[CAS NO. 66504-40-3] DOV-216,303FreeBase
PRODUCTS SPECIFICATIONS [66504-40-3]
DESCRIPTION [66504-40-3]
Overview
| MDL | MFCD22381599 |
|---|---|
| Molecular Weight | 228.12 |
| Molecular Formula | C11H11Cl2N |
| SMILES | ClC1=C(Cl)C=C(C=C1)C12CC1CNC2 |
Summary
DOV-216,303 (Free Base) is a potent triple serotonin , norepinephrine, and dopamine reuptake inhibitor, with IC 50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively [1] . Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats [2] .
IC50 & Target
IC50: 14 nM (serotonin), 20 nM (norepinephrine), 78 nM (dopamine) [1] .
In Vivo
Acute treatment of DOV-216,303 (20 mg/kg, i.p.) significantly increases dopamine, norepinephrine and serotonin levels in both OBX and Sham animals
[2]
.
Chronic treatment with DOV 216,303 (20 mg/kg, i.p., for 17 days) increases extracellular concentrations of dopamine, norepinephrine and serotonin in the medial prefrontal cortex of both OBX and Sham animals and significantly increases extracellular baseline serotonin concentrations
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Sprague Dawley rats weighing between 290 and 350 g at time of OBX or Sham surgery [2] . |
| Dosage: | 20 mg/kg. |
| Administration: | I.P. daily for 17days. |
| Result: | Increased extracellular concentrations of dopamine, norepinephrine and serotonin in the medial prefrontal cortex of both OBX and Sham animals and significantly increased extracellular baseline serotonin concentrations. |
| Animal Model: | Male Sprague Dawley rats weighing between 290 and 350 g at time of OBX or Sham surgery [2] . |
| Dosage: | 20 mg/kg. |
| Administration: | I.P. once. |
| Result: | Significant increases in dopamine, norepinephrine and serotonin levels were measured in both OBX and Sham animals. |
Appearance
Oil
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Pure form | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 125 mg/mL ( 547.96 mM )
Ethanol : 100 mg/mL ( 438.37 mM ; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.3837 mL | 21.9183 mL | 43.8366 mL |
| 5 mM | 0.8767 mL | 4.3837 mL | 8.7673 mL |
| 10 mM | 0.4384 mL | 2.1918 mL | 4.3837 mL |
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1.
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Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (9.12 mM); Clear solution
References
- [1] Shao L, et al. Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1438-41.
- [2] Prins J, et al. 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.
