| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In cerebellar granule cells, orphenadrine hydrochloride (12 µM; 24.5 hours) has neuroprotective properties against 3-NPA-induced neurotoxicity [1].
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|---|---|
| ln Vivo |
In a dose-dependent manner, orphenadrine hydrochloride (10, 20, 30 mg/kg; intraperitoneal injection; once daily for 3 days) decreases 3-NPA-induced mortality [1]. In vivo, orphenadrine hydrochloride (30 mg/kg; intraperitoneally; once daily for three days) exhibits efficacy against neuronal injury produced by 3-NPA [1].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: CGC cells (7-day-old Sprague Dawley rats) Tested Concentrations: 6, 12, 24, 48 µM Incubation Duration: 24.5 h Experimental Results: Prevent cells from aggregation and volume reduction induced by 3-NPA and broken nerves. |
| Animal Protocol |
Animal/Disease Models: Adult male Sprague Dawley rat (275-300 g; 3-NPA toxicity model) [1].
Doses: 10, 20, 30 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 3 days (30 minutes before 3-NPA) Experimental Results: The mortality rate of rats poisoned by 3-NPA was diminished to 10-40% (3 -NPA-treated animals demonstrated general incoordination, lethargy, and general weakness). 3-NPA-induced weight loss was restored, and PBR levels and HSP27 expression were diminished when the dose was 30 mg/kg. (PBR and HSP27 are markers of neuronal damage). |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No published information is available on the use of orphenadrine during breastfeeding. Manufacturer’s estimates indicate that the amount in milk may be low. The drug’s anticholinergic activity might interfere with milk production. An alternate agent may be preferred. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Orphenadrine has anticholinergic activity. Anticholinergics can inhibit lactation in animals, apparently by inhibiting growth hormone and oxytocin secretion. Anticholinergic drugs can also reduce serum prolactin in nonnursing women. The prolactin level in a mother with established lactation may not affect her ability to breastfeed. |
| References | |
| Additional Infomation |
Orphenadrine hydrochloride appears as odorless white or almost white crystalline powder. pH (aqueous solution) about 5.5. Bitter numbing taste. (NTP, 1992)
A muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm. See also: Orphenadrine (has active moiety). |
| Molecular Formula |
C18H23NO.HCL
|
|---|---|
| Molecular Weight |
305.84226
|
| Exact Mass |
305.155
|
| CAS # |
341-69-5
|
| Related CAS # |
Orphenadrine citrate;4682-36-4;Orphenadrine-d3 hydrochloride;1309283-23-5
|
| PubChem CID |
9568
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.014g/cm3
|
| Boiling Point |
363ºC at 760mmHg
|
| Melting Point |
156 - 157ºC
|
| Flash Point |
107.1ºC
|
| LogP |
4.464
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
21
|
| Complexity |
260
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1=CC=CC=C1C(C2=CC=CC=C2)OCCN(C)C.[H]Cl
|
| InChi Key |
UQZKYYIKWZOKKD-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H23NO.ClH/c1-15-9-7-8-12-17(15)18(20-14-13-19(2)3)16-10-5-4-6-11-16;/h4-12,18H,13-14H2,1-3H3;1H
|
| Chemical Name |
N,N-dimethyl-2-[(2-methylphenyl)-phenylmethoxy]ethanamine;hydrochloride
|
| 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 | 3.2697 mL | 16.3484 mL | 32.6968 mL | |
| 5 mM | 0.6539 mL | 3.2697 mL | 6.5394 mL | |
| 10 mM | 0.3270 mL | 1.6348 mL | 3.2697 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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