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Chemical Compound Review

Pacinone     9-chloro-6-phenyl-2-(2,2,2- trifluoroethyl)...

Synonyms: Halazepam, Paxipam, Halazepamum, CHEMBL970, Paxipam (TN), ...
 
 
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Disease relevance of Pacinone

  • Since halazepam and quazepam, like the triazolopyridazines, have behavioral effects in animals at doses much lower than those that cause ataxia, it is tempting to attribute this separation of pharmacologic activities to differential activity at subpopulations of benzodiazepine receptors [1].
 

Psychiatry related information on Pacinone

  • Similar differences in favor of halazepam were observed at the same time points on paired comparison of percent improvement from baseline in scores for physician's global assessment of psychopathology and the Hamilton Anxiety Scale [2].
 

High impact information on Pacinone

 

Biological context of Pacinone

  • Our study was undertaken to evaluate its steady-state kinetics and those of its major active plasma metabolite N- desalkylhalazepam . Eleven healthy men aged 19 to 35 yr were given oral, 40-mg halazepam tablets every 8 hr for 14 days [3].
  • Computer EEG and somatosensory evoked potential studies demonstrated that halazepam has a significant effect on the EEG, characteristic of changes that occur with benzodiazepines [7].
  • In binding studies with rat brain membranes, 1,4-benzodiazepines containing a trifluoroethyl moeity at the 1-N position, including halazepam and quazepam, had significantly higher affinities for binding sites in cerebellum than in cortex [1].
 

Anatomical context of Pacinone

 

Associations of Pacinone with other chemical compounds

 

Gene context of Pacinone

  • In initial clinical studies, halazepam exhibited not only anxiolytic properties but also reduced symptoms of depression and had a therapeutic effect on epilepsy [7].
 

Analytical, diagnostic and therapeutic context of Pacinone

  • A double-blind crossover study of halazepam and placebo was carried out with 22 patients, 20 completing the study [10].
  • Later double-blind studies generally demonstrated that halazepam is significantly superior to placebo in alleviating symptoms of anxiety and tension [7].
  • In preliminary, uncontrolled clinical trials, halazepam was effective in ameliorating anxiety and tension in alcoholic and acute schizophrenic patients, with few adverse effects [7].

References

  1. Selective affinity of 1-N-trifluoroethyl benzodiazepines for cerebellar type 1 receptor sites. Iorio, L.C., Barnett, A., Billard, W. Life Sci. (1984) [Pubmed]
  2. Effectiveness of bedtime dosing of benzodiazepines: a placebo-controlled comparison of halazepam and clorazepate. Aden, G.C., O'Hair, D.E. Clinical therapeutics. (1980) [Pubmed]
  3. Multiple-dose halazepam kinetics. Chung, M., Hilbert, J.M., Gural, R.P., Radwanski, E., Symchowicz, S., Zampaglione, N. Clin. Pharmacol. Ther. (1984) [Pubmed]
  4. Clinical pharmacokinetics of the newer benzodiazepines. Greenblatt, D.J., Divoll, M., Abernethy, D.R., Ochs, H.R., Shader, R.I. Clinical pharmacokinetics. (1983) [Pubmed]
  5. Liquid chromatographic assay and pharmacokinetics of halazepam and its metabolite in humans. Gupta, S.K., Ellinwood, E.H. Journal of pharmaceutical sciences. (1990) [Pubmed]
  6. Metabolism of halazepam by rat liver microsomes: stereoselective formation and N-dealkylation of 3-hydroxyhalazepam. Lu, X.L., Yang, S.K. Chirality. (1990) [Pubmed]
  7. Pharmacology, efficacy, and adverse effects of halazepam, a new benzodiazepine. Fann, W.E., Pitts, W.M., Wheless, J.C. Pharmacotherapy (1982) [Pubmed]
  8. Autoradiographic demonstration of the selectivity of two 1-N-trifluoroethyl benzodiazepines for the BZD-1 receptors in the rat brain. Wamsley, J.K., Golden, J.S., Yamamura, H.I., Barnett, A. Pharmacol. Biochem. Behav. (1985) [Pubmed]
  9. Diazepam and halazepam in anxiety: some prognostic indicators. Rickels, K., Case, W.G., Chung, H., Downing, R.W., Vlahovich, J. International pharmacopsychiatry. (1978) [Pubmed]
  10. The effects of one-day treatment of anxiety with high doses of halazepam. Kellner, R., Bruzzese, D., Winslow, W.W., Rada, R.T., Wall, F.J. Journal of clinical pharmacology. (1978) [Pubmed]
 
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