The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

Tak-044     disodium 2-[(2R,5S,8S,11R,14S,17R)-8...

Synonyms: CHEMBL61425, CHEBI:193908, AC1L3XH4, 157380-72-8
This record was replaced with 123883.
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of


High impact information on


Chemical compound and disease context of


Biological context of


Anatomical context of


Associations of with other chemical compounds

  • Vasodilation to TAK-044 was abolished after treatment with candesartan cilexetil; this effect is associated with a reduced plasma ET-1 concentration [14].
  • METHODS: We administered acutely either the selective ETA receptor antagonist FR139317 (FR, n = 6, 1 and 10 mg/kg) or the mixed ETA/ETB receptor antagonist TAK-044 (TAK, n = 6, 1 and 3 mg/kg) to conscious dogs with CHF induced by rapid right ventricular pacing for ten days [15].
  • In addition, the ETB-mediated vasoconstriction and pressor responses were inhibited by TAK-044 and not by BQ-123 [16].
  • The influence of a nonselective antagonist of endothelin receptors, TAK-044 (cyclo-[d-alpha-aspartyl-3-[(4-phenylpiperazin-1-yl)carbonyl]-l-alanyl-l-alpha-aspartyl-d-2-(2-thienyl)glycyl-l-leucyl-d-tryptophyl] disodium), on the positive inotropic effect of endothelin-1 and endothelin-3 was investigated in isolated rabbit myocardium [17].
  • Treatment with TAK-044 resulted in a significant decrease in systolic blood pressure (SBP), blood urea nitrogen (BUN), serum creatinine concentration, plasma aldosterone level, heart weight, and kidney weight [18].

Gene context of


Analytical, diagnostic and therapeutic context of

  • TAK-044 dose-dependently reversed the effects of ET-1 on RBFprobe and cortical perfusion [11].
  • METHODS: In a porcine orthotopic liver transplantation model, changes in the serum and liver tissue ET-1 concentration were measured and the effects of an ET receptor antagonist, TAK-044, were evaluated [5].
  • CONCLUSIONS: These findings indicate TAK-044 treatment has protective effects on postoperative function of hepatic allografts procured from NHBDs [5].
  • 6. Intravenous injection of TAK-044 10 min before coronary occlusion reduced the infarct size in a dose-dependent manner: 32% and 54% reductions at 1 and 3 mg kg-1, respectively [12].
  • 3. A 15 min intravenous infusion of placebo or 30 mg TAK-044 (giving a serum concentration of 2 nM, calculated to block > 95% of ETA but < 5% ETB receptors) had no effect on the immunoreactive plasma concentrations of the three peptides [19].


