DOV-216,303

DOV-216,303
Legal status
Legal status	US: Investigational New Drug ;
Identifiers
	IUPAC name 1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane;
CAS Number	410074-75-8 ;
PubChem CID	9795276;
ChemSpider	7971043 ;
ChEMBL	ChEMBL528995 ;
Chemical and physical data
Formula	C11H11Cl2N
Molar mass	228.117 g/mol g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1C2C1(CNC2)C3=CC(=C(C=C3)Cl)Cl;
	InChI 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 ; Key:BSMNRYCSBFHEMQ-UHFFFAOYSA-N ;
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DOV 216,303 is an 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 K_i 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

Update:[5]

References

McCoy, Michael (August 12, 2004). "Merck and DOV Pharmaceutical In Drug Pact". C&EN.
"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". AdisInsight. Retrieved 26 February 2017.
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): 123–134. doi:10.1111/j.1527-3458.2006.00123.x. PMC 6494125. PMID 16958986.
Chu, Tak-Ho; Cummins, Karen; Stys, Peter K. (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. ISSN 0304-3940. PMID 29578004.

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[1] McCoy, Michael (August 12, 2004). "Merck and DOV Pharmaceutical In Drug Pact". C&EN.

[10K2007-2] "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.

[3] "DOV 216303". AdisInsight. Retrieved 26 February 2017.

[pmid16958986-4] 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): 123–134. doi:10.1111/j.1527-3458.2006.00123.x. PMC 6494125. PMID 16958986.

[ChuCummins2018-5] Chu, Tak-Ho; Cummins, Karen; Stys, Peter K. (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. ISSN 0304-3940. PMID 29578004.

DOV-216,303

See also

References