Introduction：Basic information about Orphenadrine citrate CAS 4682-36-4, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Orphenadrine citrate Basic information
| Product Name: | Orphenadrine citrate |
| Synonyms: | beta-dimethylaminoethyl 2-methylbenzhydryl ether citrate;BETA-DIMETHYLAMINOETHYL 2-METHYLBENZHYDRYL ETHER CITRATE SALT;o-methyldiphenhydramine citrate;ORPHENADRINE CITRATE SALT;orphenadrine dihydrogen citrate;Banflex;N,N-Dimethyl-2-[(2-methylphenyl)phenylmethoxy]ethanamine Citrate Salt;X-Ota |
| CAS: | 4682-36-4 |
| MF: | C24H31NO8 |
| MW: | 461.5 |
| EINECS: | 225-137-5 |
| Product Categories: | Relieve pain of the local muscle spasmodic auxiliary drug use;API;APIs;Inhibitors;NORFLEX;Intermediates & Fine Chemicals;Pharmaceuticals;Amines;Aromatics |
| Mol File: | 4682-36-4.mol |
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Orphenadrine citrate Chemical Properties
| Melting point | 132-1340C |
| storage temp. | Sealed in dry,2-8°C |
| solubility | Sparingly soluble in water, slightly soluble in ethanol (96 per cent). |
| form | Solid |
| color | White to Pale Beige |
| Major Application | forensics and toxicology
pharmaceutical (small molecule) |
| InChIKey | ASDBZPGDZBFZAH-UHFFFAOYSA-N |
| SMILES | OC(=O)CC(CC(O)=O)C(O)=O.CN(C)CCOC(c1ccccc1)c2ccccc2C |
| CAS DataBase Reference | 4682-36-4(CAS DataBase Reference) |
Safety Information
| Hazard Codes | Xn,Xi |
| Risk Statements | 22-40-20/21/22 |
| Safety Statements | 22-36-62-38-36/37/39-28-26-24/25 |
| RIDADR | 3249 |
| WGK Germany | 3 |
| HazardClass | 6.1(b) |
| PackingGroup | III |
| HS Code | 2922190900 |
| Storage Class | 6.1C - Combustible acute toxic Cat.3
toxic compounds or compounds which causing chronic effects |
| Hazard Classifications | Acute Tox. 3 Oral |
Orphenadrine citrate Usage And Synthesis
| Chemical Properties | White Solid |
| Originator | Norflex,Riker,US,1959 |
| Uses | Muscle relaxant (skeletal); antihistaminic |
| Uses | skeletal muscle relaxant, antihistaminic agent |
| Uses | A histaminergic compound |
| Definition | ChEBI: A citrate salt which comprises equimolar amounts of orphenadrine and citric acid. |
| Manufacturing Process | As described in US Patent 2,567,351, o-methylbenzhydryl bromide is added slowly to β-dimethylaminoethanol at refluxing temperature. After the addition has been completed the mixture is refluxed and stirred for an additional 16 hours. The mixture is cooled and the bottom layer consisting of the crude hydrobromide salt of β-dimethylaminoethanol is drawn off. The excess amino alcohol is distilled from the upper layer in vacuo and the residue is reacted with citric acid. |
| Brand name | Norflex (3M Pharmaceuticals). |
| Therapeutic Function | Muscle relaxant |
| General Description | Orphenadrine citrate, N,Ndimethyl-2-(o-methyl-α-phenylbenzyloxy)ethylamine citrate(1:1) (Norflex), introduced in 1957, is closely related todiphenhydramine structurally but has much lower antihistaminicactivity and much higher anticholinergic action.Likewise, it lacks the sedative effects characteristic ofdiphenhydramine. Pharmacological testing indicates that itis not primarily a peripherally acting anticholinergic becauseit has only weak effects on smooth muscle, on the eye,and on secretory glands. It does reduce voluntary musclespasm, however, by a central inhibitory action on cerebralmotor areas, a central effect similar to that of atropine. |
| Biological Activity | Muscarinic receptor antagonist; H1 histamine receptor antagonist; muscle relaxant. Orphenadrine has also been reported to inhibit the noradrenergic transporter and to block the NMDA receptor ion channel. |
| Clinical Use | Orphenadrine citrate is used for the symptomatic treatment ofParkinson disease. It relieves rigidity better than it doestremor, and in certain cases, it may accentuate the latter. Thedrug combats mental sluggishness, akinesia, adynamia, andlack of mobility, but this effect seems to diminish rather rapidlywith prolonged use. It is best used as an adjunct to theother agents, such as benztropine, procyclidine, cycrimine,and trihexyphenidyl, in the treatment of paralysis agitans.Orphenadrine citrate is also used as an adjunct to rest, physiotherapy,and other measures to relieve pain of local musclespasm (e.g., nocturnal leg cramps).
The drug has a low incidence of the usual side effectsfor this group, namely, dryness of mouth, nausea, and mildexcitation. |
Orphenadrine citrate Preparation Products And Raw materials
