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Chemical Compound Review

Diblocin     [4-(4-amino-6,7-dimethoxy- quinazolin-2...

Synonyms: Alfadil, Normothen, Supressin, doxazosin, Doxazosina, ...
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Disease relevance of doxazosin

  • Furthermore, the inhibitory effects of a low dose of TCV-116 on cardiac hypertrophy and altered gene expressions of TGR(mRen2)27 were greater than those of doxazosin (alpha 1-adrenergic receptor blocker) combined with atenolol, despite their similar hypotensive effects [1].
  • Recent evidence from our laboratory has demonstrated that alpha1-adrenoceptor antagonists doxazosin and terazosin induced apoptosis in prostate epithelial and smooth muscle cells in patients with benign prostatic hypertrophy (BPH; J. Urol., 159: 1810-1815, 1998; J. Urol., 161: 2002-2007, 1999) [2].
  • These findings provide the first evidence that the apoptotic activity of the quinazoline-based alpha1-adrenoceptor antagonists (doxazosin and terazosin) against prostate cancer cells is independent of: (a) their capacity to antagonize alpha1-adrenoceptors; and (b) the hormone sensitivity status of the cells [3].
  • Furthermore, an in vivo efficacy trial demonstrated that doxazosin administration (at tolerated pharmacologically relevant doses) in SCID mice bearing PC-3 prostate cancer xenografts resulted in a significant inhibition of tumor growth [2].
  • Doxazosin, an alpha 1-adrenergic inhibitor, has been shown to decrease hypertension and plasma lipids, especially total cholesterol (TC) and low-density lipoprotein cholesterol (LDL-C), thus reducing certain risk factors associated with increased incidence of cardiovascular disease [4].

Psychiatry related information on doxazosin


High impact information on doxazosin

  • Heterogeneity was significant between trials because of high risk of cardiovascular events on doxazosin in one trial, and high risk of stroke on captopril in another; but systolic pressure differed between groups in these two trials by 2-3 mm Hg [10].
  • We randomized 11-week-old LVH rats to chronic treatment with the endothelin receptor antagonist bosentan (Bos, 100 mg. kg-1. d-1, n=14), the alpha1-receptor antagonist doxazosin (Dox, 1 mg. kg-1. d-1, n=12), or vehicle (Cont, n=14) [11].
  • Bos (93%; P<0.0001 versus Cont) but not Dox (42%; P=0.8465 versus Cont) ameliorated the survival rate at 17 weeks (Cont; 36%) [11].
  • The single intra-arterial infusion of yohimbine, as well as doxazosin, resulted in vasodilation [12].
  • The effect of doxazosin on recruitment of Fas-associated death domain (FADD) and procaspase-8 to the Fas receptor was examined via analysis of death-inducing signaling complex formation [13].

Chemical compound and disease context of doxazosin


Biological context of doxazosin


Anatomical context of doxazosin


Associations of doxazosin with other chemical compounds

  • In this study, to identify the precise molecular mechanism underlying this apoptosis induction, we examined whether doxazosin and terazosin (both piperazinyl quinazolines) affect prostate growth via an alpha1-adrenoceptor-independent action [3].
  • Mean arterial blood pressure (114 +/- 2 mmHg) was similar in all groups before initiating antihypertensive therapy and declined to 102 +/- 2 (captopril), 103 +/- 1 (nifedipine), and 103 +/- 2 (doxazosin) mmHg (P < 0.001) [25].
  • There were no significant differences in HDL apolipoprotein (apo) A-I or low-density lipoprotein apoB between the drugs, but atenolol decreased the ratio of HDL-C to apoA-I, and doxazosin increased this ratio, differences that were statistically significant (P < .002) [26].
  • Enalapril (128 +/- 1 mmHg) and doxazosin (132 +/- 2 mmHg) decreased mean blood pressure compared with control levels (148 +/- 1 mmHg) (P < .01) [27].
  • In contrast, despite a hypotensive effect comparable to these two drug treatments, doxazosin (an alpha 1-blocker) alone or manidipine (a calcium antagonist) did not normalize these altered gene expressions of SHR [28].

