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Chemical Compound Review

CHEMBL907     2-butyl-5-chloro-3-[[4-[2- (2H-tetrazol-5...

Synonyms: SureCN179, EXP-3174, AG-D-52606, SureCN2187501, ACMC-20mr6h, ...
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Disease relevance of Exp3174


Psychiatry related information on Exp3174


High impact information on Exp3174

  • The facilitatory effect of Ang II was blocked by either the peptide Ang II receptor antagonist saralasin (1.0 mumol/L) or EXP 3174 (0.1 mumol/L), the in vitro active form of the nonpeptide Ang II receptor antagonist losartan [4].
  • Background and aim Previous data indicate that the urinary losartan/E-3174 ratio is a marker for cytochrome P450 (CYP) 2C9 activity in vivo [5].
  • The urinary losartan/E-3174 ratio of the single CYP2C9*1/*6 subject was higher than the 95% confidence interval of the mean of the CYP2C9*1/*1 group (0.0-3.7), whereas the metabolic ratio of the CYP2C9*8/*11 carrier was inside the 95% confidence interval of the means of the CYP2C9*1/*1 and CYP2C9*1/*11 groups (0.0-18) [5].
  • RESULTS: The urinary losartan/E-3174 ratio in the various genotypes was as follows: 1.85 +/- 2.4 (mean +/- SD) for CYP2C9*1/*1, 14.6 for CYP2C9*1/*5, 4.2 for CYP2C9*1/*6, 188 for CYP2C9*5/*6, 11.6 for CYP2C9*5/*8, 0.44 +/- 0.13 (mean +/- SD) for CYP2C9*1/*8, 2.2 for CYP2C9*8/*11, and 5.72 +/- 4.5 (mean +/- SD) for CYP2C9*1/*11 [5].
  • Pharmacokinetics of losartan and its metabolite E-3174 in relation to the CYP2C9 genotype [6].

Biological context of Exp3174

  • Effect of EXP 3174 on blood pressure of normoreninemic renal hypertensive rats [7].
  • RESULTS: The maximum plasma concentration of E-3174 was significantly (P <.05) lower in the CYP2C9*1/*3 (n = 5) and CYP2C9*2/*3 (n = 4) groups compared with the CYP2C9*1/*1 (n = 6) and CYP2C9*1/*2 (n = 3) groups and extremely low in 1 subject with the CYP2C9*3/*3 genotype [6].
  • Our aim was to evaluate the pharmacokinetics of losartan and E-3174 in relation to the CYP2C9 genotype [6].
  • CONCLUSION: Chronic, but not acute, administration of EXP 3174 normalized baroreflex function in SHR [8].
  • HR 720 blocked the increase in protein synthesis with potency similar to EXP 3174; the respective IC50 values were 1.04 x 10(-9) M and 1.36 x 10(-9) M [9].

Anatomical context of Exp3174


Associations of Exp3174 with other chemical compounds


Gene context of Exp3174

  • OBJECTIVE: Losartan is metabolised to its active metabolite E-3174 by CYP2C9 and CYP3A4 in vitro [17].
  • Our study demonstrated that acute blockade of the AT1 receptor with E-3174 reduced elevated pre- and after-load and consequently increased stroke volume in a canine HF model [18].
  • Reflex elevation of plasma renin activity induced by 1 mg/kg of E-3174 was similar to that caused by 1 mg/kg of enalapril, suggesting that the two drugs achieved similar inhibition of the endogenous renin angiotensin system [18].
  • The present study suggests that CYP2D6 and CYP2C19 are not involved to any major extent in the in vivo conversion of losartan to E-3174 [19].
  • These effects appeared to be essentially mediated by AT1 receptor stimulation as indicated by the equal inhibitory effects of HR 720 and EXP 3174 [9].

