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Chemical Compound Review

Avishot     1-[4-(2- methoxyphenyl)piperazin-1- yl]-3...

Synonyms: Flivas, naftopidil, Naftopidilum, Flivas (TN), S2126_Selleck, ...
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Disease relevance of Flivas


High impact information on Flivas


Chemical compound and disease context of Flivas


Biological context of Flivas

  • The inhibition of Ca2+ mobilization was not reflected by a concentration-dependent inhibition of platelet aggregation, although 40 microM naftopidil produced statistically significant inhibition (23.3 +/- 11.7%, P < 0.05) [10].
  • I.v. administration of naftopidil significantly increased BC in CI rats without an increase in residual volume, but it had no effects on BC in RTX-CI rats [2].
  • Both prazosin and urapidil showed similar affinity to [3H]-prazosin binding sites in human tissue, whereas YM617 and naftopidil showed approximately a 12 and two times higher affinity, respectively, to alpha 1-adrenoceptor sites of prostate than aorta [11].
  • The pharmacological profiles of the alpha1-adrenoceptor antagonists naftopidil, tamsulosin and prazosin were studied in an anesthetized dog model that allowed the simultaneous assessment of their antagonist potency against phenylephrine-mediated increases in prostatic pressure and mean blood pressure [12].
  • Pharmacokinetics of naftopidil, a novel anti-hypertensive drug, in patients with hepatic dysfunction [5].

Anatomical context of Flivas

  • Therefore, in addition to the antagonistic action of these agents on the alpha-1 adrenergic receptors of prostatic smooth muscle, both agents (especially naftopidil) may also act on the lumbosacral cord, and thus may improve collecting disorders in patients with benign prostatic hyperplasia [13].
  • 3H-prazosin and 3H-clonidine binding to the rat cortex membranes was inhibited by KT-611 with pKi values of 7.69 and 5.75, respectively [14].
  • Thus, it is suggested that naftopidil antagonizes alpha 1-adrenoceptors in human prostates in a competitive and reversible manner [15].
  • KT-611 also inhibited the sympathetic adrenergic contraction evoked by electrical transmural stimulation in the dog mesenteric artery, and the inhibition was not relieved upon repetitive washing for 1 hour with the drug-free solution [14].
  • Naftopidil exerts its antihypertensive action via alpha 1-adrenoceptor blockage and Ca2+ antagonism in vascular smooth muscle [16].

Associations of Flivas with other chemical compounds


Gene context of Flivas

  • Naftopidil, a novel antihypertensive compound, possesses 5-HT1A agonistic properties in addition to being an alpha 1-adrenoceptor antagonist [20].
  • However, the responses mediated through prejunctional alpha 2-adrenoceptors (rat vas deferens), beta-adrenoceptors (rat atria), muscarinic receptors (guinea pig ileum) and 5-HT2 receptors (dog mesenteric artery) were little affected by KT-611 [14].
  • Naftopidil had no effect on collagen-induced PDGF release [19].
  • The metabolism of 14C-naftopidil ((R,S)-1-(2-methoxyphenyl)-1-piperazinyl-3- (1-naphthyl-oxy-2-propanol, CAS 57149-07-2) and the pharmacodynamic action of the metabolites was investigated [21].

