WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H413910
CAS#: 66504-40-3 (free base)
Description: DOV-216303 free base is a potent triple serotonin, norepinephrine, and dopamine reuptake inhibitor, with IC50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats.
Hodoodo Cat#: H413910
Name: DOV-216303 free base
CAS#: 66504-40-3 (free base)
Chemical Formula: C11H11Cl2N
Exact Mass: 227.03
Molecular Weight: 228.116
Elemental Analysis: C, 57.92; H, 4.86; Cl, 31.08; N, 6.14
Related CAS #: 86215-36-3 (HCl) 66504-40-3 (free base)
Synonym: DOV-216303 free base; DOV 216,303 free base
IUPAC/Chemical Name: 1-(3,4-Dichlorophenyl)-3-azabicyclo(3.1.0)hexane
InChi Key: BSMNRYCSBFHEMQ-UHFFFAOYSA-N
InChi Code: 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
SMILES Code: ClC1=CC=C(C23CNCC2C3)C=C1Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
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The following data is based on the product molecular weight 228.12 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Sørensen G, Husum H, Brennum LT, Bundgaard C, Montezinho LC, Mørk A, Wörtwein G, Woldbye DP. Addiction-related effects of DOV 216,303 and cocaine: A comparative study in the mouse. Basic Clin Pharmacol Toxicol. 2014 Jun;114(6):451-9. doi: 10.1111/bcpt.12182. Epub 2014 Jan 16. PMID: 24314270.
2: Skolnick P, Krieter P, Tizzano J, Basile A, Popik P, Czobor P, Lippa A. Preclinical and clinical pharmacology of DOV 216,303, a "triple" reuptake inhibitor. CNS Drug Rev. 2006 Summer;12(2):123-34. doi: 10.1111/j.1527-3458.2006.00123.x. PMID: 16958986; PMCID: PMC6494125.
3: Beer B, Stark J, Krieter P, Czobor P, Beer G, Lippa A, Skolnick P. DOV 216,303, a "triple" reuptake inhibitor: safety, tolerability, and pharmacokinetic profile. J Clin Pharmacol. 2004 Dec;44(12):1360-7. doi: 10.1177/0091270004269560. PMID: 15545306.
4: Chu TH, Cummins K, Stys PK. The triple monoamine re-uptake inhibitor DOV 216,303 promotes functional recovery after spinal cord contusion injury in mice. Neurosci Lett. 2018 May 14;675:1-6. doi: 10.1016/j.neulet.2018.03.050. Epub 2018 Mar 22. PMID: 29578004.
5: Skolnick P, Popik P, Janowsky A, Beer B, Lippa AS. Antidepressant-like actions of DOV 21,947: a "triple" reuptake inhibitor. Eur J Pharmacol. 2003 Feb 14;461(2-3):99-104. doi: 10.1016/s0014-2999(03)01310-4. PMID: 12586204.
6: Tizzano JP, Stribling DS, Perez-Tilve D, Strack A, Frassetto A, Chen RZ, Fong TM, Shearman L, Krieter PA, Tschöp MH, Skolnick P, Basile AS. The triple uptake inhibitor (1R,5S)-(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0] hexane hydrochloride (DOV 21947) reduces body weight and plasma triglycerides in rodent models of diet-induced obesity. J Pharmacol Exp Ther. 2008 Mar;324(3):1111-26. doi: 10.1124/jpet.107.133132. Epub 2007 Dec 18. PMID: 18089843.
7: Breuer ME, Chan JS, Oosting RS, Groenink L, Korte SM, Campbell U, Schreiber R, Hanania T, Snoeren EM, Waldinger M, Olivier B. The triple monoaminergic reuptake inhibitor DOV 216,303 has antidepressant effects in the rat olfactory bulbectomy model and lacks sexual side effects. Eur Neuropsychopharmacol. 2008 Dec;18(12):908-16. doi: 10.1016/j.euroneuro.2008.07.011. Epub 2008 Sep 11. PMID: 18789657.
8: Prins J, Westphal KG, Korte-Bouws GA, Quinton MS, Schreiber R, Olivier B, Korte SM. The potential and limitations of DOV 216,303 as a triple reuptake inhibitor for the treatment of major depression: a microdialysis study in olfactory bulbectomized rats. Pharmacol Biochem Behav. 2011 Jan;97(3):444-52. doi: 10.1016/j.pbb.2010.10.001. Epub 2010 Oct 8. PMID: 20934452.
9: Prins J, Denys DA, Westphal KG, Korte-Bouws GA, Quinton MS, Schreiber R, Groenink L, Olivier B, Korte SM. The putative antidepressant DOV 216,303, a triple reuptake inhibitor, increases monoamine release in the prefrontal cortex of olfactory bulbectomized rats. Eur J Pharmacol. 2010 May 10;633(1-3):55-61. doi: 10.1016/j.ejphar.2010.02.009. Epub 2010 Feb 12. PMID: 20153745.
10: Prins J, Kenny PJ, Doomernik I, Schreiber R, Olivier B, Mechiel Korte S. The triple reuptake inhibitor DOV 216,303 induces long-lasting enhancement of brain reward activity as measured by intracranial self-stimulation in rats. Eur J Pharmacol. 2012 Oct 15;693(1-3):51-6. doi: 10.1016/j.ejphar.2012.07.047. Epub 2012 Aug 21. PMID: 23010469.
