Sultopride |
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| Trade names | Barnetil, Barnotil, Topral |
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| AHFS/Drugs.com | International Drug Names |
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Routes of administration | Oral, IM |
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| ATC code | |
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| Legal status |
- BR: Class C1 (Other controlled substances)[1]
- In general: ℞ (Prescription only)
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| Elimination half-life | 3–5 hours |
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N-[(1-ethylpyrrolidin-2-yl)methyl]-5-ethylsulfonyl-2-methoxybenzamide
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| CAS Number | |
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| PubChem CID | |
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| ChemSpider | |
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| UNII | |
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| KEGG | |
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| ChEMBL | |
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| CompTox Dashboard (EPA) | |
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| ECHA InfoCard | 100.053.293 |
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| Formula | C17H26N2O4S |
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| Molar mass | 354.47 g·mol−1 |
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| 3D model (JSmol) | |
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O=S(=O)(c1cc(c(OC)cc1)C(=O)NCC2N(CC)CCC2)CC
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InChI=1S/C17H26N2O4S/c1-4-19-10-6-7-13(19)12-18-17(20)15-11-14(24(21,22)5-2)8-9-16(15)23-3/h8-9,11,13H,4-7,10,12H2,1-3H3,(H,18,20) YKey:UNRHXEPDKXPRTM-UHFFFAOYSA-N Y
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N Y (what is this?) (verify) |
Sultopride (trade names Barnetil, Barnotil, Topral) is an atypical antipsychotic of the benzamide chemical class used in Europe, Japan, and Hong Kong for the treatment of schizophrenia.[2][3][4] It was launched by Sanofi-Aventis in 1976.[2] Sultopride acts as a selective D2 and D3 receptor antagonist.[5] It has also been shown to have clinically relevant affinity for the GHB receptor as well, a property it shares in common with amisulpride and sulpiride.[6]
Pharmacology
Sultopride
| Site
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Ki
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Species
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Ref
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| D2
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1.6
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Human
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[7]
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| D3
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3.8
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Human
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[7]
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References
- ^ Anvisa (2023-03-31). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 2023-04-04). Archived from the original on 2023-08-03. Retrieved 2023-08-16.
- ^ a b Miguel Vela J, Buschmann H, Holenz J, Párraga A, Torrens A (2007). Antidepressants, Antipsychotics, Anxiolytics: From Chemistry and Pharmacology to Clinical Application. Weinheim: Wiley-VCH. ISBN 978-3-527-31058-6.
- ^ Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. ISBN 3-88763-075-0.
- ^ European Drug Index (4th ed.). Boca Raton: CRC Press. 1998. ISBN 3-7692-2114-1.
- ^ Burstein ES, Ma J, Wong S, Gao Y, Pham E, Knapp AE, et al. (December 2005). "Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist". The Journal of Pharmacology and Experimental Therapeutics. 315 (3): 1278–1287. doi:10.1124/jpet.105.092155. PMID 16135699. S2CID 2247093.
- ^ Maitre M, Ratomponirina C, Gobaille S, Hodé Y, Hechler V (April 1994). "Displacement of [3H] gamma-hydroxybutyrate binding by benzamide neuroleptics and prochlorperazine but not by other antipsychotics". European Journal of Pharmacology. 256 (2): 211–214. doi:10.1016/0014-2999(94)90248-8. PMID 7914168.
- ^ a b Burstein ES, Ma J, Wong S, Gao Y, Pham E, Knapp AE, et al. (December 2005). "Intrinsic efficacy of antipsychotics at human D2, D3, and D4 dopamine receptors: identification of the clozapine metabolite N-desmethylclozapine as a D2/D3 partial agonist". The Journal of Pharmacology and Experimental Therapeutics. 315 (3): 1278–1287. doi:10.1124/jpet.105.092155. PMID 16135699. S2CID 2247093.
Antipsychotics (N05A) |
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| Typical | |
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| Disputed |
- Tricyclics: Carpipramine
- Clocapramine
- Clorotepine
- Clotiapine
- Loxapine
- Mosapramine
- Oxyprothepin decanoate
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| Atypical | |
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| Others |
- Muscarinic agonists: Xanomeline/trospium chloride
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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Dopamine receptor modulators |
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| D1-like | | Agonists |
- Benzazepines: 6-Br-APB
- Fenoldopam
- SKF-38,393
- SKF-77,434
- SKF-81,297
- SKF-82,958
- SKF-83,959
- Trepipam
- Zelandopam
- Dihydrexidine derivatives: A-77636
- A-86929
- Adrogolide (ABT-431, DAS-431)
- Dihydrexidine
- Dinapsoline
- Dinoxyline
- Doxanthrine
- Phenethylamines: BCO-001
- Deoxyepinephrine (N-methyldopamine, epinine)
- Dipropyldopamine (DPDA)
- Dopamine
- Dopexamine
- Etilevodopa
- Ibopamine
- L-DOPA (levodopa)
- Lu AE04621
- Melevodopa
- L-Phenylalanine
- L-Tyrosine
- XP21279
- Others: A-68930
- Apomorphine
- Isocorypalmine
- Lu AF28996
- Nuciferine
- PF-06412562
- PF-6649751
- PF 6669571
- Propylnorapomorphine
- Rotigotine
- SKF-89,145
- SKF-89,626
- Stepholidine
- Tavapadon
- Tetrahydropalmatine
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| PAMs |
- Tetrahydroisoquinolines: DETQ
- DPTQ
- Glovadalen
- Mevidalen
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| Antagonists |
- Others: Berupipam
- Ecopipam
- EEDQ
- Metitepine (methiothepin)
- Odapipam
- Perlapine
- SCH-23390
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| D2-like | | Agonists |
- Aminotetralins: 5-OH-DPAT
- 7-OH-DPAT
- 8-OH-PBZI
- CHF-1024
- Nolomirole
- Rotigotine
- UH-232
- Dihydrexidine derivatives: 2-OH-NPA
- Ciladopa
- Dihydrexidine
- Dinoxyline
- N,N-Propyldihydrexidine
- Phenethylamines: Deoxyepinephrine (N-methyldopamine, epinine)
- Dipropyldopamine (DPDA)
- Dopamine
- Dopexamine
- Etilevodopa
- Ibopamine
- L-DOPA (levodopa)
- Lu AE04621
- L-Phenylalanine
- RU-24213
- L-Tyrosine
- Melevodopa
- XP21279
- Atypical antipsychotics: Alentemol (U-66444B)
- Aripiprazole (+sertraline)
- Aripiprazole lauroxil
- Bifeprunox
- Brexpiprazole
- Brilaroxazine
- Cariprazine
- F-15063
- Lumateperone
- Norclozapine
- Others: 3-PPP
- A-412997
- ABT-670
- ABT-724
- Adrafinil
- Aplindore
- Apomorphine
- Arketamine
- Armodafinil
- BP-897
- Captodiame
- CP-226,269
- Debenzergoline
- Dizocilpine
- Esketamine
- Etrabamine
- Flibanserin
- 7-Hydroxyropinirole (SK&F-89124)
- Ketamine
- Lu AF28996
- Matsupexole
- Modafinil
- Naxagolide
- OSU-6162
- Pardoprunox
- PD-128,907
- PD-168,077
- PF-219,061
- PF-592,379
- Phencyclidine
- Piribedil
- Pramipexole
- Preclamol
- Propylnorapomorphine
- Pukateine
- Quinagolide
- Quinelorane
- Quinpirole
- RDS-127
- Ro10-5824
- Ropinirole
- Roxindole
- S32504
- Salvinorin A
- SKF-39315
- SKF-83,959
- Sumanirole
- Talipexole
- Umespirone
- WAY-100,635
- XC-130
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| Antagonists |
- Others: 3-PPP
- Alpiropride
- Azapride
- Bromerguride
- Bromocriptine
- Buspirone
- Carmoxirole
- Desmethoxyfallypride
- EEDQ
- F-15063
- Fallypride
- Fananserin
- Fenfluramine
- Iodobenzamide
- Isocorypalmine
- L-741,626
- L-745,870
- Levofenfluramine
- LEK-8829
- Metitepine (methiothepin)
- N-Methylspiperone
- Nafadotride
- Nuciferine
- Ordopidine
- PNU-99,194
- Pridopidine
- Raclopride
- Sarizotan
- SB-277,011-A
- Seridopidine
- Sonepiprazole
- Spiroxatrine
- Stepholidine
- SV-293
- Tetrahydropalmatine
- Tiapride
- UH-232
- XC-130
- Yohimbine
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- See also: Receptor/signaling modulators
- Adrenergics
- Serotonergics
- Monoamine reuptake inhibitors
- Monoamine releasing agents
- Monoamine metabolism modulators
- Monoamine neurotoxins
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Receptor (ligands) | | GHBRTooltip GHB receptor |
- Agonists: Main site: 1,4-BD
- 3-HPA
- Aceburic acid (GHB acetate)
- BDDA (DABD)
- EAB
- GBL
- GCL
- GHB
- GHBAL
- GHV (4-methyl-GHB)
- GVL
- HOCHCA
- HOCPCA
- JZP-386
- MAB
- NCS-356
- NCS-435
- Sodium oxybate
- T-HCA (GHC)
- THF
- UMB58
- UMB66
- UMB68
- UMB72
- UMB73
- UMB86
- Valiloxybate (XW-10172); Positive allosteric modulators: (+)-Catechin
- Monastrol
- Antagonists: Main site: Gabazine (SR-95531)
- NCS-382
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| GABABTooltip γ-Aminobutyric acid B receptor | |
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Transporter (blockers) | | MCTsTooltip Monocarboxylate transporters | |
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| SMCTsTooltip Sodium-coupled monocarboxylate transporters | |
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| VIATTTooltip Vesicular inhibitory amino acid transporter | |
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Enzyme (inhibitors) | | SSRTooltip Succinic semialdehyde reductase | |
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| GHBDHTooltip 4-Hydroxybutyrate dehydrogenase | |
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| HOTTooltip Hydroxyacid-oxoacid transhydrogenase | |
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| ADHTooltip Alcohol dehydrogenase | |
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| ALDHTooltip Aldehyde dehydrogenase | |
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- See also
- Receptor/signaling modulators
- GABA receptor modulators
- Glutamate receptor modulators
- Glycine receptor modulators
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