Analytical, diagnostic and therapeutic context of Flivas


  1. Effect of naftopidil on urethral obstruction in benign prostatic hyperplasia: assessment by urodynamic studies. Yasuda, K., Yamanishi, T., Tojo, M., Nagashima, K., Akimoto, S., Shimazaki, J. Prostate (1994) [Pubmed]
  2. Improvement of bladder storage function by alpha1-blocker depends on the suppression of C-fiber afferent activity in rats. Yokoyama, O., Yusup, A., Oyama, N., Aoki, Y., Tanase, K., Matsuta, Y., Miwa, Y., Akino, H. Neurourol. Urodyn. (2006) [Pubmed]
  3. Vascular alpha1-adrenoceptor subtype selectivity and alpha1-blocker-induced orthostatic hypotension. Take, H., Shibata, K., Awaji, T., Hirasawa, A., Ikegaki, I., Asano, T., Takada, T., Tsujimoto, G. Jpn. J. Pharmacol. (1998) [Pubmed]
  4. Comparison of two alpha1-adrenoceptor antagonists, naftopidil and tamsulosin hydrochloride, in the treatment of lower urinary tract symptoms with benign prostatic hyperplasia: a randomized crossover study. Nishino, Y., Masue, T., Miwa, K., Takahashi, Y., Ishihara, S., Deguchi, T. BJU international. (2006) [Pubmed]
  5. Pharmacokinetics of naftopidil, a novel anti-hypertensive drug, in patients with hepatic dysfunction. Farthing, M.J., Alstead, E.M., Abrams, S.M., Haug, G., Johnston, A., Hermann, R., Niebch, G., Ruus, P., Molz, K.H., Turner, P. Postgraduate medical journal. (1994) [Pubmed]
  6. Activation of alpha1D adrenergic receptors in the rat urothelium facilitates the micturition reflex. Ishihama, H., Momota, Y., Yanase, H., Wang, X., de Groat, W.C., Kawatani, M. J. Urol. (2006) [Pubmed]
  7. Single-blind, randomized controlled study of the clinical and urodynamic effects of an alpha-blocker (naftopidil) and phytotherapy (eviprostat) in the treatment of benign prostatic hyperplasia. Kaplan, S.A. J. Urol. (2005) [Pubmed]
  8. Effects of intrathecal injection of tamsulosin and naftopidil, alpha-1A and 1D adrenergic receptor antagonists, on bladder activity in rats. Kaplan, S.A. J. Urol. (2003) [Pubmed]
  9. Comparison of tamsulosin and naftopidil for efficacy and safety in the treatment of benign prostatic hyperplasia: a randomized controlled trial. Gotoh, M., Kamihira, O., Kinukawa, T., Ono, Y., Ohshima, S., Origasa, H. BJU international. (2005) [Pubmed]
  10. In vitro adrenaline and collagen-induced mobilization of platelet calcium and its inhibition by naftopidil, doxazosin and nifedipine. Alarayyed, N.A., Cooper, M.B., Prichard, B.N., Betteridge, D.J., Smith, C.C. British journal of clinical pharmacology. (1997) [Pubmed]
  11. Comparative study on alpha 1-adrenoceptor antagonist binding in human prostate and aorta. Yamada, S., Suzuki, M., Tanaka, C., Mori, R., Kimura, R., Inagaki, O., Honda, K., Asano, M., Takenaka, T., Kawabe, K. Clin. Exp. Pharmacol. Physiol. (1994) [Pubmed]
  12. Naftopidil, a novel alpha1-adrenoceptor antagonist, displays selective inhibition of canine prostatic pressure and high affinity binding to cloned human alpha1-adrenoceptors. Takei, R., Ikegaki, I., Shibata, K., Tsujimoto, G., Asano, T. Jpn. J. Pharmacol. (1999) [Pubmed]
  13. Effects of intrathecal injection of tamsulosin and naftopidil, alpha-1A and -1D adrenergic receptor antagonists, on bladder activity in rats. Sugaya, K., Nishijima, S., Miyazato, M., Ashitomi, K., Hatano, T., Ogawa, Y. Neurosci. Lett. (2002) [Pubmed]
  14. Pharmacological profile of the novel alpha-adrenoceptor antagonist KT-611 (naftopidil). Muramatsu, I., Yamanaka, K., Kigoshi, S. Jpn. J. Pharmacol. (1991) [Pubmed]
  15. Binding characteristics of naftopidil and alpha 1-adrenoceptor antagonists to prostatic alpha-adrenoceptors in benign prostatic hypertrophy. Yamada, S., Suzuki, M., Kato, Y., Kimura, R., Mori, R., Matsumoto, K., Maruyama, M., Kawabe, K. Life Sci. (1992) [Pubmed]
  16. Naftopidil inhibits 5-hydroxytryptamine-induced platelet aggregation and 5-hydroxytryptamine uptake in platelets of healthy volunteers. Kirsten, R., Breidert, M., Nelson, K., Heine, A., Rosenkranz, S., Erdeg, B., Niebch, G., Borbe, H.O., Siebert-Weigel, M., Respondek, J. Eur. J. Clin. Pharmacol. (1994) [Pubmed]
  17. The potentiation of adrenaline-induced in vitro platelet aggregation by ADP, collagen and serotonin and its inhibition by naftopidil and doxazosin in normal human subjects. Alarayyed, N.A., Graham, B.R., Prichard, B.N., Smith, C.C. British journal of clinical pharmacology. (1995) [Pubmed]
  18. In vitro effect of naftopidil, a novel alpha-adrenergic antagonist on cation transport systems in human erythrocytes, leukocytes and platelets. Lijnen, P. Methods and findings in experimental and clinical pharmacology. (1991) [Pubmed]
  19. Differential actions of naftopidil, doxazosin and nifedipine on platelet thromboxane generation and platelet-derived growth factor efflux in vitro. Alarayyed, N.A., Prichard, B.N., Betteridge, D.J., Smith, C.C. Platelets (2002) [Pubmed]
  20. 5-HT1A-agonistic properties of naftopidil, a novel antihypertensive drug. Borbe, H.O., Metzenauer, P., Szelenyi, I. Eur. J. Pharmacol. (1991) [Pubmed]
  21. Metabolic fate of the novel antihypertensive drug naftopidil. Niebch, G., Locher, M., Peter, G., Borbe, H.O. Arzneimittel-Forschung. (1991) [Pubmed]
  22. High-performance liquid chromatography of naftopidil, a novel antihypertensive drug, and two metabolites in human plasma. Niebch, G., Borbe, H.O., Besenfelder, E. J. Chromatogr. (1990) [Pubmed]
  23. Radioreceptor assay for the determination of alpha 1-adrenoceptor-binding material in rat plasma following single oral administration of naftopidil. Borbe, H.O., Peter, G. Arzneimittel-Forschung. (1990) [Pubmed]
  24. Cellular and humoral effects of naftopidil in man. Lijnen, P. Methods and findings in experimental and clinical pharmacology. (1992) [Pubmed]
  25. Usefulness of tamsulosin hydrochloride and naftopidil in patients with urinary disturbances caused by benign prostatic hyperplasia: a comparative, randomized, two-drug crossover study. Ikemoto, I., Kiyota, H., Ohishi, Y., Abe, K., Goto, H., Kishimoto, K., Miki, K. International journal of urology : official journal of the Japanese Urological Association. (2003) [Pubmed]
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