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Chemical Compound Review

Isotazin     N,N-diethyl-1-phenothiazin- 10-yl-propan-2...

Synonyms: Lysivane, Parcidol, Pardidol, Parkisol, Parsidan, ...
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Psychiatry related information on Parfezin


High impact information on Parfezin

  • The volume of the butyrylcholinesterase active site gorge is approximately 200 A3 larger than that of the acetylcholinesterase gorge, which allows the accommodation of ethopropazine in two different orientations as demonstrated by rigid-body refinement and molecular dynamics calculations [2].
  • Volume calculations for the active site gorge showed that the poor inhibitory activity of ethopropazine toward acetylcholinesterase was due to the smaller dimension of the active site gorge which was unable to accommodate the bulky inhibitor molecule [2].
  • In one group of controls ethopropazine was used to inhibit pseudocholinesterases and in another group BW 284C 51 was used to inhibit acetylcholinesterase (AChE) [3].
  • For the analysis of the data in the presence of ethopropazine at two temperatures, we have enlarged the reaction scheme to allow primarily its competition with the substrate at the peripheral site, but the competition at the acylation site was not excluded [4].
  • Cholinesterase inhibitors Ro 2-1250 and Ro 2-0638 inhibited both canine cholinesterases, while huperzine A preferentially inhibited canine AChE and ethopropazine inhibited canine BuChE [5].

Biological context of Parfezin


Anatomical context of Parfezin


Associations of Parfezin with other chemical compounds


Gene context of Parfezin

  • More than 97% of AChE activity was inhibited by 10 microM eserine or BW284C51, but only 53% of the activity was inhibited by ethopropazine at the same concentration [18].
  • Ethopropazine totally depressed the pseudo ChE activity from horse serum at a concentration of 5 X 10(-5) M [14].
  • An inhibition study with specific pseudo-chE inhibitor (ethopropazine), or with anti-human pseudo-chE sera, has produced evidence that this genetically variant chE is pseudo-chE [19].

Analytical, diagnostic and therapeutic context of Parfezin


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  3. Acetylcholinesterase-positive fibers and cell bodies in the cochlear nuclei of normal and reeler mutant mice. Martin, M.R. J. Comp. Neurol. (1981) [Pubmed]
  4. Kinetic model of ethopropazine interaction with horse serum butyrylcholinesterase and its docking into the active site. Golicnik, M., Sinko, G., Simeon-Rudolf, V., Grubic, Z., Stojan, J. Arch. Biochem. Biophys. (2002) [Pubmed]
  5. Cholinesterases in cardiac ganglia and modulation of canine intrinsic cardiac neuronal activity. Darvesh, S., MacDonald, S.E., Losier, A.M., Martin, E., Hopkins, D.A., Armour, J.A. J. Auton. Nerv. Syst. (1998) [Pubmed]
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  8. In vitro human plasma leucine(5)-enkephalin degradation is inhibited by a select number of drugs with the phenothiazine molecule in their chemical structure. Mosnaim, A.D., Puente, J., Saavedra, R., Diamond, S., Wolf, M.E. Pharmacology (2003) [Pubmed]
  9. Pharmacokinetics of ethopropazine in the rat after oral and intravenous administration. Maboudian-Esfahani, M., Brocks, D.R. Biopharmaceutics & drug disposition. (1999) [Pubmed]
  10. Disposition of ethopropazine enantiomers in the rat: tissue distribution and plasma protein binding. Brocks, D.R., Maboudian-Esfahani, M. Journal of pharmacy & pharmaceutical sciences [electronic resource] : a publication of the Canadian Society for Pharmaceutical Sciences, Société canadienne des sciences pharmaceutiques. (1999) [Pubmed]
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  12. Mucosal delivery of cytotoxic therapeutic agents: response of rat nasal mucosa to microencapsulated ethopropazine HCl enantiomer. Persyn, J.T., McDonough, J.A., Nino, J.A., Dixon, H., Boland, E.J. Journal of microencapsulation. (2005) [Pubmed]
  13. Area-specific modification of acetylcholinesterase activity following 3-mercaptopropionic acid-induced seizures. Girardi, E., Schneider, P., Rodriguez De Lores Arnaiz, G. Mol. Chem. Neuropathol. (1994) [Pubmed]
  14. Use of ethopropazine and BW 284C51 as selective inhibitors for cholinesterases from various species. Mikalsen, A., Andersen, R.A., Alexander, J. Comp. Biochem. Physiol. C, Comp. Pharmacol. Toxicol. (1986) [Pubmed]
  15. Rivastigmine is a potent inhibitor of acetyl- and butyrylcholinesterase in Alzheimer's plaques and tangles. Eskander, M.F., Nagykery, N.G., Leung, E.Y., Khelghati, B., Geula, C. Brain Res. (2005) [Pubmed]
  16. Separation, conformation in solution and absolute configuration of ethopropazine enantiomers. Sinko, G., Novak, P., Ziher, D., Vinković, V., Sunjić, V., Simeon-Rudolf, V. Enantiomer. (2002) [Pubmed]
  17. Comparison of efficacy of ginger with various antimotion sickness drugs. Wood, C.D., Manno, J.E., Wood, M.J., Manno, B.R., Mims, M.E. Clinical research practices and drug regulatory affairs. (1988) [Pubmed]
  18. Purification and characterization of acetylcholinesterase from oriental fruit fly [Bactrocera dorsalis (Hendel)] (Diptera: Tephritidae). Hsiao, Y.M., Lai, J.Y., Liao, H.Y., Feng, H.T. J. Agric. Food Chem. (2004) [Pubmed]
  19. Characterization of serum cholinesterase in familial hyper-cholinesterasemia associated with an isozyme variant band. Yamamoto, K., Morito, F., Setoguchi, Y., Fujii, S., Kariya, T., Sakai, T. Gastroenterol. Jpn. (1987) [Pubmed]
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