Gene context of doxazosin


Analytical, diagnostic and therapeutic context of doxazosin

  • Quantitative microarray assays were done in PC-3 and BPH-1 cells after treatment with doxazosin (25 micromol/L, 6 and 24 hours) to identify the early gene changes [13].
  • Western blot analysis revealed activation of caspase-8 and caspase-3 within the first 6 to 12 hours of treatment with doxazosin in both PC-3 and BPH-1 cells [13].
  • Plasma glucose, insulin, and free fatty acid (FFA) concentrations during the OGTT were similar in all groups before antihypertensive treatment and did not change with captopril and nifedipine; after doxazosin, plasma glucose and FFA concentrations during the OGTT decreased (both P < 0.05) without change in plasma insulin response [25].
  • The antihypertensive efficacy and pharmacokinetics of a single 1 mg oral dose of doxazosin were investigated in five healthy male volunteers, six patients with renal failure not on hemodialysis, and four patients with end-stage renal failure studied between two hemodialyses [32].
  • Both doxazosin and yohimbine caused an increased vasodilatory effect in the sodium-depleted versus the control group (228 +/- 42 versus 83 +/- 13% and 192 +/- 24 versus 95 +/- 8%, respectively; P < 0.05) [33].


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  2. Suppression of human prostate cancer cell growth by alpha1-adrenoceptor antagonists doxazosin and terazosin via induction of apoptosis. Kyprianou, N., Benning, C.M. Cancer Res. (2000) [Pubmed]
  3. Quinazoline-derived alpha1-adrenoceptor antagonists induce prostate cancer cell apoptosis via an alpha1-adrenoceptor-independent action. Benning, C.M., Kyprianou, N. Cancer Res. (2002) [Pubmed]
  4. Dose-related effects of doxazosin on plasma lipids and aortic fatty streak formation in the hypercholesterolemic hamster model. Foxall, T.L., Shwaery, G.T., Stucchi, A.F., Nicolosi, R.J., Wong, S.S. Am. J. Pathol. (1992) [Pubmed]
  5. Effect of doxazosin with and without rho-kinase inhibitor on human corpus cavernosum smooth muscle in the presence of bladder outlet obstruction. Demir, O., Murat, N., Aslan, G., Gidener, S., Esen, A.A. J. Urol. (2006) [Pubmed]
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  11. Cardiac endothelin-1 plays a critical role in the functional deterioration of left ventricles during the transition from compensatory hypertrophy to congestive heart failure in salt-sensitive hypertensive rats. Iwanaga, Y., Kihara, Y., Hasegawa, K., Inagaki, K., Yoneda, T., Kaburagi, S., Araki, M., Sasayama, S. Circulation (1998) [Pubmed]
  12. Identification of vascular postsynaptic alpha 1- and alpha 2-adrenoceptors in man. Jie, K., van Brummelen, P., Vermey, P., Timmermans, P.B., van Zwieten, P.A. Circ. Res. (1984) [Pubmed]
  13. Doxazosin induces apoptosis of benign and malignant prostate cells via a death receptor-mediated pathway. Garrison, J.B., Kyprianou, N. Cancer Res. (2006) [Pubmed]
  14. Doxazosin and captopril in mildly hypercholesterolemic hypertensive patients. The Doxazosin-Captopril in Hypercholesterolemic Hypertensives Study. Ferrara, L.A., Di Marino, L., Russo, O., Marotta, T., Mancini, M. Hypertension (1993) [Pubmed]
  15. Alpha-blockade and calcium antagonism: an effective and well-tolerated combination for the treatment of resistant hypertension. Brown, M.J., Dickerson, J.E. J. Hypertens. (1995) [Pubmed]
