1-(4-Amino-6,7-dimethoxy-2-chinazolinyl)-4-(2-furoyl)piperazinmonohydrochlorid

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

  H361：Kann vermutlich die Fruchtbarkeit beeinträchtigen oder das Kind im Mutterleib schädigen.

• Sicherheit

  P201：Vor Gebrauch besondere Anweisungen einholen.

  P302+P352：BEI BERÜHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckmäßig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.

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

  P308+P313：BEI Exposition oder falls betroffen: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

Prazosin hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

• R-Sätze Betriebsanweisung:

  R22:Gesundheitsschädlich beim Verschlucken.
  R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
  R62:Kann möglicherweise die Fortpflanzungsfähigkeit beeinträchtigen.

• S-Sätze Betriebsanweisung:

  S28:Bei Berührung mit der Haut sofort abwaschen mit viel . . . (vom Hersteller anzugeben).
  S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.

• Chemische Eigenschaften

  Off-White to Yellow Powder

• Originator

  Hypovase, Pfizer, UK,1974

• Verwenden

  Prazosin Hydrochloride (Terazosin EP Impurity K) is an antihypertensive. α1-Adrenergic blocker.

• Verwenden

  Prazosin hydrochloride has been used:
  
  • to block the α1adrenergic receptors that mediate sympathetic vasoconstriction in mice
  • as an α1-adrenoceptor blocker,administered intragastrically in rats
  • as a vasodilator,administered together with inuslin into the left ventricle of mice for the assessment of its effects on renal functions
  
  

• Manufacturing Process

  Preparation of 2-Chloro-4-Amino-6,7-Dimethoxyquinazoline: To 800 ml of a solution of anhydrous ammonia in tetrahydrofuran at room temperature is added 30 g of 2,4-dichloro-6,7-dimethoxyquinazoline [F.H.S. Curd et al., J. Chem. Soc., p 1759 (1948)]. The mixture is stirred for 44 hours. The precipitate (29 g, MP 267° to 268°C) is filtered and recrystallized from methanol to yield 19 g of 2-chloro-4-amino-6,7-dimethoxyquinazoline, MP 302°C (dec.).
  Preparation of 2-(1-Piperazinyl)-4-Amino-6,7-Dimethoxyquinazoline: To 5 g of 2-chloro-4-amino-6,7-dimethoxyquinazoline, is added 20 g of a 25% solution of piperazine in ethanol. The mixture is heated at 160°C for 16 hours in a pressure bottle. The solvent is then evaporated and the residue is recrystallized from methanol/water.
  Preparation of 2[4-(2-Furoyl)-Piperazinyl]-4-Amino-6,7-Dimethoxyquinazoline: To 0.10 mol 2-(1-piperazinyl)-4-amino-6,7-dimethoxyquinazoline in 300 ml methanol is added with vigorous stirring, 0.10 mol 2-furoyl chloride. After addition is complete, the mixture is stirred for 3 hours at room temperature. The solids are filtered to give the desired product, MP 278° to 280°C.

• Trademarks

  Minipress (Pfizer).

• Therapeutic Function

  Antihypertensive

• Allgemeine Beschreibung

  The antihypertensive effectsof prazosin hydrochloride, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-furoyl)piperazine monohydrochloride(Minipress), are caused by peripheral vasodilation as a resultof its blockade of 1-adrenergic receptors. In ligand-bindingstudies, prazosin hydrochloride has 5,000-fold greater affinityfor α1-receptors than for some α2-adrenergic receptors.

• Biologische Aktivität

  α 1 and α 2B -adrenoceptor antagonist. Also a potent antagonist at the melatonin MT 3 receptor (K i = 10.2 nM). Also available as part of the α 1 -Adrenoceptor Tocriset™ and Mixed Adrenergic Tocriset™ .

• Biochem/physiol Actions

  Peripheral α1-adrenoceptor antagonist; vasodilator. Prazosin can be used to treat chronic posttraumatic stress disorder (PTSD). It plays a role in reducing blood pressure by relaxing blood vessels, hence used in the treatment of high blood pressure.

• Clinical Use

  Prazosin hydrochloride is readily absorbed, and plasmaconcentrations reach a peak about 3 hours after administration.Plasma half-life is between 2 and 3 hours. Prazosin hydrochlorideis highly bound to plasma protein; it does notcause adverse reactions, however, with drugs that might bedisplaced from their protein-binding sites (e.g., cardiac glycosides).It may cause severe orthostatic hypertension becauseof its -adrenergic blocking action, which preventsthe reflex venous constriction that is activated when an individualsits up from a prone position.

• Lager

  Room temperature

• läuterung methode

  The salt is recrystallised by dissolving it in hot MeOH, adding a small volume of MeOH/HCl (dry MeOH saturated with dry HCl gas) followed by dry Et2O until crystallisation is complete. Dry it in vacuo over solid KOH till the odour of HCl is absent. It has been recrystallised from hot H2O, the crystals are washed with H2O, and the H2O is removed azeotropically with CH2Cl2, and dried in a vacuum. [NMR and IR: Honkanen et al. J Heterocycl Chem 17 797 1980, cf Armarego & Reece Aust J Chem 34 1561 1981.] It is an antihypertensive drug and is an 1-adrenergic antagonist [Brosman et al. Proc Natl Acad Sci USA 82 5915 1985].

Prazosin hydrochloride Upstream-Materialien And Downstream Produkte

1-(4-Amino-6,7-dimethoxy-2-chinazolinyl)-4-(2-furoyl)piperazinmonohydrochlorid Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global(321)Suppliers

19237-84-4, Prazosin hydrochloride Verwandte Suche: