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Chemical Compound Review

Bunazosin     1-[4-(4-amino-6,7-dimethoxy- quinazolin-2...

Synonyms: Bunazosina, Bunazosine, bunazocine, Bunazosinum, SureCN49348, ...
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Disease relevance of Bunazosin


High impact information on Bunazosin

  • The voltage-dependent block and use-dependent block of the maximal rate of rise (Vmax) of action potentials by bunazosin (10(-5) to 10(-4) M) and yohimbine (10(-6) to 10(-5) M) were studied [1].
  • The analysis of the onset and recovery kinetics from the use-dependent block of drugs showed that both bunazosin and yohimbine act as slow kinetic drugs [1].
  • Although addition of bunazosin to L-NAME restored systolic blood pressure to the control level, PAC and AT1-R numbers remained significantly higher than those of control level [6].
  • Topically instilled bunazosin at 0.01% partly inhibited both of these vasoconstrictions on the ipsilateral side, but not on the contralateral side [7].
  • Sodium nitroprusside, but not timolol or bunazosin, also significantly prevented the NMDA-induced reduction of cell numbers in the GCL and IPL thickness [8].

Chemical compound and disease context of Bunazosin


Biological context of Bunazosin


Anatomical context of Bunazosin

  • Pretreatment with intracoronary bunazosin, an alpha 1 adrenoceptor antagonist (100 micrograms), showed no protective effect on narrowing of the epicardial major coronary artery or blood flow delay [17].
  • The myosin isoenzyme pattern of the left ventricle was significantly shifted toward VM-1 in the bunazosin treated SHR, the VM-1 concentration in the treated group being 38% greater than in the untreated group [2].
  • There was a similarity in the potency and rank order of seven alpha 1, adrenoceptor antagonists for the inhibition of [3H] bunazosin and [3H]prazosin binding in human prostates [15].
  • In the hippocampus, prazosin and bunazosin produced biphasic displacement of [3H]YM617, but not [3H]prazosin binding [18].
  • The results suggest that bunazosin protects the myocardium against ischemic damage [19].

Associations of Bunazosin with other chemical compounds


Gene context of Bunazosin

  • Insulin insensitivity in nonobese, nondiabetic essential hypertension and its improvement by an alpha 1-blocker (bunazosin) [24].
  • Serum total cholesterol level decreased and HDL cholesterol increased significantly after treatment with bunazosin [24].
  • Bunazosin HCl significantly inhibited the expression of bFGF and TGFbeta1 mRNA in VSMCs from SHRs, but not in cells from WKY rats [25].
  • Bunazosin HCl significantly suppressed the response of DNA synthesis to PDGF-AA and EGF, but not to Ang II, in VSMCs from SHRs [25].
  • Phentolamine (an alpha blocker) or yohimbine (an alpha 2 blocker) administration completely inhibited the increase of glucagon secretion caused by epinephrine infusion, but neither the administration of bunazosin (an alpha 1 blocker) nor beta blockers inhibited it [26].

Analytical, diagnostic and therapeutic context of Bunazosin

  • In group 2 (n = 12), the alpha 1 blocker bunazosin (0.2, intravenously) blunted the shortening of the refractory period in the ischaemic zone induced by OMB ligation (p < 0.01), resulting in a reduction in refractory period dispersion between the ischaemic and non-ischaemic (border and normal) zones [27].
  • After a single-blind placebo run-in period lasting 4-6 weeks, the patients were treated either with bunazosin retard or with atenolol for a further 16 weeks including an initial dose titration period to achieve blood pressure control [20].
  • Forty-three anesthetized dogs were divided into three groups; the occlusion group (n = 7), the reperfusion group (n = 24), and a group treated with the alpha 1-adrenergic blocker, bunazosin (n = 12) [4].
  • 5-HT- and KCl-induced constrictions were not modified by a potent alpha 1-adrenoceptor antagonist, bunazosin [28].
  • The contractile response evoked by electrical stimulation at 4 Hz was abolished by tetrodotoxin (10(-7) M) and depressed to approximately 10% by bunazosin (10(-6) M), an alpha 1-antagonist [29].


  1. Antiarrhythmic effects of alpha-adrenoceptor antagonists in guinea pig ventricular myocardium. Hasegawa, J., Hirai, S., Saitoh, M., Kotake, H., Mashiba, H. J. Am. Coll. Cardiol. (1988) [Pubmed]
  2. Effects of long term treatment with an alpha 1 adrenoceptor blocker on cardiac hypertrophy, contractility, and myosin isoenzymes in spontaneously hypertensive rats. Takeda, N., Nakamura, I., Ohkubo, T., Iwai, T., Tanamura, A., Nagano, M. Cardiovasc. Res. (1991) [Pubmed]
  3. Sympatholytic effects of the intravenously injected alpha 1-adrenergic blocker, bunazosin, in anaesthetized rats. Takahashi, H., Okabayashi, H., Suga, K., Matsuzawa, M., Ikegaki, I., Yoshimura, M. J. Hypertens. (1987) [Pubmed]
  4. Biochemical basis for reperfusion arrhythmias. Sugiyama, S., Ozawa, T. J. Mol. Cell. Cardiol. (1987) [Pubmed]
  5. Renal haemodynamic effects of bunazosin retard and prazosin in mild to moderately hypertensive patients with normal or moderately impaired renal function. Anderton, J.L., Gill, M., Notghi, A. Nephrol. Dial. Transplant. (1994) [Pubmed]
  6. Regulation of angiotensin II receptor expression by nitric oxide in rat adrenal gland. Usui, M., Ichiki, T., Katoh, M., Egashira, K., Takeshita, A. Hypertension (1998) [Pubmed]
  7. Effects of topically instilled bunazosin, an alpha1-adrenoceptor antagonist, on constrictions induced by phenylephrine and ET-1 in rabbit retinal arteries. Ichikawa, M., Okada, Y., Asai, Y., Hara, H., Ishii, K., Araie, M. Invest. Ophthalmol. Vis. Sci. (2004) [Pubmed]
  8. Neuroprotective effect and intraocular penetration of nipradilol, a beta-blocker with nitric oxide donative action. Mizuno, K., Koide, T., Yoshimura, M., Araie, M. Invest. Ophthalmol. Vis. Sci. (2001) [Pubmed]
  9. A comparative study of the effects of alpha 1-adrenoceptor antagonists on sympathetic function in rats. Saito, H., Togashi, H., Yoshioka, M. Am. J. Hypertens. (1996) [Pubmed]
  10. Renal effects of bunazosin, a new alpha 1-adrenoceptor blocker, in patients with mild-to-moderate essential hypertension. Baba, T., Tomiyama, T., Murabayashi, S., Takebe, K. J. Cardiovasc. Pharmacol. (1990) [Pubmed]
  11. Efficacy of bunazosin hydrochloride 0.01% as adjunctive therapy of latanoprost or timolol. Kobayashi, H., Kobayashi, K., Okinami, S. Journal of glaucoma. (2004) [Pubmed]
  12. Antihypertensive efficacy and orthostatic tolerance of bunazosin vs nitrendipine: a multicentre double-blind randomized controlled study. Langenfeld, M.R., Bräutigam, M., Weidinger, G., Assmann, I., Krönig, B., Schmieder, R.E. Journal of human hypertension. (1996) [Pubmed]
  13. Selective suppression by bunazosin of alpha-adrenergic agonist evoked elevation of intraocular pressure in sympathectomized rabbit eyes. Nishimura, K., Kuwayama, Y., Matsugi, T., Sun, N., Shirasawa, E. Invest. Ophthalmol. Vis. Sci. (1993) [Pubmed]
  14. Do alpha-adrenergic receptors participate in control of the circadian rhythm of IOP? Kiuchi, Y., Yoshitomi, T., Gregory, D.S. Invest. Ophthalmol. Vis. Sci. (1992) [Pubmed]
  15. [3H]bunazosin, a novel selective radioligand of alpha 1 adrenoceptors in human prostates. Yamada, S., Suzuki, M., Matsuoka, Y., Kato, Y., Kimura, R., Maruyama, M., Kawabe, K. J. Urol. (1991) [Pubmed]