  16. Platelet alpha2-adrenoceptor alterations in patients with essential hypertension are normalized after treatment with doxazosin but not propranolol. Portaluppi, F., Manfredini, R., Varani, K., Gessi, S., Caiazza, A., Borea, P.A. J. Hypertens. (2000) [Pubmed]
  17. Combination treatment with propiverine hydrochloride plus doxazosin controlled release gastrointestinal therapeutic system formulation for overactive bladder and coexisting benign prostatic obstruction: a prospective, randomized, controlled multicenter study. Lee, K.S., Choo, M.S., Kim, D.Y., Kim, J.C., Kim, H.J., Min, K.S., Lee, J.B., Jeong, H.J., Lee, T., Park, W.H. J. Urol. (2005) [Pubmed]
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  19. Alpha1-adrenergic receptor antagonists: novel therapy for pituitary adenomas. Fernando, M.A., Heaney, A.P. Mol. Endocrinol. (2005) [Pubmed]
  20. Maspin sensitizes prostate cancer cells to doxazosin-induced apoptosis. Tahmatzopoulos, A., Sheng, S., Kyprianou, N. Oncogene (2005) [Pubmed]
  21. Doxazosin inhibits retinoblastoma protein phosphorylation and G(1)-->S transition in human coronary smooth muscle cells. Kintscher, U., Wakino, S., Kim, S., Jackson, S.M., Fleck, E., Hsueh, W.A., Law, R.E. Arterioscler. Thromb. Vasc. Biol. (2000) [Pubmed]
  22. Role of alpha 1- and alpha 2-adrenergic receptors in the human hypertensive kidney. de Leeuw, P.W., van Es, P.N., de Bos, R., Birkenhäger, W.H. Hypertension (1987) [Pubmed]
  23. Alteration of response to neuropeptide Y in the nucleus tractus solitarius of spontaneously hypertensive rats. Takesako, T., Takeda, K., Kuwahara, T., Takenaka, K., Tanaka, M., Itoh, H., Nakata, T., Sasaki, S., Nakagawa, M. Hypertension (1994) [Pubmed]
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  26. Lipids and lipoproteins during antihypertensive drug therapy. Comparison of doxazosin and atenolol in a randomized, double-blind trial: the Alpha Beta Canada Study. Rabkin, S.W., Huff, M.W., Newman, C., Sim, D., Carruthers, S.G. Hypertension (1994) [Pubmed]
  27. Kinins contribute to the improvement of insulin sensitivity during treatment with angiotensin converting enzyme inhibitor. Tomiyama, H., Kushiro, T., Abeta, H., Ishii, T., Takahashi, A., Furukawa, L., Asagami, T., Hino, T., Saito, F., Otsuka, Y. Hypertension (1994) [Pubmed]
  28. Role of angiotensin-converting enzyme, adrenergic receptors, and blood pressure in cardiac gene expression of spontaneously hypertensive rats during development. Ohta, K., Kim, S., Iwao, H. Hypertension (1996) [Pubmed]
  29. The role of the {alpha}-1 adrenoceptor in modulating human mesangial cell matrix production. Pawluczyk, I.Z., Patel, S.R., Harris, K.P. Nephrol. Dial. Transplant. (2006) [Pubmed]
  30. Doxazosin induces apoptosis in LNCaP prostate cancer cell line through DNA binding and DNA-dependent protein kinase down-regulation. Arencibia, J.M., Del Rio, M., Bonnin, A., Lopes, R., Lemoine, N.R., López-Barahona, M. Int. J. Oncol. (2005) [Pubmed]
  31. alpha1-Adrenergic receptor antagonists induce production of IL-18 and expression of ICAM-1 and CD40 in human monocytes. Takahashi, H.K., Iwagaki, H., Tamura, R., Katsuno, G., Xue, D., Sugita, S., Mori, S., Yoshino, T., Tanaka, N., Nishibori, M. J. Immunother. (2005) [Pubmed]
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  33. Effects of sodium depletion on the role of AT1- and alpha-adrenergic receptors in the regulation of forearm vascular tone in humans. Baan, J., Chang, P.C., Vermeij, P., Pfaffendorf, M., van Zwieten, P.A. J. Hypertens. (1999) [Pubmed]
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