(±)-Nefopam hydrochloride
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(±)-Nefopam hydrochloride
structure -
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CAS No:
23327-57-3
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Formula:
C17H19NO.ClH
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Chemical Name:
(±)-Nefopam hydrochloride
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Synonyms:
1H-2,5-Benzoxazocine,3,4,5,6-tetrahydro-5-methyl-1-phenyl-,hydrochloride (1:1);1H-2,5-Benzoxazocine,3,4,5,6-tetrahydro-5-methyl-1-phenyl-,hydrochloride;Fenazoxine;Fenazoxine hydrochloride;Nefopam hydrochloride;R 738;Ajan;Acupan;(±)-Nefopam hydrochloride;24358-94-9;34791-79-2;69319-31-9
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CAS No:
Description
Nefopam is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain.
Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26)
Characteristics
12.5
3.97790
white to beige
1.064g/cm3
238-242 °C
369.5ºC at 760mmHg
109ºC
H2O: soluble 5mg/mL, clear
2-8°C
1.18E-05mmHg at 25°C
LD50 in mice, rats (mg/kg): 119, 178 orally; 44.5, 28 i.v. (Baltes)
Safety Information
Ⅲ
6.1(b)
3249
3
23/24/25
36/37/39-45
T
P261-P280-P301 + P310-P311
H301 + H311 + H331
|Danger|H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P310, P302+P352, P304+P340, P311, P312, P321, P322, P330, P361, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 53 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
Drug Information
Treatment of acute pain
A subclass of analgesic agents that typically do not bind to OPIOID RECEPTORS and are not addictive. Many non-narcotic analgesics are offered as NONPRESCRIPTION DRUGS. (See all compounds classified as Analgesics, Non-Narcotic.)
Acupan
(±)-Nefopam hydrochloride Use and Manufacturing
Intermediate 1-((2-(methylamino)methyl)phenyl)-1-phenylmethanol hydrochloride (14.5 g, 0.055 mol), Dichloromethane (200 mL), Triethylamine (14.0 g, 0.14 mol) was added to the nitrogen protected reaction system.Reduce the temperature to 0 °C, A solution of chloroacetyl chloride (7 g, 0.06 mmol) in DCM (50 mL) was slowly added dropwise. After completion of the addition, the reaction was continued for 2 h and the temperature was raised to 25 °C.Add isopropyl alcohol (150 mL), Potassium tert-butoxide (6.8g, 0.06mol)Isopropanol (50mL)The solution was slowly added dropwise to the reaction system.After the addition, the reaction was completed for 1 h, and the pH was adjusted to about 6.5 with glacial acetic acid.Sodium borohydride (6.3 g, 0.165 mol) was added, Stir at room temperature for 18h, slowly add ice water, stir for 30min, layer, The organic layer is flushed with hydrochloric acid to a pH of about 1, Hydrochloric acid gas was stopped and the mixture was filtered. The filter cake was washed with a mixture of isopropyl alcohol and dichloromethane (volume ratio of 1:1) and dried to obtain 10.4 g of the target compound in a yield of 65percent
A cyclized analog of orphenadrine and diphenhydramine; representative of a new class of centrally acting skeletal muscle relaxants, the benzoxazocines. Analgesic; antidepressant.
Human Drugs -> EU pediatric investigation plans
Computed Properties
Molecular Weight:289.8
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:2
Rotatable Bond Count:1
Exact Mass:289.1233420
Monoisotopic Mass:289.1233420
Topological Polar Surface Area:12.5
Heavy Atom Count:20
Complexity:274
Undefined Atom Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes
Drug Function and Efficacy
This product is a new type of non-narcotic analgesic, with mild antipyretic and muscle relaxant effects. It is effective for moderate and severe pain. An intramuscular injection of 20 mg of this product is equivalent to the effect of 12 mg of morphine. It has a mild respiratory depressant effect. It has no depressant effect on the circulatory system. There is no tolerance and dependence.
Registered Holders
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ARENE LIFE SCIENCES PRIVATE LTD
Active
United States
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PMC ISOCHEM
Active
France
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Jiangsu Hengfeng Pharmaceutical Co., Ltd.
Active
China
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