  16. Vascular alpha-1 antagonistic and agonistic effects of beta adrenoceptor agonists in rabbit common carotid arteries. Fujiwara, T., Chiba, S. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  17. Protective effects of nipradilol, isosorbide dinitrate, and bunazosin on coronary artery constriction induced by intracoronary injection of acetylcholine in pigs. Kawamura, A., Fujiwara, H., Ishida, M., Takemura, G., Kida, M., Uegaito, T., Tanaka, M., Kawai, C. Cardiovasc. Res. (1990) [Pubmed]
  18. Characterization of [3H]YM617, R-(-)-5-[2-[[2[ethoxyring(n)-3H](o-ethoxyphenoxy)ethyl]amino]- propyl]-2-methoxybenzenesulfonamide HCl, a potent and selective alpha-1 adrenoceptor radioligand. Yazawa, H., Takanashi, M., Sudoh, K., Inagaki, O., Honda, K. J. Pharmacol. Exp. Ther. (1992) [Pubmed]
  19. Effect of bunazosin, a selective alpha 1-adrenoceptor blocker, on ischemic myocardium in perfused rat heart. Haneda, T., Tanaka, H., Abe, M., Obata, H., Onodera, S. Clinical therapeutics. (1992) [Pubmed]
  20. Insulin sensitivity following treatment with the alpha 1-blocker bunazosin retard and the beta 1-blocker atenolol in hypertensive non-insulin-dependent diabetes mellitus patients. Eriksson, J.W., Jansson, P.A., Foley, K., Lithell, H. J. Hypertens. (1996) [Pubmed]
  21. Possible mechanism of acetaldehyde-induced noradrenaline release from sympathetic nerve terminals in isolated blood vessels. Chiba, S., Tsukada, M. Br. J. Pharmacol. (1988) [Pubmed]
  22. Differential effects of omega-conotoxin GVIA and tetrodotoxin on vasoconstrictions evoked by electrical stimulation and nicotinic receptor stimulation in canine isolated, perfused splenic arteries. Ren, L.M., Nakane, T., Chiba, S. Br. J. Pharmacol. (1994) [Pubmed]
  23. Bunazosin, an alpha 1-adrenoceptor blocker, differentially releases co-transmitters in dog mesenteric vessels. Komori, K., Nagao, T., Zhang, G.L., Ibengwe, J.K., Fujioka, M., Suzuki, H. Eur. J. Pharmacol. (1989) [Pubmed]
  24. Insulin insensitivity in nonobese, nondiabetic essential hypertension and its improvement by an alpha 1-blocker (bunazosin). Suzuki, M., Hirose, J., Asakura, Y., Sato, A., Kageyama, A., Harano, Y., Omae, T. Am. J. Hypertens. (1992) [Pubmed]
  25. Bunazosin hydrochloride inhibits exaggerated growth of vascular smooth muscle cells from spontaneously hypertensive rats by suppressing the response to growth factors. Hu, W.Y., Fukuda, N., Soma, M., Izumi, Y., Kanmatsuse, K. J. Cardiovasc. Pharmacol. (1998) [Pubmed]
  26. Alpha 2-adrenergic modulation of pancreatic glucagon secretion in rats. Saito, M., Saitoh, T., Inoue, S. Physiol. Behav. (1992) [Pubmed]
  27. Effects of sympathetic stimulation, with and without previous alpha 1 and beta adrenoceptor blockade, on refractoriness dispersion in canine heart. Tanabe, T., Takahashi, K., Kitada, M., Yoshioka, K., Handa, S., Mori, H. Cardiovasc. Res. (1994) [Pubmed]
  28. Pharmacological analysis of 5-HT-induced vasoconstriction in isolated, perfused dog skeletal muscle arteries. Sinanović, O., Chiba, S. Eur. J. Pharmacol. (1987) [Pubmed]
  29. Role of nitric oxide from the endothelium on the neurogenic contractile responses of rabbit pulmonary artery. Shinozuka, K., Kobayashi, Y., Shimoura, K., Hattori, K. Eur. J. Pharmacol. (1992) [Pubmed]
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