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In [[in vitro]] studies on mouse neurons, fasoracetam modulated [[mGluR]] II/III activity.<ref>{{cite journal |title=A novel cognition enhancer NS-105 modulates adenylate cyclase activity through metabotropic glutamate receptors in primary neuronal culture. | pmid=9272724 | volume=356 | journal=Naunyn Schmiedebergs Arch Pharmacol | pages=189–96 | last1 = Oka | first1 = M | last2 = Itoh | first2 = Y | last3 = Tatsumi | first3 = S | last4 = Ma | first4 = FH | last5 = Ukai | first5 = Y | last6 = Yoshikuni | first6 = Y | last7 = Kimura | first7 = K | doi=10.1007/pl00005040}}.</ref> In studies in rats, it blocked memory disruptions caused by [[baclofen]], a [[GABAB receptor|GABA<sub>B</sub>]] agonist<ref name=study1>{{cite journal |title=Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer. | pmid=10494996 | volume=64 | journal=Pharmacol Biochem Behav | pages=41–52 | last1 = Ogasawara | first1 = T | last2 = Itoh | first2 = Y | last3 = Tamura | first3 = M | last4 = Mushiroi | first4 = T | last5 = Ukai | first5 = Y | last6 = Kise | first6 = M | last7 = Kimura | first7 = K | doi=10.1016/s0091-3057(99)00108-2}}</ref> and [[upregulate]]d production of GABA<sub>B</sub> receptors after repeat dosing.<ref>{{cite journal |title=Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of GABA(B) receptor up-regulation after repeated treatment. | pmid=9424016 | volume=338 | journal=Eur J Pharmacol | pages=225–32 | last1 = Shimidzu | first1 = T | last2 = Itoh | first2 = Y | last3 = Oka | first3 = M | last4 = Ishima | first4 = T | last5 = Ukai | first5 = Y | last6 = Yoshikuni | first6 = Y | last7 = Kimura | first7 = K | doi=10.1016/s0014-2999(97)81925-5}}</ref>
In [[in vitro]] studies on mouse neurons, fasoracetam modulated [[mGluR]] II/III activity.<ref>{{cite journal |title=A novel cognition enhancer NS-105 modulates adenylate cyclase activity through metabotropic glutamate receptors in primary neuronal culture. | pmid=9272724 | volume=356 | journal=Naunyn Schmiedebergs Arch Pharmacol | pages=189–96 | last1 = Oka | first1 = M | last2 = Itoh | first2 = Y | last3 = Tatsumi | first3 = S | last4 = Ma | first4 = FH | last5 = Ukai | first5 = Y | last6 = Yoshikuni | first6 = Y | last7 = Kimura | first7 = K | doi=10.1007/pl00005040}}.</ref> In studies in rats, it blocked memory disruptions caused by [[baclofen]], a [[GABAB receptor|GABA<sub>B</sub>]] agonist<ref name=study1>{{cite journal |title=Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer. | pmid=10494996 | volume=64 | journal=Pharmacol Biochem Behav | pages=41–52 | last1 = Ogasawara | first1 = T | last2 = Itoh | first2 = Y | last3 = Tamura | first3 = M | last4 = Mushiroi | first4 = T | last5 = Ukai | first5 = Y | last6 = Kise | first6 = M | last7 = Kimura | first7 = K | doi=10.1016/s0091-3057(99)00108-2}}</ref> and [[upregulate]]d production of GABA<sub>B</sub> receptors after repeat dosing.<ref>{{cite journal |title=Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of GABA(B) receptor up-regulation after repeated treatment. | pmid=9424016 | volume=338 | journal=Eur J Pharmacol | pages=225–32 | last1 = Shimidzu | first1 = T | last2 = Itoh | first2 = Y | last3 = Oka | first3 = M | last4 = Ishima | first4 = T | last5 = Ukai | first5 = Y | last6 = Yoshikuni | first6 = Y | last7 = Kimura | first7 = K | doi=10.1016/s0014-2999(97)81925-5}}</ref>
==Experimental Medical Uses==
In a five-week, single-site, phase one trial, 30 adolescents with ADHD and genetic disorders impacting [[metabotropic glutamate receptor]]s (mGluRs) showed improvement in symptoms. <ref>{{cite conference | title=Exploratory Dose-Escalation Study of NFC-1 in ADHD Adolescents With Glutamatergic Gene Network Variants. | conference=American Academy of Child and Adolescent Psychiatry | date=2015 | last1 = Jones | first1 = G | last2 = Dejesus-Rosario | first2 = N | last3 = Kao | first3 = C | last4 = Larsen | first4 = L | last5 = Chiavacci | first5 = R | last6 = Pallotto | first6 = A | last7 = Kurian | first7 = C | url=http://phx.corporate-ir.net/External.File?item=UGFyZW50SUQ9NTk5Mzk0fENoaWxkSUQ9MzEwMTg5fFR5cGU9MQ==&t=1}}</ref><ref>{{cite web | title=Efficacy and Safety of NFC-1 in Adolescents With Genetic Disorders Impacting mGluR and ADHD. | url=https://clinicaltrials.gov/ct2/show/NCT02777931 | author=ClinicalTrials.gov}} </ref>

