(5α)-17-Allyl-4,5-epoxy-3,14-dihydroxymorphinan-6-onhydrochlorid

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

  P304+P340：BEI EINATMEN: Die Person an die frische Luft bringen und für ungehinderte Atmung sorgen.

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

  P405：Unter Verschluss aufbewahren.

Naloxone hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.

• S-Sätze Betriebsanweisung:

  S22:Staub nicht einatmen.
  S24/25:Berührung mit den Augen und der Haut vermeiden.
  S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
  S36/37/39:Bei der Arbeit geeignete Schutzkleidung,Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.

• Beschreibung

  Naloxone (hydrochloride) (CRM) (Item No. ISO60191) is a certified reference material categorized as an opioid antagonist. Formulations containing naloxone have been used as antidotes for opioid overdose and the prevention of overdose. They have also been used in combination with buprenorphine (Item Nos. ISO60178 | 14025) in the treatment of opiate addiction and in pain management. This product is intended for research and forensic applications.

• Chemische Eigenschaften

  Crystalline Solid

• Originator

  Narcan,Du Pont,US,1971

• Verwenden

  A nonspecific opiate receptor antagonist that displays anitnociceptive effects

• Verwenden

  Opioate antidote;

• Verwenden

  Naloxone Hydrochloride is a specific opioid antagonist. Narcotic antagonist.

• Definition

  ChEBI: A hydrochloride resulting from the formal reaction of equimolar amounts of naloxone and hydrogen chloride. A specific opioid antagonist, it is used to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known r suspected opioid overdose.

• Manufacturing Process

  10 grams of 14-hydroxydihydromorphinone (oxymorphone) was converted into its diacetate by warming it on the steam bath with 80 cc of acetic anhydride for about 2 hours. The acetic anhydride was removed on the water bath under a vacuum of about 30 mm absolute pressure. The melting point of the residue was 220°C. The residue was taken up in 100 cc of chloroform. An equal amount by weight of cyanogen bromide was added and the mixture was refluxed at about 60°C for about 5 hours. After refluxing, the mixture was washed with 100 cc of a 5% aqueous hydrochloric acid solution, dried over sodium sulfate and the chloroform removed by evaporation under a vacuum of about 30 mm. The residue had a melting point of 240°C.
  The residue was then heated at about 90°C for 16 hours on a steam bath with 300 cc of 20% aqueous hydrochloric acid solution, and treated with a small amount, e.g., 1 gram of charcoal. The hydrochloric acid was then removed under a vacuum of 15 mm, the residue dissolved in 30 cc of water and precipitated by the addition of 2.4 cc of concentrated aqueous ammonia. The precipitate was filtered off and dried. It consists of 14- hydroxydihydronormorphinone. It is soluble in ethanol.
  The 14-hydroxydihydronormorphinone was suspended in 200 cc of pure ethyl alcohol, half its weight of sodium bicarbonate and half its weight of allyl bromide added and the resulting mixture was refluxed at about 75°C for 48 hours. The solution was cooled, e.g., to 10°C and filtered and the alcohol removed under a vacuum of 30 mm. The residue was dissolved in chloroform and filtered. The chloroform was removed under a vacuum of 30 mm and the residue was crystallized from ethylacetate. The crystallized product, N-allyl- 1,4-hydroxydihydronormorphinone, has a melting point of 184°C, is soluble in chloroform and insoluble in petroleum ether. The yield amounts to 20% based on the weight of the reacted 14-hydroxydihydromorphinone.

• Trademarks

  Narcan (Bristol-Myers Squibb); Narcan (Endo).

• Therapeutic Function

  Narcotic antagonist

• Biologische Aktivität

  Opioid antagonist.

• Veterinary Drugs and Treatments

  Naloxone is used in veterinary medicine almost exclusively for its opiate reversal effects, but the drug is being investigated for treating other conditions (e.g., septic, hypovolemic or cardiogenic shock). Naloxone may also be employed as a test drug to see if endogenous opiate blockade will result in diminished tail chasing or other self-mutilating behaviors. It, potentially, could be useful for treating overdoses of clonidine or the CNS effects of benzodiazepines (ivermectin?), but more research is necessary before recommending its use.

• Stoffwechsel

  Naloxone hydrochloride is rapidly metabolised in the liver, mainly by conjugation with glucuronic acid to naloxone-3-glucuronide, which is excreted in the urine

• Lager

  Room temperature

• Einzelnachweise

  1) Le Bourdonnec?et al., (2008),?Novel trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidines as mu opioid receptor antagonists with improved opioid receptor selectivity profiles: Bioorg. Med. Chem. Lett..?18?2006 2) Boyer?et al.?(2012),?Management of opioid analgesic overdose; New Engl. J. Med.?367?146 3) Wang?et al.?(2017),?Opioids and opioid receptors orchestrate wound repair;?Transl. Res.?185?13 4) Wright and Rodgers (2013),?Low dose naloxone attenuates the pruritic but not anorectic response to rimonabant in male rats; Psychopharmacology (Berl.)?226?415

Naloxone hydrochloride Upstream-Materialien And Downstream Produkte

(5α)-17-Allyl-4,5-epoxy-3,14-dihydroxymorphinan-6-onhydrochlorid Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(271)Suppliers

357-08-4, Naloxone hydrochloride Verwandte Suche: