- Loxapine
- Mesoridazine
- Nemonapride
- Penfluridol
- Perazine
- Periciazine
- Perphenazine
- Pimozide
- Prochlorperazine
- Promazine
- Sulforidazine
- Sulpiride
- Sultopride
- Thioridazine
- Thiothixene
- Trifluoperazine
- Triflupromazine
- Trifluperidol
- Zuclopenthixol
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- Atypical antipsychotics
- Amisulpride
- Asenapine
- Blonanserin
- Cariprazine
- Carpipramine
- Clocapramine
- Clorotepine
- Clozapine
- Gevotroline
- Iloperidone
- Lurasidone
- Melperone
- Molindone
- Mosapramine
- Olanzapine
- Paliperidone
- Perospirone
- Piquindone
- Quetiapine
- Remoxipride
- Risperidone
- Sertindole
- Tiospirone
- Zicronapine
- Ziprasidone
- Zotepine
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- Antiemetics
- AS-8112
- Alizapride
- Bromopride
- Clebopride
- Domperidone
- Metoclopramide
- Thiethylperazine
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- Others
- Amoxapine
- Buspirone
- Butaclamol
- Ecopipam
- EEDQ
- Eticlopride
- Fananserin
- Hydroxyzine
- L-745,870
- Nafadotride
- Nuciferine
- PNU-99,194
- Raclopride
- Sarizotan
- SB-277,011-A
- SCH 23390
- SKF-83,959
- Sonepiprazole
- Spiperone
- Spiroxatrine
- Stepholidine
- Tetrahydropalmatine
- Tiapride
- UH-232
- Yohimbine
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Reuptake modulators
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DAT |
Inhibitors |
- Piperazines
- DBL-583
- GBR-12783
- GBR-12935
- GBR-13069
- GBR-13098
- Nefazodone
- Vanoxerine
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- Piperidines
- 4-Fluoropethidine
- Benocyclidine (BTCP)
- Desoxypipradrol
- Dexmethylphenidate
- Difemetorex
- Ethylphenidate
- HDMP-28
- Methylphenidate
- Pethidine (meperidine)
- Phencyclidine
- Pipradrol
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- Pyrrolidines
- Diphenylprolinol
- MDPV
- Naphyrone
- Prolintane
- Pyrovalerone
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- Tropanes
- Altropane
- Benzatropine (benztropine)
- Brasofensine
- CFT
- Cocaine
- Dichloropane
- Difluoropine
- Etybenzatropine (ethybenztropine)
- FE-β-CPPIT
- FP-β-CPPIT
- Ioflupane (123I)
- RTI-55
- RTI-112
- RTI-113
- RTI-121
- RTI-126
- RTI-150
- RTI-177
- RTI-229
- RTI-336
- Tenocyclidine
- Tesofensine
- Troparil
- Tropoxane
- WF-11
- WF-23
- WF-31
- WF-33
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- Others
- Adrafinil
- Armodafinil
- Amfonelic acid
- Amineptine
- Bromantane
- BTQ
- BTS 74,398
- Bupropion
- Chaenomeles speciosa
- Ciclazindol
- Dasotraline
- Desmethylsertraline
- Diclofensine
- Dimethocaine
- Diphenylpyraline
- Dizocilpine (MK-801)
- DOV-102,677
- DOV-21947
- DOV-216,303
- Efavirenz
- EXP-561
- Fencamfamine
- Fezolamine
- Fluorenol
- GYKI-52895
- Indatraline
- Ketamine
- Lefetamine
- Levophacetoperane
- Liafensine
- LR-5182
- Manifaxine
- Mazindol
- Medifoxamine
- Mesocarb
- Metaphit
- Modafinil
- Nefopam
- Nomifensine
- NS-2359
- O-2172
- Oroxylin A
- Perafensine
- Pridefine
- Radafaxine
- Rimcazole
- Sertraline
- Sibutramine
- Tametraline
- Tedatioxetine
- Tripelennamine
- Venlafaxine
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Enhancers |
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Modulators |
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- Antagonist-like
- SoRI-20041
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VMATs |
- Inhibitors
- Amiodarone
- Amphetamines (e.g., amphetamine, methamphetamine, MDMA)
- Bietaserpine
- Deserpidine
- Efavirenz
- GBR-12935
- Ibogaine
- Ketanserin
- Lobeline
- Reserpine
- Rose bengal
- Tetrabenazine
- Vanoxerine (GBR-12909)
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Releasing agents
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- Morpholines
- Fenbutrazate
- Fenmetramide
- Morazone
- Morforex
- Phendimetrazine
- Phenmetrazine
- Pseudophenmetrazine
|
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- Oxazolines
- 4-MAR
- Aminorex
- Clominorex
- Cyclazodone
- Fenozolone
- Fluminorex
- Pemoline
- Thozalinone
|
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- Phenethylamines (also amphetamines, cathinones, etc)