==References==
==References==


Revision as of 06:27, 1 June 2017

Fasoracetam
Names
IUPAC name
(5R)-5-(piperidine-1-carbonyl) pyrrolidin-2-one
Other names
(5R)-5-oxo-D-prolinepiperidinamide
Identifiers
3D model (JSmol)
ChEMBL
ChemSpider
KEGG
  • InChI=1S/C10H16N2O2/c13-9-5-4-8(11-9)10(14)12-6-2-1-3-7-12/h8H,1-7H2,(H,11,13)/t8-/m1/s1 checkY
    Key: GOWRRBABHQUJMX-MRVPVSSYSA-N checkY
  • InChI=1/C10H16N2O2/c13-9-5-4-8(11-9)10(14)12-6-2-1-3-7-12/h8H,1-7H2,(H,11,13)/t8-/m1/s1
    Key: GOWRRBABHQUJMX-MRVPVSSYBL
  • O=C(N1CCCCC1)[C@@H]2NC(=O)CC2
Properties
C10H16N2O2
Molar mass 196.250 g·mol−1
Pharmacology
Oral
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
☒N verify (what is checkY☒N ?)

Fasoracetam (NS-105, 5-oxo-D-prolinepiperidinamide monohydrate)[1] is a research chemical of the racetam family.[2] It is a nootropic, and has been in a clinical trial for attention deficit hyperactivity disorder.[3]

In in vitro studies on mouse neurons, fasoracetam modulated mGluR II/III activity.[4] In studies in rats, it blocked memory disruptions caused by baclofen, a GABAB agonist[5] and upregulated production of GABAB receptors after repeat dosing.[6]

Experimental Medical Uses

In a five-week, single-site, phase one trial, 30 adolescents with ADHD and genetic disorders impacting metabotropic glutamate receptors (mGluRs) showed improvement in symptoms. [7][8]

References

  1. ^ FDA/NIH Substance registration system. Page accessed March 21, 2016
  2. ^ "5-oxo-D-prolinepiperidinamide monohydrate - Compound Summary". Retrieved 21 July 2013.
  3. ^ "Drug Profile Fasoracetam".
  4. ^ Oka, M; Itoh, Y; Tatsumi, S; Ma, FH; Ukai, Y; Yoshikuni, Y; Kimura, K. "A novel cognition enhancer NS-105 modulates adenylate cyclase activity through metabotropic glutamate receptors in primary neuronal culture". Naunyn Schmiedebergs Arch Pharmacol. 356: 189–96. doi:10.1007/pl00005040. PMID 9272724..
  5. ^ Ogasawara, T; Itoh, Y; Tamura, M; Mushiroi, T; Ukai, Y; Kise, M; Kimura, K. "Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer". Pharmacol Biochem Behav. 64: 41–52. doi:10.1016/s0091-3057(99)00108-2. PMID 10494996.
  6. ^ Shimidzu, T; Itoh, Y; Oka, M; Ishima, T; Ukai, Y; Yoshikuni, Y; Kimura, K. "Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of GABA(B) receptor up-regulation after repeated treatment". Eur J Pharmacol. 338: 225–32. doi:10.1016/s0014-2999(97)81925-5. PMID 9424016.
  7. ^ Jones, G; Dejesus-Rosario, N; Kao, C; Larsen, L; Chiavacci, R; Pallotto, A; Kurian, C (2015). Exploratory Dose-Escalation Study of NFC-1 in ADHD Adolescents With Glutamatergic Gene Network Variants. American Academy of Child and Adolescent Psychiatry.
  8. ^ ClinicalTrials.gov. "Efficacy and Safety of NFC-1 in Adolescents With Genetic Disorders Impacting mGluR and ADHD".


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