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Chemical Compound Review

Pivagabine     4-(2,2- dimethylpropanoylamino) butanoic acid

Synonyms: Tonerg, CXB-722, AG-C-43734, AG-K-94979, CHEMBL1870796, ...
 
 
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Disease relevance of Pivagabine

  • In conclusion, in patients with hypothalamic amenorrhea related to weight loss pivagabine induced a significant decrease of cortisol secretion and an increase of GH release by pivagabine administration, suggesting that this drug exerts a specific neuroendocrine modulatory role [1].
  • Effect of pivagabine on stress-induced gastric ulcer formation in rats [2].
  • Pivagabine determined a significant reduction in the number of animals with gastric lesions (5 vs. 10, p < 0.05), in the linear extension of ulcers (2.0 +/- 0.8 vs. 7.2 +/- 1.7 mm, percent protection 72.2, p < 0.05) and in the linear extension of hemorrhages (2.6 +/- 1.0 vs. 10.3 +/- 1.6 mm, percent protection 74.8, p < 0.01) [2].
 

Psychiatry related information on Pivagabine

 

High impact information on Pivagabine

 

Biological context of Pivagabine

 

Anatomical context of Pivagabine

  • These results demonstrate that pivagabine increases the amount of CRF mRNA in both the hypothalamus and cerebral cortex of rats, effects that might be relevant to the action of this drug in preventing the stress-induced changes in CRF hypothalamic concentration [9].
 

Gene context of Pivagabine

  • A double-blind, placebo-controlled study was performed in order to evaluate the efficacy of pivagabine (4-[(2,2-dimethyl-1-oxopropyl)amino]butanoic acid, CAS 69542-93-4, Tonerg) on "distress" in children hospitalized for acute disorders [11].
  • The results shown in the present study were positive and likely attributable to the inhibitory modulating activity of pivagabine on corticotropin releasing factor secretion, that is considered to be responsible for insomnia associated with anxiety or coexisting anxiety and depression, observed in patients with chronic stress [5].
  • It is likely that the observed effects of pivagabine are mediated by inhibition of release of corticotropin-releasing factor, a neurohormone involved in stress-generating mechanisms [12].
  • One hundred and eighteen patients with neurasthenia, as defined by ICD 10 (International Classification of Diseases), participated in a randomised, double-blind, placebo-controlled trial of pivagabine (4-[(2,2-dimethyl-1-oxopropyl)amino]butanoic acid, CAS 69542-93-4, Tonerg) [4].
 

Analytical, diagnostic and therapeutic context of Pivagabine

References

  1. Pivagabine decreases stress-related hormone secretion in women with hypothalamic amenorrhea. Genazzani, A.D., Stomati, M., Bersi, C., Luisi, S., Fedalti, M., Santuz, M., Esposito, G., Petraglia, F., Genazzani, A.R. J. Endocrinol. Invest. (2000) [Pubmed]
  2. Effect of pivagabine on stress-induced gastric ulcer formation in rats. Gianni, A.M., Bruno, G., Sirtori, C. Arzneimittel-Forschung. (1997) [Pubmed]
  3. Pivagabine effects on neuroendocrine responses to experimentally-induced psychological stress in humans. Gerra, G., Zaimovic, A., Giusti, F., Baroni, M.C., Delsignore, R., Raggi, M.A., Brambilla, F. Behav. Brain Res. (2001) [Pubmed]
  4. Randomised, double-blind, placebo-controlled study of pivagabine in neurasthenia. Pizzolato, G., Cagnin, A., Mancia, D., Caffarra, P., Avanzi, S., Copelli, S., Ciappina, C., Lo Presti, F., Spilimbergo, P.G., D'Antonio, E., Di Costanzo, E., Matrango, M., Pastres, P., Urbani, P.P., Signorino, M., Simoncelli, M., Provinciali, L., Regnicolo, L., Albano, C., Roccatagliata, G., Rubino, V., Cultrera, S., Fracassi, M. Arzneimittel-Forschung. (1997) [Pubmed]
  5. Evaluation of the efficacy of pivagabine on insomnia associated with mood disorders. Negri, L. Arzneimittel-Forschung. (1997) [Pubmed]
  6. Clinical evaluation of the efficacy of pivagabine in the treatment of mood and adjustment disorders. Terranova, R., Gilotta, S.M., Luca, S. Arzneimittel-Forschung. (1997) [Pubmed]
  7. Pivagabine: a novel psychoactive drug. Esposito, G., Luparini, M.R. Arzneimittel-Forschung. (1997) [Pubmed]
  8. Antagonism by pivagabine of stress-induced changes in GABAA receptor function and corticotropin-releasing factor concentrations in rat brain. Serra, M., Concas, A., Mostallino, M.C., Chessa, M.F., Stomati, M., Petraglia, F., Genazzani, A.R., Biggio, G. Psychoneuroendocrinology (1999) [Pubmed]
  9. Pivagabine-induced increases in the abundance of CRF mRNA in the cerebral cortex and hypothalamus of rats. Follesa, P., Cagetti, E., Porta, S., Espositoto, G., Biggio, G. Brain Res. Mol. Brain Res. (2000) [Pubmed]
  10. Role of pivagabine in the treatment of climacteric syndrome. Gigliotti, B., Multinu, A., Lai, V.R. Arzneimittel-Forschung. (1997) [Pubmed]
  11. Use of pivagabine in the management of hospitalization distress in children. Gelsomini, S. Arzneimittel-Forschung. (1997) [Pubmed]
  12. Effects of pivagabine on psychophysical performance and behavioural response in experimental models of stress. Scapagnini, U., Matera, M. Arzneimittel-Forschung. (1997) [Pubmed]
 
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