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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
Chemical Compound Review

Diprivan     2,6-dipropan-2-ylphenol

Synonyms: Fresofol, propofol, Aquafol, Recofol, Disoprivan, ...
 
 
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Disease relevance of Disoprofol

 

Psychiatry related information on Disoprofol

 

High impact information on Disoprofol

 

Chemical compound and disease context of Disoprofol

 

Biological context of Disoprofol

 

Anatomical context of Disoprofol

 

Associations of Disoprofol with other chemical compounds

 

Gene context of Disoprofol

  • All of the CYPs evaluated were capable of hydroxylating propofol; however, CYP2B6 and CYP2C9 were most active [33].
  • A competitive inhibition of CYP2E1 by propofol was observed with low inhibition constants in the therapeutic range in both porcine (19 microM) and human (48 microM) liver microsomes [34].
  • CONCLUSIONS: Cytochrome P-450 2B6, and to a lesser extent CYP2C9, contribute to the oxidative metabolism of propofol [33].
  • Here we studied the effects of propofol on recombinant HCN1, HCN2, and HCN4 channels and found that the drug inhibits and slows activation of all three channels at clinically relevant concentrations [35].
  • Valproic acid inhibited UGT1A9 catalyzed propofol glucuronidation in an uncompetitive manner and UGT2B7 catalyzed AZT glucuronidation competitively (K(i)=1.6+/-0.06mM) [36].
 

Analytical, diagnostic and therapeutic context of Disoprofol

References

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  14. Heat shock protein 60 in rostral ventrolateral medulla reduces cardiovascular fatality during endotoxaemia in the rat. Chang, A.Y., Chan, J.Y., Chou, J.L., Li, F.C., Dai, K.Y., Chan, S.H. J. Physiol. (Lond.) (2006) [Pubmed]
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  20. Glucuronidation as a mechanism of intrinsic drug resistance in human colon cancer: reversal of resistance by food additives. Cummings, J., Ethell, B.T., Jardine, L., Boyd, G., Macpherson, J.S., Burchell, B., Smyth, J.F., Jodrell, D.I. Cancer Res. (2003) [Pubmed]
  21. Changes in drug plasma concentrations of an extensively bound and highly extracted drug, propofol, in response to altered plasma binding. Hiraoka, H., Yamamoto, K., Okano, N., Morita, T., Goto, F., Horiuchi, R. Clin. Pharmacol. Ther. (2004) [Pubmed]
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  23. The general anesthetic pentobarbital slows desensitization and deactivation of the glycine receptor in the rat spinal dorsal horn neurons. Lu, H., Xu, T.L. J. Biol. Chem. (2002) [Pubmed]
  24. Propofol decreases the clearance of midazolam by inhibiting CYP3A4: an in vivo and in vitro study. Hamaoka, N., Oda, Y., Hase, I., Mizutani, K., Nakamoto, T., Ishizaki, T., Asada, A. Clin. Pharmacol. Ther. (1999) [Pubmed]
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  28. Ethanol enhances alpha 4 beta 3 delta and alpha 6 beta 3 delta gamma-aminobutyric acid type A receptors at low concentrations known to affect humans. Wallner, M., Hanchar, H.J., Olsen, R.W. Proc. Natl. Acad. Sci. U.S.A. (2003) [Pubmed]
  29. Pharmacokinetics of midazolam, propofol, and fentanyl transfer to human breast milk. Nitsun, M., Szokol, J.W., Saleh, H.J., Murphy, G.S., Vender, J.S., Luong, L., Raikoff, K., Avram, M.J. Clin. Pharmacol. Ther. (2006) [Pubmed]
  30. Isoflurane and propofol inhibit voltage-gated sodium channels in isolated rat neurohypophysial nerve terminals. Ouyang, W., Wang, G., Hemmings, H.C. Mol. Pharmacol. (2003) [Pubmed]
  31. A comparison of spectral edge, delta power, and bispectral index as EEG measures of alfentanil, propofol, and midazolam drug effect. Billard, V., Gambus, P.L., Chamoun, N., Stanski, D.R., Shafer, S.L. Clin. Pharmacol. Ther. (1997) [Pubmed]
  32. Sub-clinical hepatic encephalopathy in cirrhotic patients is not aggravated by sedation with propofol compared to midazolam: a randomized controlled study. Khamaysi, I., William, N., Olga, A., Alex, I., Vladimir, M., Kamal, D., Nimer, A. J. Hepatol. (2011) [Pubmed]
  33. Cytochrome P-450 2B6 is responsible for interindividual variability of propofol hydroxylation by human liver microsomes. Court, M.H., Duan, S.X., Hesse, L.M., Venkatakrishnan, K., Greenblatt, D.J. Anesthesiology (2001) [Pubmed]
  34. Inhibition of cytochrome P450 2E1 by propofol in human and porcine liver microsomes. Lejus, C., Fautrel, A., Mallédant, Y., Guillouzo, A. Biochem. Pharmacol. (2002) [Pubmed]
  35. Impairment of hyperpolarization-activated, cyclic nucleotide-gated channel function by the intravenous general anesthetic propofol. Cacheaux, L.P., Topf, N., Tibbs, G.R., Schaefer, U.R., Levi, R., Harrison, N.L., Abbott, G.W., Goldstein, P.A. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  36. The effect of valproic acid on drug and steroid glucuronidation by expressed human UDP-glucuronosyltransferases. Ethell, B.T., Anderson, G.D., Burchell, B. Biochem. Pharmacol. (2003) [Pubmed]
  37. Long-term propofol infusion and cardiac failure in adult head-injured patients. Cremer, O.L., Moons, K.G., Bouman, E.A., Kruijswijk, J.E., de Smet, A.M., Kalkman, C.J. Lancet (2001) [Pubmed]
  38. Propofol for conscious sedation? Byrne, M.F., Baillie, J. Gastroenterology (2002) [Pubmed]
  39. Propofol for endoscopy sedation. Bassett, M., Ashton, C., Gavaghan, T., Hillman, L., Kaye, G., Clarke, A. Gastroenterology (2003) [Pubmed]
 
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