[R-(R*,R*)]-2-[2-[1-(p-Chlorphenyl)-1-phenylethoxy]ethyl]-1-methylpyrrolidiniumhydrogenfumarat

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

• Sicherheit

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

Clemastine fumarate Chemische Eigenschaften,Einsatz,Produktion Methoden

• Chemische Eigenschaften

  White Solid

• Originator

  Tavegyl,Sandoz,France,1967

• Verwenden

  anti-inflammatory

• Verwenden

  Clemastine fumarate is a selective histamine H1 receptor antagonist (Ki = 0.26 nM) that also displays high affinity for muscarinic receptors (Ki = 16 nM). It has also recently been identified as a positive allosteric modulator of P2X7 receptor signaling. Clemastine fumarate has long been used to inhibit histamine-induced bronchoconstriction in asthma and airway hyperresponsive studies.

• Verwenden

  H1 Histamine receptor antagonist. Antihistaminic.

• Definition

  ChEBI: The fumaric acid salt of clemastine. An antihistamine with antimuscarinic and moderate sedative properties, it is used for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin condi ions.

• Manufacturing Process

  9.9 g of α-methyl-p-chlorobenzhydrol are added to a suspension of 2.3 g of powdered sodamide in 30 cc of benzene. Subsequently 7.4 g of Nmethylpyrrolidyl-(2)-ethyl chloride are added and the solution is heated to the boil at reflux for 20 hours. Then shaking is first effected with water and then 4 times each time with 25 cc of 2 N hydrochloric acid. The acid extracts are made alkaline with potassium hydroxide solution while cooling strongly, and the precipitated oil is extracted with ether. After drying of the ethereal solution over potassium carbonate, the solvent is evaporated and the residue is fractionally distilled in a high vacuum, whereby N-methyl-2-[2'-(α-methyl-pchlorobenzhydryloxy)-ethyl]-pyrrolidine boils over at 154°C/0.02 mm Hg. The base is converted to the fumarate by reaction with fumaric acid.

• Trademarks

  Tavist (Novartis).

• Therapeutic Function

  Antihistaminic

• Allgemeine Beschreibung

  Dextrorotatory clemastine, R,R-2[2[1-(4-chlorophenyl)-1-phenylethoxy]ethyl]-1- methylpyrrolidine hydrogen furnarate (1:1) (Tavist), has two chiral centers, each of which has the (R) absolute configuration. A comparison of the activities of the enantiomers indicates that the asymmetric center close to the terminal side chain nitrogen is of lesser importance to antihistaminic activity.
  ? This member of the ethanolamine series is characterized by a long duration of action, with an activity that reaches a maximum in 5 to 7 hours and persists for 10 to 12 hours. It is well absorbed when administered orally, and it is excreted primarily in the urine. The side effects are those usually encountered with this series of antihistamines. Clemastine is closely related to chlorphenoxamine, which is used for its central cholinergic-blocking activity. Therefore, it is not surprising that clemastine has significant antimuscarinic activity.

• Biologische Aktivität

  H 1 -receptor antagonist. Clinically-used antihistamine.

• Biochem/physiol Actions

  Clemastine fumarate is an antihistamine H1-antagonist and anticholinergic that also has antipruritic activity.

• Veterinary Drugs and Treatments

  Clemastine may be used for symptomatic relief of histamine1-related allergic conditions.

• Lager

  Store at RT

Clemastine fumarate Upstream-Materialien And Downstream Produkte

[R-(R*,R*)]-2-[2-[1-(p-Chlorphenyl)-1-phenylethoxy]ethyl]-1-methylpyrrolidiniumhydrogenfumarat Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(321)Suppliers

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