| CAS |
77883-43-3 |
| Chinese Name |
甲磺酸多沙唑嗪 |
| English Name |
Doxazosin |
| Synonyms |
UK 33274 mesylate |
| Molecular Formula |
C24H29N5O8S |
| Molecular Weight |
547.58 |
| Solubility |
Soluble in DMSO |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 1308068-626-2 |
| MDL |
MFCD00216023 |
| SMILES |
O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)C4OC5=CC=CC=C5OC4.CS(=O)(O)=O |
| InChIKey |
VJECBOKJABCYMF-UHFFFAOYSA-N |
| InChI |
InChI=1S/C23H25N5O5.CH4O3S/c1-30-18-11-14-15(12-19(18)31-2)25-23(26-21(14)24)28-9-7-27(8-10-28)22(29)20-13-32-16-5-3-4-6-17(16)33-20;1-5(2,3)4/h3-6,11-12,20H,7-10,13H2,1-2H3,(H2,24,25,26);1H3,(H,2,3,4) |
| PubChem CID |
62978 |
| Target Point |
Adrenergic Receptor |
| Passage |
Endocrinology & Hormones;GPCR & G Protein;Neuronal Signaling |
| Background |
It selectively antagonizes postsynaptic α1 adrenergic receptors. |
| Biological Activity |
Doxazosin mesylate (UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic聽伪1-adrenergic receptors. |
| IC50 |
α adrenergic receptor |
| In Vitro |
UK 33274 mesylate is the mesylate salt form of doxazosin， which is a long-lasting inhibitor of α1-adrenoceptors that is widely used to treat benign prostatic hyperplasia and lower urinary tract symptoms[1]. doxazosin may have a direct inhibitory effect on cholesterol synthesis independent of the LDL receptor. The inhibition of cholesterol synthesis by doxazosin may cause cells to compensate by upregulating the LDL receptor， thereby increasing the importation of lipoprotein cholesterol and reducing LDL cholesterol in the medium[2]. Doxazosin monotherapy was effective in eight of 12 patients (66.7%)， and combined therapy with a beta-blocker was effective in 11 of 12 patients (91.7%). The mean pulse rate remained constant throughout therapy. Adverse reactions were minor and transient and occurred in only three patients. Urinary and plasma catecholamine levels tended to decrease or remained unchanged during doxazosin therapy[3]. |
| Data Literature Source |
[1]. Sun，J.A.，et al.，Stereoselective binding of doxazosin enantiomers to plasma proteins from rats，dogs and humans in vitro. Acta Pharmacol Sin，2013. 34(12): p. 1568-74.
[2]. D'Eletto，R.D. and N.B. Javitt，Effect of doxazosin on cholesterol synthesis in cell culture. J Cardiovasc Pharmacol，1989. 13 Suppl 2: p. S1-4; discussion S4.
[3]. Miura，Y. and K. Yoshinaga，Doxazosin: a newly developed，selective alpha 1-inhibitor in the management of patients with pheochromocytoma. Am Heart J，1988. 116(6 Pt 2): p. 1785-9. |
| Unit |
Bottle |
| Specification |
100mg 500mg 1g |
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