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Chemical Compound Review

SureCN2812700     [5- (carbamimidoylsulfanylmethyl) thiophen-2...

Synonyms: AC1L9729, NCIOpen2_007575
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Disease relevance of NSC55712


High impact information on NSC55712


Chemical compound and disease context of NSC55712


Biological context of NSC55712

  • Therefore, if biotransformation by this pathway is responsible for the production of nephrotoxic metabolites of compound A, humans may be less susceptible to compound A renal toxicity than are rats [3].
  • Areas under the inspired and expired compound A concentration versus time curves (AUC) were 79 +/- 54-ppm-h (range, 10-223 ppm-h) and 53 +/- 40 ppm-h (range, 6-159 ppm-h), respectively [11].
  • Mean maximum inhalation concentration of compound A using baralyme was 20.28 +/- 8.6 ppm (mean +/- SEM) compared to 8.16 +/- 2.67 ppm obtained with soda lime, a difference that did not reach statistical significance [12].
  • RESULTS: The lowest concentration of compound A applied without metabolic activator (27 ppm) significantly increased (P < 0.001) sister chromatid exchanges, and increasing concentrations of compound A increased the incidence of exchanges [13].
  • RESULTS: During anesthesia, average and maximum inspired compound A concentrations were 27 +/- 7 and 34 +/- 6 (mean +/- SD) and median mean blood pressure, esophageal temperature, and end-tidal carbon dioxide levels were 63 mmHg, 36.8 degrees C, and 32 mmHg, respectively [14].

Anatomical context of NSC55712


Associations of NSC55712 with other chemical compounds

  • Quantitative determination of vapor-phase compound A in sevoflurane anesthesia using gas chromatography-mass spectrometry [17].
  • Both the "shallow" probe (compound A) and the "depth" probe (compound B) were coupled for 10-14% (of the label added) to apoA-I and apoA-II from HDL3 and for about 6% to apoA-I and apoA-II from HDL2 [18].
  • These results suggest that binding of the test substances to CBG in female rat plasma and concomitant displacement of endogenous corticosterone could be part of the contraceptive mechanism of S. tuberculatiformis and the aziridine precursor, compound A [19].
  • The results demonstrate that most of the reactive intermediates and products formed by the beta-lyase-catalyzed biotransformation of compound A-derived cysteine S-conjugates are also formed in the two chemical systems studied [20].
  • The primary active transport previously assessed in an in vitro study in canalicular membrane vesicles was also highest for BQ-485 and lowest for compound A, similar to CLbile, h/fT in vivo [21].