  1. Systemic endothelin receptor blockade decreases peripheral vascular resistance and blood pressure in humans. Haynes, W.G., Ferro, C.J., O'Kane, K.P., Somerville, D., Lomax, C.C., Webb, D.J. Circulation (1996) [Pubmed]
  2. Hepatoprotective effect of the endothelin receptor antagonist TAK-044 against ischemia-reperfusion injury in the canine liver. Kitayama, Y., Yamanaka, N., Kawamura, E., Kuroda, N., Okamoto, E. Hepatology (1997) [Pubmed]
  3. Effects of the endothelin receptor antagonist TAK-044 on hepatocyte element alterations in the ischemic-reperfused liver in Beagle dogs. Imakita, M., Yamanaka, N., Kuroda, N., Kitayama, Y., Sasaki, S., Nakagaki, I., Hori, S., Okamoto, E. J. Hepatol. (1998) [Pubmed]
  4. Pharmacologic graft protection without donor pretreatment in liver transplantation from non-heart-beating donors. Gu, M., Takada, Y., Fukunaga, K., Ishiguro, S., Taniguchi, H., Seino, K., Yuzawa, K., Otsuka, M., Todoroki, T., Fukao, K. Transplantation (2000) [Pubmed]
  5. Endothelin antagonist treatment for successful liver transplantation from non-heart-beating donors. Fukunaga, K., Takada, Y., Taniguchi, H., Mei, G., Seino, K.I., Yuzawa, K., Otsuka, M., Todoroki, T., Goto, K., Fukao, K. Transplantation (1999) [Pubmed]
  6. Modulation of endothelin and nitric oxide: a rational approach to improve canine hepatic microcirculation. Dhar, D.K., Yamanoi, A., Ohmori, H., Nakashima, Y., Yamamoto, A., Osama, N.E., Kubota, H., Kohno, H., Nagasue, N. Hepatology (1998) [Pubmed]
  7. Improvement of renal dysfunction in dogs with endotoxemia by a nonselective endothelin receptor antagonist. Mitaka, C., Hirata, Y., Yokoyama, K., Nagura, T., Tsunoda, Y., Amaha, K. Crit. Care Med. (1999) [Pubmed]
  8. An endothelin receptor antagonist TAK-044 ameliorates carbon tetrachloride-induced acute liver injury and portal hypertension in rats. Gandhi, C.R., Nemoto, E.M., Watkins, S.C., Subbotin, V.M. Liver (1998) [Pubmed]
  9. Effect of an endothelin receptor antagonist and an angiotensin converting enzyme inhibitor on metabolism and contraction in the ischemic and reperfused rabbit heart. Kawabata, H., Ryomoto, T., Ishikawa, K. Jpn. Circ. J. (1999) [Pubmed]
  10. Effects of the ET(A)/ET(B) antagonist, TAK-044, on blood pressure and renal excretory function after unclipping of conscious one-kidney-one-clip hypertensive rats. Bergström, G., Nyström, H.C., Jia, J., Evans, R.G. J. Hypertens. (2001) [Pubmed]
  11. Renal haemodynamic effects of endothelin-1 and the ETA/ETB antagonist TAK-044 in anaesthetized rabbits. Evans, R.G., Bergström, G., Cotterill, E., Anderson, W.P. J. Hypertens. (1998) [Pubmed]
  12. Pharmacology of a non-selective ETA and ETB receptor antagonist, TAK-044 and the inhibition of myocardial infarct size in rats. Watanabe, T., Awane, Y., Ikeda, S., Fujiwara, S., Kubo, K., Kikuchi, T., Kusumoto, K., Wakimasu, M., Fujino, M. Br. J. Pharmacol. (1995) [Pubmed]
  13. Inhibitory effects of TAK-044 on endothelin induced vasoconstriction in various canine arteries and porcine coronary arteries: a comparison with selective ETA and ETB receptor antagonists. Awane-Igata, Y., Ikeda, S., Watanabe, T. Br. J. Pharmacol. (1997) [Pubmed]
  14. Effect of the angiotensin II type 1 receptor blocker candesartan on endothelial function in patients with essential hypertension. Ghiadoni, L., Virdis, A., Magagna, A., Taddei, S., Salvetti, A. Hypertension (2000) [Pubmed]
  15. Comparison of the acute effects of a selective endothelin ETA and a mixed ETA/ETB receptor antagonist in heart failure. Ohnishi, M., Wada, A., Tsutamoto, T., Fukai, D., Kinoshita, M. Cardiovasc. Res. (1998) [Pubmed]
  16. A new endothelin receptor antagonist, TAK-044, shows long-lasting inhibition of both ETA- and ETB-mediated blood pressure responses in rats. Ikeda, S., Awane, Y., Kusumoto, K., Wakimasu, M., Watanabe, T., Fujino, M. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  17. Differential inhibition by TAK-044 of the inotropic effects of endothelin-1 and endothelin-3. Yomogida, S., Maruya, J., Norota, I., Ishii, K., Endoh, M. Eur. J. Pharmacol. (2004) [Pubmed]
  18. Hemodynamic and biochemical effects of endothelin-A- and -B-receptor antagonist TAK-044 in stroke-prone spontaneously hypertensive rats. Naruse, M., Tanabe, A., Naruse, K., Adachi, C., Yoshimoto, T., Seki, T., Takagi, S., Imaki, T., Watanabe, T., Takano, K. J. Cardiovasc. Pharmacol. (2000) [Pubmed]
  19. The increase in human plasma immunoreactive endothelin but not big endothelin-1 or its C-terminal fragment induced by systemic administration of the endothelin antagonist TAK-044. Plumpton, C., Ferro, C.J., Haynes, W.G., Webb, D.J., Davenport, A.P. Br. J. Pharmacol. (1996) [Pubmed]
  20. Receptor binding and antagonist properties of a novel endothelin receptor antagonist, TAK-044 [cyclo[D-alpha-aspartyl-3-[(4-phenylpiperazin-1-yl) carbonyl]-L-alanyl-L-alpha-aspartyl-D-2-(2-thienyl) glycyl-L-leucyl-D-tryptophyl]disodium salt], in human endothelinA and endothelinB receptors. Masuda, Y., Sugo, T., Kikuchi, T., Kawata, A., Satoh, M., Fujisawa, Y., Itoh, Y., Wakimasu, M., Ohtaki, T. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  21. Renal vascular effects of the selective endothelin receptor antagonists in anaesthetized rats. Matsuura, T., Miura, K., Ebara, T., Yukimura, T., Yamanaka, S., Kim, S., Iwao, H. Br. J. Pharmacol. (1997) [Pubmed]
WikiGenes - Universities