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Chemical Compound Review

Fasoracetam     (5R)-5-(1- piperidylcarbonyl)pyrrolidin- 2-one

Synonyms: LAM-105, SureCN194770, NS-105, CHEMBL2106179, LS-115850, ...
 
 
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Disease relevance of C13311

  • Conversely, in pertussis toxin-pretreated neurons, NS-105 (10(-7)-10(-5) M) significantly enhanced the forskolin-stimulated cyclic AMP formation, and this action was completely reversed by cholera toxin [1].
 

Psychiatry related information on C13311

  • The present experiment was designed to evaluate the antidepressant activity of NS-105 in the forced swimming and learned helplessness tests in rats [2].
 

High impact information on C13311

  • These findings suggest that the inhibitory action of NS-105 on adenylyl cyclase activity is mediated through group II and group III mGlu receptor subclasses while the facilitatory action is dependent on the group I mGlu receptor subclass [3].
  • The effect of (+)-5-oxo-D-prolinepiperidinamide monohydrate (NS-105), a novel cognition enhancer, on adenylate cyclase activity was investigated in cultured neurons of the mouse cerebral cortex [1].
  • Biochemical data showed that repeated administration of NS-105 increased the number of GABA(B) receptors in rat cerebral cortex without affecting the binding properties of beta-adrenoceptors and 5-HT2 receptors [2].
  • NS-105 (10(-8)-10(-6) M) inhibited forskolin-stimulated cAMP formation in membranes, however, the compound significantly enhanced the cAMP formation in pertussis toxin-pre-treated membranes, an action that was abolished by cholera toxin [4].
  • Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of GABA(B) receptor up-regulation after repeated treatment [2].
 

Biological context of C13311

  • The effect of a novel cognition enhancer [(+)-5-oxo-D-prolinepiperidinamide monohydrate] (NS-105) on cAMP formation was investigated in both slices and membranes of the rat cerebral cortex [4].
  • These findings suggest that NS-105, which lacks an effect on monoaminergic systems, has potent antidepressant activity, which may involve up-regulation of GABA(B) receptors after repeated administration [2].
  • The phosphoinositides hydrolysis was enhanced by 1S, 3R-ACPD (10(-4) M) but not by NS-105 (10(-6) M), however, 1S, 3R-ACPD-induced increase in phosphoinositides turnover was attenuated by NS-105 [1].
  • Comparison of pharmacokinetics of NS-105, a novel agent for cerebrovascular disease, in elderly and young subjects [5].
  • The tissue distribution patterns of radioactivity in female (non-pregnant) and pregnant rats after the oral administration of 14C-NS-105 did not differ from the pattern in male rats, revealing neither sex- nor pregnancy-related differences in NS-105 distribution [6].
 

Anatomical context of C13311

 

Associations of C13311 with other chemical compounds

  • We have previously found that a cognition enhancer [(+)-5-oxo-D-prolinepiperidinamide monohydrate] (NS-105) reversed the inhibition of cyclic AMP formation induced by the GABA(B) receptor agonist baclofen [2].
  • Involvement of metabotropic glutamate receptors in Gi- and Gs-dependent modulation of adenylate cyclase activity induced by a novel cognition enhancer NS-105 in rat brain [4].
 

Gene context of C13311

  • The absorption, metabolism and excretion of NS-105 ((+)-5-oxo-D-prolinepiperidinamide monohydrate, CAS 110958-19-5), a novel cognition enhancer, were studied in rats, dogs and monkeys after intravenous or oral administration of 14C-NS-105 [7].
 

Analytical, diagnostic and therapeutic context of C13311

  • In primary cultured neurons of mouse cerebral cortex, the inhibitory action of NS-105 on adenylyl cyclase activity disappeared after treatment with antisense oligodeoxynucleotides for group II (mGlu(2) and mGlu(3) receptors) and group III (mGlu(4) and mGlu(7) receptors) but not group I (mGlu(5) receptor) mGlu receptor subclasses [3].
  • NS-105 showed antiamnestic actions in a variety of animal models of cholinergic dysfunction employed in this study [8].
  • Repeated oral administration of NS-105 (10 mg/kg) to male rats did not affect hepatic drug-metabolizing enzyme activities [6].
  • After the intravenous injection, the plasma concentration of NS-105 decreased monoexponentially with respective elimination half-lives of 0.67, 2.1 and 1.3 h for the rats, dogs and monkeys [7].

References

  1. A novel cognition enhancer NS-105 modulates adenylate cyclase activity through metabotropic glutamate receptors in primary neuronal culture. Oka, M., Itoh, Y., Tatsumi, S., Ma, F.H., Ukai, Y., Yoshikuni, Y., Kimura, K. Naunyn Schmiedebergs Arch. Pharmacol. (1997) [Pubmed]
  2. Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of GABA(B) receptor up-regulation after repeated treatment. Shimidzu, T., Itoh, Y., Oka, M., Ishima, T., Ukai, Y., Yoshikuni, Y., Kimura, K. Eur. J. Pharmacol. (1997) [Pubmed]
  3. Role of metabotropic glutamate receptor subclasses in modulation of adenylyl cyclase activity by a nootropic NS-105. Hirouchi, M., Oka, M., Itoh, Y., Ukai, Y., Kimura, K. Eur. J. Pharmacol. (2000) [Pubmed]
  4. Involvement of metabotropic glutamate receptors in Gi- and Gs-dependent modulation of adenylate cyclase activity induced by a novel cognition enhancer NS-105 in rat brain. Oka, M., Itoh, Y., Shimidzu, T., Ukai, Y., Yoshikuni, Y., Kimura, K. Brain Res. (1997) [Pubmed]
  5. Comparison of pharmacokinetics of NS-105, a novel agent for cerebrovascular disease, in elderly and young subjects. Kumagai, Y., Yokota, S., Isawa, S., Murasaki, M., Mukai, H., Miyatake, S. International journal of clinical pharmacology research. (1999) [Pubmed]
  6. Pharmacokinetics of NS-105, a novel cognition enhancer. 2nd communication: distribution and transfer into fetus and milk after single administration, and effects of repeated administration on pharmacokinetics and hepatic drug-metabolizing enzyme activities in rats. Mukai, H., Sugimoto, T., Ago, M., Morino, A., Takaichi, M., Ogawa, Y., Seki, H., Matsuura, C., Esumi, Y. Arzneimittel-Forschung. (1999) [Pubmed]
  7. Pharmacokinetics of NS-105, a novel cognition enhancer. 1st communication: absorption, metabolism and excretion in rats, dogs and monkeys after single administration of 14C-NS-105. Mukai, H., Sugimoto, T., Ago, M., Morino, A. Arzneimittel-Forschung. (1999) [Pubmed]
  8. Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer. Ogasawara, T., Itoh, Y., Tamura, M., Mushiroi, T., Ukai, Y., Kise, M., Kimura, K. Pharmacol. Biochem. Behav. (1999) [Pubmed]
 
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