- 2-OH-PEA
- 4-CAB
- 4-FA
- 4-FMA
- 4-MA
- 4-MMA
- Alfetamine
- Amfecloral
- Amfepentorex
- Amfepramone
- Amphetamine (Dextroamphetamine
- Levoamphetamine)
- Amphetaminil
- β-Me-PEA
- BDB
- BOH
- Benzphetamine
- Buphedrone
- Bupropion
- Butylone
- Cathine
- Cathinone
- Clobenzorex
- Clortermine
- D-Deprenyl
- DMA
- DMMA
- Dimethylamphetamine
- Ephedrine
- Ethcathinone
- EBDB
- Ethylone
- Etilamfetamine
- Famprofazone
- Fenethylline
- Fenproporex
- Flephedrone
- Fludorex
- Furfenorex
- Hordenine
- 4-Hydroxyamphetamine
- Iofetamine (123I)
- Lophophine
- Mefenorex
- Mephedrone
- Metamfepramone
- Methamphetamine
- Dextromethamphetamine
- Levomethamphetamine
- Methcathinone
- Methedrone
- MMDA
- MMDMA
- MBDB
- MDA
- MDEA
- MDMA
- MDMPEA
- MDOH
- MDPEA
- Methylone
- Morforex
- Ortetamine
- pBA
- pCA
- pIA
- Pholedrine
- Phenethylamine
- Pholedrine
- Phenpromethamine
- Prenylamine
- Propylamphetamine
- Pseudoephedrine
- Tiflorex
- Tyramine
- Xylopropamine
- Zylofuramine
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- Piperazines
- 2C-B-BZP
- BZP
- MBZP
- MDBZP
- MeOPP
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- Others
- 2-ADN
- 2-AI
- 2-AT
- 4-BP
- 5-APDI
- 5-IAI
- Clofenciclan
- Cyclopentamine
- Cypenamine
- Cyprodenate
- Feprosidnine
- Gilutensin
- Heptaminol
- Hexacyclonate
- Indanorex
- Isometheptene
- Methylhexanamine
- Naphthylaminopropane
- Octodrine
- Phthalimidopropiophenone
- Propylhexedrine
- Levopropylhexedrine
- Tuaminoheptane
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Enzyme inhibitors
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PAH |
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TH |
- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
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AAAD |
- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
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MAO |
- Nonselective
- Benmoxin
- Caroxazone
- Echinopsidine
- Furazolidone
- Hydralazine
- Indantadol
- Iproclozide
- Iproniazid
- Isocarboxazid
- Isoniazid
- Linezolid
- Mebanazine
- Metfendrazine
- Nialamide
- Octamoxin
- Paraxazone
- Phenelzine
- Pheniprazine
- Phenoxypropazine
- Pivhydrazine
- Procarbazine
- Safrazine
- Tranylcypromine
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- MAO-A selective
- Amiflamine
- Bazinaprine
- Befloxatone
- Brofaromine
- Cimoxatone
- Clorgiline
- CX157 (Tyrima)
- Eprobemide
- Esuprone
- Harmala alkaloids
- Methylene Blue
- Metralindole
- Minaprine
- Moclobemide
- Pirlindole
- Sercloremine
- Tetrindole
- Toloxatone
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- MAO-B selective
- D-Deprenyl
- Ethanol
- Ladostigil
- Lazabemide
- Milacemide
- Nicotine
- Pargyline‡
- Rasagiline
- Safinamide
- Selegiline (L-deprenyl)
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COMT |
- Entacapone
- Nitecapone
- Tolcapone
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DBH |
- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Tropolone
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Others
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Precursors |
- L-Phenylalanine → L-Tyrosine → L-DOPA (levodopa)
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Cofactors |
- Ferrous iron (Fe2+)
- Tetrahydrobiopterin
- Vitamin B3 (Niacin
- Nicotinamide → NADPH)
- Vitamin B6 (Pyridoxine
- Pyridoxamine
- Pyridoxal → Pyridoxal phosphate)
- Vitamin B9 (Folic acid → Tetrahydrofolic acid)
- Vitamin C (Ascorbic acid)
- Zinc (Zn2+)
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Neurotoxins |
- Amphetamine
- Methamphetamine
- MPP+
- MPTP
- Norsalsolinol
- Oxidopamine (6-OHDA)
- Rotenone
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Others |
- Activity enhancers
- BPAP
- PPAP
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- Levodopa prodrugs
- XP21279
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- See also:
- Adrenergics
- Melatonergics
- Serotonergics
- List of dopaminergic drugs
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