Doxazosin mesylate

Chemical properties

White or almost white crystalline powder.

Originator

Alfadil,Roerig/Pfizer,Sweden

The Uses of Doxazosin mesylate

A selective a-1-adrenergicblocker related to prazosin

The Uses of Doxazosin mesylate

A selective α-1-adrenergicblocker related to prazosin.

The Uses of Doxazosin mesylate

antihypertensive

The Uses of Doxazosin mesylate

Doxazosin is a selective α1-adrenoceptor antagonist. Doxazosin relaxes smooth muscles of the prostate.

The Uses of Doxazosin mesylate

Doxazosin ER is indicated for the treatment of the signs and symptoms of benign prostatic hyperplasia

What are the applications of Application

Doxazosin Mesylate is an alpha-1-adrenoreceptor antagonist

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.

brand name

Cardura (Pfizer).

Therapeutic Function

Adrenergic blocker

Biological Activity

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

storage

Desiccate at RT

References

[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.