6-Chlor-2,3,4,5-tetrahydro-7,8-dihydroxy-1-(p-hydroxyphenyl)-1H-3-benzazepiniummethansulfonat

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H317：Kann allergische Hautreaktionen verursachen.

  H319：Verursacht schwere Augenreizung.

• 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.

Fenoldopam mesylate Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  Fenoldopam, first approved in the Netherlands in 1992, ended by reaching its first market, the US, for the short-term management of severe hypertension, including malignant hypertension, in the hospital setting. Fenoldopam can be prepared in 3 steps from the corresponding phenethylamine and aryloxiran, the pivotal step being the cyclisation in benzazepine in acidic medium. Fenoldopam is a potent dopamine D1 receptor agonist acting peripherally to produce systemic vasodilation.As it does not cross the bloodbrain barrier, it does not exert significant central dopaminergic activity. Fenoldopam also interacts significantly with 5HT1c and 5HT2 receptors. In comparative trials with the most common drug used for this condition in Europe, Fenoldopam was found to be appreciably more potent than nifedipine. Furthermore, Fenoldopam is fast acting and maintains a long-lasting antihypertensive effect.

• Beschreibung

  Fenoldopam is an agonist of dopamine D_1A (D1R) and D_1B (D5R) receptors (K_ds = 17 and 11 nM, respectively). Fenoldopam is used to study the roles of these receptors, in cells and in vivo, and to alter hemodynamic properties, including hypertension, in animals.

• Chemische Eigenschaften

  White to Off-White Solid

• Originator

  SmithKline Beecham (US)

• Verwenden

  Fenoldopam mesylate may be used to study dopamine D₁-mediated cell signaling.

• Verwenden

  antihypertensive, dopamine agonist

• Verwenden

  Dopamine D1-receptor agonist. Antihypertensive.

• Definition

  ChEBI: Fenoldopam mesylate is a benzazepine.

• Manufacturing Process

  2-Chloro-3,4-dimethoxyphenethylamine (1.0 g) was reacted with 0.70 g of pmethoxystyrene oxide to give the hydroxyphenethylamine; m.p. 118.5-121°C. This compound (2.16 g) was stirred at room temperature in 15 ml of trifluoroacetic acid with 4 drops of conc. sulfuric acid. After purification over a silica gel column with chloroform, 10% methanol/chloroform as eluates, was obtained 6-chloro-7,8-dimethoxy-1-p-methoxyphenyl-2,3,4,5-tetrahydro-1H- 3-benzazepine (0.78 g), m.p. 143-145°C.
  The trimethoxy product (0.87 g, 2.50 mmoles) in 25 ml of dry methylene chloride was cooled in an ice-methanol bath and 12.5 ml (25.0 mmoles) of boron tribromide in methylene chloride was added dropwise. After stirring for 4 hours, the mixture was cooled in an ice bath while methanol was carefully added to give 0.37 g of 6-chloro-7,8-dihydroxy-1-p-hydroxyphenyl-2,3,4,5- tetrahydro-1H-3-benzazepine hydrobromide, m.p. 215°C.
  The base was regenerated from the hydrobromide salt using sodium carbonate solution in 85% yield. Treating the base with various acids gave the following salts: dl-tartrate, fumarate, hydrochloride, sulfate, and the most water soluble one, the methanesulfonate, m.p. 272°C.

• Trademarks

  Corlopam (Hospira).

• Therapeutic Function

  Antihypertensive

• Biochem/physiol Actions

  Fenoldopam mesylate (FM) is considered as an effective therapeutic agent to prevent the onset of postoperative AKI (PO-AKI). In healthy cats, FM can stimulate diuresis and be well-tolerated. This benzazepine-derivative is regional specific and does not cause cerebral vasodilation.

Fenoldopam mesylate Upstream-Materialien And Downstream Produkte

6-Chlor-2,3,4,5-tetrahydro-7,8-dihydroxy-1-(p-hydroxyphenyl)-1H-3-benzazepiniummethansulfonat Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(138)Suppliers

67227-57-0, Fenoldopam mesylate Verwandte Suche: