Chemical compound
- US: Investigational New Drug
Identifiers |
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CAS Number | - 66504-40-3 N
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PubChem CID | |
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ChemSpider | - 7971043 N
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UNII | |
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ChEMBL | - ChEMBL528995 N
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Chemical and physical data |
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Formula | C11H11Cl2N |
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Molar mass | 228.12 g·mol−1 |
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3D model (JSmol) | |
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InChI=1S/C11H11Cl2N/c12-9-2-1-7(3-10(9)13)11-4-8(11)5-14-6-11/h1-3,8,14H,4-6H2 NKey:BSMNRYCSBFHEMQ-UHFFFAOYSA-N N |
NY (what is this?) (verify) |
DOV 216,303 is an experimental antidepressant drug originally developed by DOV Pharmaceutical and was licensed to Merck & Co. in 2004;[1] Merck and DOV terminated their relationship in December 2006.[2]: 12 [3]
It is a triple reuptake inhibitor (TRI), or serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI).[4] It is the racemic mixture of amitifadine (DOV-21,947) and its (–)-enantiomer, DOV-102,677. Its IC50 values for SERT, NET, and DAT are Ki 14 nM, 20 nM, and 78 nM, respectively.[4]
As of March 2008, DOV had no intention to further develop DOV-216,303 because the patent on the compound had expired.[2]: 6
In a mouse model, DOV-216,303 has shown the ability to promote recovery after spinal cord contusion.[5]
See also
References
- ^ McCoy M (August 12, 2004). "Merck and DOV Pharmaceutical In Drug Pact". Chemical & Engineering News.
- ^ a b "10-K For the fiscal year ended December 31, 2007". Dov Pharmaceutical via SEC Edgar. March 31, 2008.
DOV 216,303 was originally in development for depression; however as the patented composition of matter claim has expired, there are no ongoing clinical trials of DOV 216,303 and none are planned.
- ^ "DOV 216303". Adis Insight. Springer Nature Switzerland AG. Retrieved 26 February 2017.
- ^ a b Skolnick P, Krieter P, Tizzano J, Basile A, Popik P, Czobor P, Lippa A (2006). "Preclinical and clinical pharmacology of DOV 216,303, a "triple" reuptake inhibitor". CNS Drug Reviews. 12 (2): 123–34. doi:10.1111/j.1527-3458.2006.00123.x. PMC 6494125. PMID 16958986.
- ^ Chu TH, Cummins K, Stys PK (May 2018). "The triple monoamine re-uptake inhibitor DOV 216,303 promotes functional recovery after spinal cord contusion injury in mice". Neuroscience Letters. 675: 1–6. doi:10.1016/j.neulet.2018.03.050. PMID 29578004. S2CID 5007186.
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SSRIsTooltip Selective serotonin reuptake inhibitors | |
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SNRIsTooltip Serotonin–norepinephrine reuptake inhibitors | |
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NRIsTooltip Norepinephrine reuptake inhibitors | |
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NDRIsTooltip Norepinephrine–dopamine reuptake inhibitors | |
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NaSSAsTooltip Noradrenergic and specific serotonergic antidepressants | |
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SARIsTooltip Serotonin antagonist and reuptake inhibitors | |
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SMSTooltip Serotonin modulator and stimulators | |
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Others | |
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TCAsTooltip Tricyclic antidepressants | |
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TeCAsTooltip Tetracyclic antidepressants | |
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Others | |
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Non-selective | |
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MAOATooltip Monoamine oxidase A-selective | |
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MAOBTooltip Monoamine oxidase B-selective | |
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DATTooltip Dopamine transporter (DRIsTooltip Dopamine reuptake inhibitors) | |
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NETTooltip Norepinephrine transporter (NRIsTooltip Norepinephrine reuptake inhibitors) | | | | | | | - Others: Antihistamines (e.g., brompheniramine, chlorphenamine, pheniramine, tripelennamine)
- Antipsychotics (e.g., loxapine, ziprasidone)
- Arylcyclohexylamines (e.g., ketamine, phencyclidine)
- Dopexamine
- Ephenidine
- Ginkgo biloba
- Indeloxazine
- Nefazodone
- Opioids (e.g., desmetramadol, methadone, pethidine (meperidine), tapentadol, tramadol, levorphanol)
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SERTTooltip Serotonin transporter (SRIsTooltip Serotonin reuptake inhibitors) | | | | | - Others: A-80426
- Amoxapine
- Antihistamines (e.g., brompheniramine, chlorphenamine, dimenhydrinate, diphenhydramine, mepyramine (pyrilamine), pheniramine, tripelennamine)
- Antipsychotics (e.g., loxapine, ziprasidone)
- Arylcyclohexylamines (e.g., 3-MeO-PCP, esketamine, ketamine, methoxetamine, phencyclidine)
- Cyclobenzaprine
- Delucemine
- Dextromethorphan
- Dextrorphan
- Efavirenz
- Hypidone
- Medifoxamine
- Mesembrine
- Mifepristone
- MIN-117 (WF-516)
- N-Me-5-HT
- Opioids (e.g., dextropropoxyphene, methadone, pethidine (meperidine), levorphanol, tapentadol, tramadol)
- Roxindole
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VMATsTooltip Vesicular monoamine transporters | |
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Others | |
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See also: Receptor/signaling modulators • Monoamine releasing agents • Adrenergics • Dopaminergics • Serotonergics • Monoamine metabolism modulators • Monoamine neurotoxins |