Gene context of NSC55712


Analytical, diagnostic and therapeutic context of NSC55712


  1. A small molecule very late antigen-4 antagonist can inhibit ovalbumin-induced lung inflammation. Koo, G.C., Shah, K., Ding, G.J., Xiao, J., Wnek, R., Doherty, G., Tong, X.C., Pepinsky, R.B., Lin, K.C., Hagmann, W.K., Kawka, D., Singer, I.I. Am. J. Respir. Crit. Care Med. (2003) [Pubmed]
  2. A synthetic derivative of the natural product rocaglaol is a potent inhibitor of cytokine-mediated signaling and shows neuroprotective activity in vitro and in animal models of Parkinson's disease and traumatic brain injury. Fahrig, T., Gerlach, I., Horváth, E. Mol. Pharmacol. (2005) [Pubmed]
  3. Renal toxicity with sevoflurane: a storm in a teacup? Gentz, B.A., Malan, T.P. Drugs (2001) [Pubmed]
  4. A selective novel low-molecular-weight inhibitor of IkappaB kinase-beta (IKK-beta) prevents pulmonary inflammation and shows broad anti-inflammatory activity. Ziegelbauer, K., Gantner, F., Lukacs, N.W., Berlin, A., Fuchikami, K., Niki, T., Sakai, K., Inbe, H., Takeshita, K., Ishimori, M., Komura, H., Murata, T., Lowinger, T., Bacon, K.B. Br. J. Pharmacol. (2005) [Pubmed]
  5. Corticosterone metabolism and effects on angiotensin II receptors in vascular smooth muscle. Ullian, M.E., Walsh, L.G. Circ. Res. (1995) [Pubmed]
  6. An allosteric activator of glucokinase impairs the interaction of glucokinase and glucokinase regulatory protein and regulates glucose metabolism. Futamura, M., Hosaka, H., Kadotani, A., Shimazaki, H., Sasaki, K., Ohyama, S., Nishimura, T., Eiki, J., Nagata, Y. J. Biol. Chem. (2006) [Pubmed]
  7. Role of the renal cysteine conjugate beta-lyase pathway in inhaled compound A nephrotoxicity in rats. Kharasch, E.D., Hoffman, G.M., Thorning, D., Hankins, D.C., Kilty, C.G. Anesthesiology (1998) [Pubmed]
  8. Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity. Hirose, H., Aoki, I., Kimura, T., Fujikawa, T., Numazawa, T., Sasaki, K., Sato, A., Hasegawa, T., Nishikibe, M., Mitsuya, M., Ohtake, N., Mase, T., Noguchi, K. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  9. Influence of sevoflurane on the metabolism and renal effects of compound A in rats. Kharasch, E.D., Schroeder, J.L., Sheffels, P., Liggitt, H.D. Anesthesiology (2005) [Pubmed]
  10. Dehydration of Baralyme increases compound A resulting from sevoflurane degradation in a standard anesthetic circuit used to anesthetize swine. Steffey, E.P., Laster, M.J., Ionescu, P., Eger, E.I., Gong, D., Weiskopf, R.B. Anesth. Analg. (1997) [Pubmed]
  11. Assessment of low-flow sevoflurane and isoflurane effects on renal function using sensitive markers of tubular toxicity. Kharasch, E.D., Frink, E.J., Zager, R., Bowdle, T.A., Artru, A., Nogami, W.M. Anesthesiology (1997) [Pubmed]
  12. Quantification of the degradation products of sevoflurane in two CO2 absorbants during low-flow anesthesia in surgical patients. Frink, E.J., Malan, T.P., Morgan, S.E., Brown, E.A., Malcomson, M., Brown, B.R. Anesthesiology (1992) [Pubmed]
  13. compound A induces sister chromatid exchanges in Chinese hamster ovary cells. Eger, E.I., Laster, M.J., Winegar, R., Han, C., Gong, D. Anesthesiology (1997) [Pubmed]
  14. Absence of biochemical evidence for renal and hepatic dysfunction after 8 hours of 1.25 minimum alveolar concentration sevoflurane anesthesia in volunteers. Ebert, T.J., Frink, E.J., Kharasch, E.D. Anesthesiology (1998) [Pubmed]
  15. Reaction of sevoflurane and its degradation products with soda lime. Toxicity of the byproducts. Morio, M., Fujii, K., Satoh, N., Imai, M., Kawakami, U., Mizuno, T., Kawai, Y., Ogasawara, Y., Tamura, T., Negishi, A. Anesthesiology (1992) [Pubmed]
  16. A prostacyclin receptor antagonist inhibits the sensitized release of substance P from rat sensory neurons. Nakae, K., Saito, K., Iino, T., Yamamoto, N., Wakabayashi, M., Yoshikawa, S., Matsushima, S., Miyashita, H., Sugimoto, H., Kiba, A., Gupta, J. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  17. Quantitative determination of vapor-phase compound A in sevoflurane anesthesia using gas chromatography-mass spectrometry. Bouche, M.P., Van Bocxlaer, J.F., Rolly, G., Versichelen, L.F., Struys, M.M., Mortier, E., De Leenheer, A.P. Clin. Chem. (2001) [Pubmed]
  18. Coupling of photoactivatable glycolipid probes to apolipoproteins A-I and A-II in human high density lipoproteins 2 and 3. Berkhout, T.A., Groot, P.H., van Belzen, R., Wirtz, K.W. J. Lipid Res. (1985) [Pubmed]
  19. Salsola tuberculatiformis Botschantzev and an aziridine precursor analog mediate the in vivo increase in free corticosterone and decrease in corticosteroid-binding globulin in female Wistar rats. Louw, A., Swart, P. Endocrinology (1999) [Pubmed]
  20. Reactive intermediate formation from the 2-(Fluoromethoxy)-1,1,3,3,3-pentafluoro-1-propene (compound A)-derived cysteine S-conjugate S-[2-(Fluoromethoxy)-1,1,3,3,3-pentafluoropropyl]-L-cysteine in pyridoxal model systems. Tong, Z., Anders, M.W. Chem. Res. Toxicol. (2002) [Pubmed]
  21. Hepatobiliary transport governs overall elimination of peptidic endothelin antagonists in rats. Kato, Y., Akhteruzzaman, S., Hisaka, A., Sugiyama, Y. J. Pharmacol. Exp. Ther. (1999) [Pubmed]
  22. ABCG2 confers resistance to indolocarbazole compounds by ATP-dependent transport. Nakagawa, R., Hara, Y., Arakawa, H., Nishimura, S., Komatani, H. Biochem. Biophys. Res. Commun. (2002) [Pubmed]
  23. Metabolic aromatization of N-alkyl-1,2,3,4-tetrahydroquinoline substructures to quinolinium by human liver microsomes and horseradish peroxidase. Gu, C., Collins, R., Holsworth, D.D., Walker, G.S., Voorman, R.L. Drug Metab. Dispos. (2006) [Pubmed]
  24. Cytochrome P450 2C8 (CYP2C8)-mediated hydroxylation of an endothelin ETA receptor antagonist in human liver microsomes. Ma, B., Subramanian, R., Schrag, M.L., Rodrigues, A.D., Tang, C. Drug Metab. Dispos. (2004) [Pubmed]
  25. Frontal immunoaffinity chromatography with mass spectrometric detection: a method for finding active compounds from traditional Chinese herbs. Luo, H., Chen, L., Li, Z., Ding, Z., Xu, X. Anal. Chem. (2003) [Pubmed]
  26. Effects of low-flow sevoflurane anesthesia on renal function: comparison with high-flow sevoflurane anesthesia and low-flow isoflurane anesthesia. Bito, H., Ikeuchi, Y., Ikeda, K. Anesthesiology (1997) [Pubmed]
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