Analytical, diagnostic and therapeutic context of Exp3174


  1. Phenobarbital minimally alters plasma concentrations of losartan and its active metabolite E-3174. Goldberg, M.R., Lo, M.W., Deutsch, P.J., Wilson, S.E., McWilliams, E.J., McCrea, J.B. Clin. Pharmacol. Ther. (1996) [Pubmed]
  2. Pharmacokinetics and blood pressure response of losartan in end-stage renal disease. Sica, D.A., Halstenson, C.E., Gehr, T.W., Keane, W.F. Clinical pharmacokinetics. (2000) [Pubmed]
  3. Effects of angiotensin II AT1- or AT2-receptor antagonists on drinking evoked by angiotensin II or water deprivation in rats. Widdop, R.E., Gardiner, S.M., Bennett, T. Brain Res. (1994) [Pubmed]
  4. Beta 2-adrenergic receptor and angiotensin II receptor modulation of sympathetic neurotransmission in human atria. Rump, L.C., Schwertfeger, E., Schaible, U., Fraedrich, G., Schollmeyer, P. Circ. Res. (1994) [Pubmed]
  5. Functional impact of CYP2C95, CYP2C96, CYP2C98, and CYP2C911 in vivo among black Africans. Allabi, A.C., Gala, J.L., Horsmans, Y., Babaoglu, M.O., Bozkurt, A., Heusterspreute, M., Yasar, U. Clin. Pharmacol. Ther. (2004) [Pubmed]
  6. Pharmacokinetics of losartan and its metabolite E-3174 in relation to the CYP2C9 genotype. Yasar, U., Forslund-Bergengren, C., Tybring, G., Dorado, P., Llerena, A., Sjöqvist, F., Eliasson, E., Dahl, M.L. Clin. Pharmacol. Ther. (2002) [Pubmed]
  7. Effect of EXP 3174 on blood pressure of normoreninemic renal hypertensive rats. Basso, N., Kurnjek, M.L., Ruiz, P., Cannata, M.A. Hypertension (1995) [Pubmed]
  8. Effect of acute and chronic treatment with the angiotensin II subtype 1 receptor antagonist EXP 3174 on baroreflex function in conscious spontaneously hypertensive rats. Bartholomeusz, B., Widdop, R.E. J. Hypertens. (1995) [Pubmed]
  9. HR 720, a novel angiotensin receptor antagonist inhibits the angiotensin II-induced trophic effects, fibronectin release and fibronectin-EIIIA+ expression in rat aortic vascular smooth muscle cells in vitro. Dunn, F.W., Roux, M.H., Farhadian, F., Sabri, K., Ossart, C., Samuel, J.L., Rappaport, L., Hamon, G. J. Pharmacol. Exp. Ther. (1997) [Pubmed]
  10. Blocking hypothalamic AT1 receptors lowers blood pressure in salt-sensitive rats. Yang, R.H., Jin, H., Chen, S.J., Wyss, J.M., Oparil, S. Hypertension (1992) [Pubmed]
  11. Threshold sodium excretory and renal blood flow effects of angiotensin converting enzyme inhibition. Zhang, X., Dunham, E.W., Zimmerman, B.G. J. Hypertens. (1995) [Pubmed]
  12. Intrinsic properties of the nonpeptide angiotensin II antagonist losartan in glomeruli and mesangial cells at high concentrations. Chansel, D., Badre, L., Czekalski, S., Vandermeersch, S., Cambar, J., Ardaillou, R. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  13. Active transport of the angiotensin-II antagonist losartan and its main metabolite EXP 3174 across MDCK-MDR1 and caco-2 cell monolayers. Soldner, A., Benet, L.Z., Mutschler, E., Christians, U. Br. J. Pharmacol. (2000) [Pubmed]
  14. Beta-adrenergic, angiotensin II, and bradykinin receptors enhance neurotransmission in human kidney. Rump, L.C., Bohmann, C., Schaible, U., Schultze-Seemann, W., Schollmeyer, P.J. Hypertension (1995) [Pubmed]
  15. Application of capillary zone electrophoresis to the screening of some angiotensin II receptor antagonists. González, L., Akesolo, U., Jiménez, R.M., Alonso, R.M. Electrophoresis (2002) [Pubmed]
  16. In vitro and in vivo effects of UP 269-6, a new potent orally active nonpeptide angiotensin II receptor antagonist, on vascular smooth muscle cell proliferation. Virone-Oddos, A., Desangle, V., Provost, D., Cazes, M., Caussade, F., Cloarec, A. Br. J. Pharmacol. (1997) [Pubmed]
  17. Fluconazole but not itraconazole decreases the metabolism of losartan to E-3174. Kaukonen, K.M., Olkkola, K.T., Neuvonen, P.J. Eur. J. Clin. Pharmacol. (1998) [Pubmed]
  18. Acute effects of E-3174, a human active metabolite of losartan, on the cardiovascular system in tachycardia-induced canine heart failure. Suzuki, J., Ohta, H., Hanada, K., Kawai, N., Ikeda, T., Nakao, M., Ikemoto, F., Nishikibe, M. Hypertens. Res. (2001) [Pubmed]
  19. Lack of polymorphism of the conversion of losartan to its active metabolite E-3174 in extensive and poor metabolizers of debrisoquine (cytochrome P450 2D6) and mephenytoin (cytochrome P450 2C19). Sandwall, P., Lo, M.W., Jonzon, B., Dalén, P., Furtek, C., Ritter, M., Alván, G., McCrea, J., Sjöqvist, F. Eur. J. Clin. Pharmacol. (1999) [Pubmed]
  20. Clinical pharmacokinetics of losartan. Sica, D.A., Gehr, T.W., Ghosh, S. Clinical pharmacokinetics. (2005) [Pubmed]
  21. Sulfonylureas and sulfonylcarbamates as new non-tetrazole angiotensin II receptor antagonists. Discovery of a highly potent orally active (imidazolylbiphenylyl)sulfonylurea (HR 720). Deprez, P., Guillaume, J., Becker, R., Corbier, A., Didierlaurent, S., Fortin, M., Frechet, D., Hamon, G., Heckmann, B., Heitsch, H. J. Med. Chem. (1995) [Pubmed]
  22. The effect of AST-120 on the single-dose pharmacokinetics of losartan and losartan acid (E-3174) in healthy subjects. Marier, J.F., Guilbaud, R., Kambhampati, S.R., Mathew, P., Moberly, J., Lee, J., Salazar, D.E. Journal of clinical pharmacology. (2006) [Pubmed]
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