Doxazosin mesylate

Bezeichnung:Doxazosin mesylate

CAS-Nr77883-43-3

Englisch Name:Doxazosin mesylate

CBNumberCB3285710

SummenformelC24H29N5O8S

Molgewicht547.58

MOL-Datei77883-43-3.mol

Doxazosin mesylate physikalisch-chemischer Eigenschaften

Schmelzpunkt	275-277°C
storage temp.	2-8°C
Löslichkeit	Slightly soluble in water, soluble in a mixture of 15 volumes of water and 35 volumes of tetrahydrofuran, slightly soluble in methanol, practically insoluble in acetone. It shows polymorphism (5.9), some forms may be hygroscopic
Aggregatzustand	powder
Farbe	white
BCS Class	1
Stabilität	Protect from light
InChIKey	VJECBOKJABCYMF-UHFFFAOYSA-N
CAS Datenbank	77883-43-3(CAS DataBase Reference)

Sicherheit

Kennzeichnung gefährlicher	Xi
R-Sätze:	36/37/38
S-Sätze:	26-36/37-24/25
WGK Germany	2
RTECS-Nr.	TK8044000
HS Code	29349990
Giftige Stoffe Daten	77883-43-3(Hazardous Substances Data)

Gefahreninformationscode (GHS)

Doxazosin mesylate Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R36/37/38:Reizt die Augen, die Atmungsorgane und die Haut.
S-Sätze Betriebsanweisung:
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
Chemische Eigenschaften
White or almost white crystalline powder.
Originator
Alfadil,Roerig/Pfizer,Sweden
Verwenden
Doxazosin ER is indicated for the treatment of the signs and symptoms of benign prostatic hyperplasia
Verwenden
A selective α-1-adrenergicblocker related to prazosin.
Verwenden
antihypertensive
Verwenden
A selective a-1-adrenergicblocker related to prazosin
Verwenden
Doxazosin is a selective α1-adrenoceptor antagonist. Doxazosin relaxes smooth muscles of the prostate.
Manufacturing Process
4-Amino-2-chloro-6,7-dimethoxyquinazoline (140 g) and N-(1,4-benzodioxan- 2-carbonyl)piperazine (150 g) were stirred together under reflux in n-butanol (2 L) for 3.5 hours. The mixture was then cooled to 80°C, the solid product collected, washed with cold n-butanol (2 times 250 ml), and dried. The crude product was dissolved in hot (80°C) dimethylformamide (530 ml) and water (130 ml), filtered, concentrated in vacuo to about 300 ml, then cooled and ether (1.8 L) added. The solid so obtained was collected and washed with ether to give 4-amino-2-[4-(1,4-benzodioxan-2-carbonyl)piperazin-1-yl]-6,7- dimethoxyquinazoline hydrochloride (215 g), melting point 289°C-290°C. Mesylate may be prepared by usual method from hydrochloride with methylsulphonic acid.
Trademarks
Cardura (Pfizer).
Therapeutic Function
Adrenergic blocker
Biologische Aktivität
Selective α 1 -adrenoceptor antagonist (pK i values are 9.0, 8.5 and 8.4 for human α 1B , α 1A and α 1D receptors respectively). Displays antihypertensive activity.
Biochem/physiol Actions
α1-adrenoceptor antagonist; relaxes smooth muscles of the prostate
Lager
Desiccate at RT
Einzelnachweise
[1] zhao y1, cao xb, ren lm. doxazosin selectively potentiates contraction to serotonin via 5-ht₂a receptors in longitudinal muscle strips of the rabbit gastric body. can j physiol pharmacol. 2014 mar;92(3):197-204.
[2] o'neil ml1, beckwith le, kincaid cl, rasmussen dd. the α1-adrenergic receptor antagonist, doxazosin, reduces alcohol drinking in alcohol-preferring (p) rats. alcohol clin exp res. 2013 feb;37(2):202-12.
[3] tung d1, ciallella j, cheung ph, saha s. novel anti-inflammatory effects of doxazosin in rodent models of inflammation. pharmacology. 2013;91(1-2):29-34.

Doxazosin mesylate Upstream-Materialien And Downstream Produkte

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