| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
5-HT
|
|---|---|
| ln Vitro |
Duloxetine ((S)-Duloxetine hydrochloride) (sold under the brand names Cymbalta, Ariclaim, Xeristar, Yentreve, Duzela, Dulane) is an SNRI (serotonin-norepinephrine reuptake inhibitor) that Eli Lilly makes and sells. It is recommended for both generalized anxiety disorder (GAD) and major depressive disorder. Moreover, duloxetine is approved for the treatment of musculoskeletal pain and osteoarthritis. Due to worries about liver toxicity and suicidal thoughts, duloxetine was not approved for this indication in the US; however, it was approved in Europe, where it is advised as a supplement to surgery in cases of stress urinary incontinence. It can also relieve the symptoms of painful peripheral neuropathy, particularly diabetic neuropathy, and it is used to control the symptoms of fibromyalgia. Duloxetine is mostly used to treat major depressive disorder, general anxiety disorder, stress-related urinary incontinence, painful peripheral neuropathy, fibromyalgia, chronic lower back pain, and musculoskeletal pain linked to osteoarthritis. Numerous other indications are being researched on it.
|
| ln Vivo |
Duloxetine is a dual reuptake inhibitor of serotonin and norepinephrine, and is shown to be effective against pain. However, whether and how duloxetine can attenuate oxaliplatin-induced allodynia in rodents is not clearly understood. A single injection of oxaliplatin (6 mg/kg, intraperitoneal; i.p.) induced a cold and mechanical allodynia, which was assessed by acetone and von Frey filament tests, respectively. When significant allodynic signs were observed, three different doses of duloxetine (10, 30, and 60 mg/kg, i.p.) were injected. Administration of 30 and 60 mg/kg of duloxetine significantly reduced the allodynia, whereas 10 mg/kg did not. By using an in vivo extracellular recording method, we further confirmed that 30 mg/kg of duloxetine could significantly inhibit the hyperexcitability of spinal wide dynamic range (WDR) cells. The anti-allodynic effect of duloxetine was completely blocked by an intrathecal injection of phentolamine (non-selective α-adrenergic receptor antagonist, 20 μg), or prazosin (α₁-adrenergic receptor antagonists, 10 μg); however, idazoxan (α₂-adrenergic receptor antagonist, 10 μg) did not block it. In conclusion, we suggest that duloxetine may have an effective protective action against oxaliplatin-induced neuropathic pain and spinal hyperexcitability, which is mediated by spinal α₁-adrenergic receptors[2].
|
| Animal Protocol |
Duloxetine was dissolved in distilled water (D.W.). Different doses of duloxetine (10, 30, and 60 mg/kg) were administered (i.p.). To test which adrenergic receptor subtypes mediated the anti-allodynic effects of duloxetine in oxaliplatin-administered mice, antagonists were administered intrathecally 20 min prior to duloxetine treatments. Non-selective α-adrenergic antagonists (phentolamine, 20 μg), α1-adrenergic receptor antagonists (prazosin, 10 μg), and α2-adrenergic receptor antagonists (idazoxan, 10 μg) were administered in volumes of 5 μL. The dose of each antagonist was determined based on previously conducted studies showing the selective and effective antagonistic action against adrenergic receptor-mediated responses.[3]
|
| References | |
| Additional Infomation |
Duloxetine hydrochloride is a hydrochloride. It contains a duloxetine.
|
| Molecular Formula |
C18H20CLNOS
|
|---|---|
| Molecular Weight |
333.88
|
| Exact Mass |
333.095
|
| Elemental Analysis |
C, 64.75; H, 6.04; Cl, 10.62; N, 4.20; O, 4.79; S, 9.60
|
| CAS # |
947316-47-4
|
| Related CAS # |
Duloxetine hydrochloride;136434-34-9;Duloxetine;116539-59-4;Duloxetine-d3 hydrochloride;1435727-97-1;(±)-Duloxetine-d3 hydrochloride
|
| PubChem CID |
44181886
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
5.823
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
22
|
| Complexity |
312
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
Cl.S1C=CC=C1C(CCNC)OC1=CC=CC2C=CC=CC1=2
|
| InChi Key |
BFFSMCNJSOPUAY-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H19NOS.ClH/c1-19-12-11-17(18-10-5-13-21-18)20-16-9-4-7-14-6-2-3-8-15(14)16;/h2-10,13,17,19H,11-12H2,1H3;1H
|
| Chemical Name |
N-methyl-3-naphthalen-1-yloxy-3-thiophen-2-ylpropan-1-amine;hydrochloride
|
| Synonyms |
RS)-Duloxetine hydrochloride; 947316-47-4; N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propan-1-amine hydrochloride; rac-Duloxetine Hydrochloride (1:1 R:S Mixtures); ( inverted exclamation markA)-Duloxetine (hydrochloride); N-methyl-3-naphthalen-1-yloxy-3-thiophen-2-ylpropan-1-amine;hydrochloride; N-methyl-gAmma-(1-naphthalenyloxy)-2-thiophenepropanamine, hydrochloride; Duloxetine EP impurity A;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9951 mL | 14.9754 mL | 29.9509 mL | |
| 5 mM | 0.5990 mL | 2.9951 mL | 5.9902 mL | |
| 10 mM | 0.2995 mL | 1.4975 mL | 2.9951 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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