Introduction：Basic information about CAS 13669-70-0|Nefopam, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Nefopam |
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| CAS Number | 13669-70-0 | Molecular Weight | 253.339 |
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| Density | 1.1±0.1 g/cm3 | Boiling Point | 369.5±37.0 °C at 760 mmHg |
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| Molecular Formula | C17H19NO | Melting Point | / |
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| MSDS | / | Flash Point | 109.0±28.8 °C |
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Names
| Name | 3-Methyl-7-phenyl-6-oxa-3-azabicyclo[6.4.0]dodeca-8,10,12-triene |
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| Synonym | More Synonyms |
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Nefopam BiologicalActivity
| Description | Nefopam (Fenazoxine) is an orally active, non-opioid and non-steroidal centrally acting analgesic agent. Nefopam blocks voltage-sensitive sodium channels (IC50=27 µM) and modulates glutamatergic transmission in rodents. Nefopam can be used in studies of neuropathic pain, anticonvulsant, as well as the prevention of postoperative shivering and hiccups[1][2][3]. |
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| Related Catalog | Signaling Pathways >>Others >>OthersResearch Areas >>Neurological Disease |
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| In Vitro | Nefopam (0.1-100 µM; 15 min) inhibits the uptake of 22Na in a concentration-dependent manner in SK-N-SH cells[1]. Cell Viability Assay[1] Cell Line: SK-N-SH cells Concentration: 0.1-100 µM Incubation Time: 15 min (preincubate) Result: Inhibited the uptake of 22Na with an IC50 value of 27 µM. |
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| In Vivo | Nefopam (0-10 mg/kg; i.v.; single) protects mice against electroshock induced seizures[1].Nefopam (10, 30, 60 mg/kg; i.p.; single) shows a dose-dependent attenuation of mechanical allodynia and decreased neurokinin-1 receptor concentration in vincristine-induced peripheral neuropathy model[2]. Animal Model: Adult male NMRI mice (25-30 g; 6 to7-week-old; electroshock-induced seizures model)[1] Dosage: 0-10 mg/kg Administration: Intravenous injection; single Result: Produced dose-dependent protection against maximal electroshock seizures in mice with an ED50 of 3.8 (2.9-5.1) mg/kg. Animal Model: Adult male mice (10-week-old; 25-30 g; vincristine-induced peripheral neuropathy model)[2]. Dosage: 10, 30, 60 mg/kg Administration: Intraperitoneal injection; single Result: Significantly decreased the percentage of NK1 receptors in the spinal cord at dosage of 60 mg/kg. Showed a sustained increase in paw withdrawal threshold against mechanical stimuli. |
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Chemical & Physical Properties
| Density | 1.1±0.1 g/cm3 |
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| Boiling Point | 369.5±37.0 °C at 760 mmHg |
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| Molecular Formula | C17H19NO |
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| Molecular Weight | 253.339 |
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| Flash Point | 109.0±28.8 °C |
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| Exact Mass | 253.146667 |
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| PSA | 12.47000 |
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| LogP | 3.44 |
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| Vapour Pressure | 0.0±0.8 mmHg at 25°C |
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| Index of Refraction | 1.564 |
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| InChIKey | RGPDEAGGEXEMMM-UHFFFAOYSA-N |
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| SMILES | CN1CCOC(c2ccccc2)c2ccccc2C1 |
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| Storage condition | 2-8°C |
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Toxicological Information
CHEMICAL IDENTIFICATION - RTECS NUMBER :
- DM4210000
- CHEMICAL NAME :
- 1H-2,5-Benzoxazocine, 3,4,5,6,7-tetrahydro-5-methyl-1-phenyl-
- CAS REGISTRY NUMBER :
- 13669-70-0
- LAST UPDATED :
- 199703
- DATA ITEMS CITED :
- 4
- MOLECULAR FORMULA :
- C17-H19-N-O
- MOLECULAR WEIGHT :
- 253.37
- WISWESSER LINE NOTATION :
- T68 HN KO&TJ H1 LR
HEALTH HAZARD DATAACUTE TOXICITY DATA - TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - woman
- DOSE/DURATION :
- 15 mg/kg
- TOXIC EFFECTS :
- Behavioral - changes in motor activity (specific assay) Cardiac - change in rate
- REFERENCE :
- BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 283,1508,1981
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Human - man
- DOSE/DURATION :
- 17 mg/kg
- TOXIC EFFECTS :
- Behavioral - hallucinations, distorted perceptions Behavioral - excitement Cardiac - pulse rate increase, without fall in BP
- REFERENCE :
- BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 283,1508,1981
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 180 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- REFERENCE :
- USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4198424
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 50 mg/kg
- TOXIC EFFECTS :
- Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation)
- REFERENCE :
- DDEVD6 Drug Development and Evaluation. (Gustav Fischer Verlag, Postfach 720143, D-7000 Stuttgart 70, Fed. Rep. Ger.) V.1- 1977- Volume(issue)/page/year: 3,10,1979
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Safety Information
Customs
| HS Code | 2933990090 |
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| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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Synonyms
| 5-Methyl-1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazocine |
| Sinalgico |
| EINECS 237-148-2 |
| 5-methyl-1-phenyl-3,4,5,6-tetrahydro-1H-2,5-benzoxazocine hydrochloride |
| 5-Methyl-1-phenyl-3,4,5,6-tetrahydro-1H-benzo[f][1,4]oxazocine |
| Ajan |
| 1H-2,5-Benzoxazocine, 3,4,5,6-tetrahydro-5-methyl-1-phenyl- |
| 3,4,5,6-Tetrahydro-5-methyl-1-phenyl-1H-2,5-benzoxazocine |
| Nefopam |
| MFCD00056181 |
| Acupan |
