Quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors
CAS：74191-85-8
分子式：C23H25N5O5
分子量：451.48
纯度：98%
存储：Store at -20°C

Background:

Doxazosin (UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.

Doxazosin(UK 33274) 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].

参考文献:
[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.