Fasoracetam Índice Pruebas Clínicas. Efectos Mecanismo de acción Referencias Menú de navegación31592CHEMBL210617917198019869542O8UF5CJBC133111S/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/s1GOWRRBABHQUJMX-MRVPVSSYSA-NNúmero CAS«5-oxo-D-prolinepiperidinamide monohydrate - Compound Summary»«Drug Profile Fasoracetam»«Phase I Single Dose, Open-label, Pharmacokinetic Study Followed by Single-blind, Placebo-controlled Dose Escalation Study to Evaluate the Safety, Tolerability, Plasma Concentration Profiles, and Targeted Efficacy of NFC-1 in Adolescents (12-17 Years of Age) With Attention-Deficit Hyperactivity Disorder and Genetic Disruption Impacting Metabotropic Glutamate Receptor Genes (NFC1-GREAT)»«Phase Ib dose-escalation trial of fasoracetam [NFC-1] in mGluR network mutation positive adolescents with attention deficit hyperactivity disorder»«Phase II/III trial of fasoracetam [NFC-1] in mGluR network mutation positive patients with attention deficit hyperactivity disorder and neuropsychiatric symptoms resulting from 22q11.2 deletion syndrome (22q11.2 DS)»«A novel cognition enhancer NS-105 modulates adenylate cyclase activity through metabotropic glutamate receptors in primary neuronal culture.»«Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer.»«Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of GABA(B) receptor up-regulation after repeated treatment.»«Copia archivada»el original

AmidasPiperidinasRacetamos


Baclofeno
























 
Fasoracetam

Fasoracetam.svg
Fórmula molecular
?
Identificadores
Número CAS
110958-19-5[1]​
ChEBI
31592
ChEMBL
CHEMBL2106179
ChemSpider
171980
PubChem
198695
UNII
42O8UF5CJB
KEGG
C13311


Propiedades físicas
Masa molar
196,121 g/mol
[editar datos en Wikidata]

Fasoracetam (NS-105, 5-oxo-D-prolinepiperidinamide monohydrate) es una sustancia química en investigación de la familia de los racetam.[2]​


Este nootropico está siendo estudiado para tratar el Síndrome de Atención con hiperactividad y está en fase de pruebas desde 2015 arrojando resultados positivos.[3]​


Es común como suplemento nutricional nootropico (que favorece las capacidades intelectuales), de venta por internet, así como otros compuestos de la misma familia.




Índice





  • 1 Pruebas Clínicas.


  • 2 Efectos


  • 3 Mecanismo de acción


  • 4 Referencias




Pruebas Clínicas.


Fasoracetam ha completado la Fase I para el trastorno por déficit de atención e hiperactividad.[4]​


También ha completado la Fase Ib con éxito, de prueba de escalación de dosis en adolescentes con mutación del gen mGluR y trastorno por déficit de atención e hiperactividad. Los resultados fueron presentados en la Reunión 62 anual de la academia de psiquiatría americada de Niños y Adolescentes. (AACAP), en febrero del 2016.[5]​


En febrero de 2016, la FDA de américa, aceptó IND para Fasoracetam para revisión para tratar el síndrome de deleción 22q11.2.[3]​


Actualmente está en la fase II/III en pacientes con mutación del gen mGluR con déficit de atención e hiperactividad.[6]​



Efectos


No posee efectos estimulantes, ni sedantes puesto que no afecta a ninguna monoamina neurotransmisora (dopamina, serotonina...), sin embargo mejora la cognición,[7]​ tiene propiedades de mejora sustancial de la memoria,[8]​ y tiene un potente efecto antidepresivo con la aplicación crónica.[9]​



Mecanismo de acción


Fasoracetam actúa como un modulador glutamatérgico mGluR II/III.[7]​[10]​ Se ha visto que bloquea las disrupciones de memoria causadas por Baclofeno, un agonista GABA B.[8]​ Fasoracetam, también regula al alza los receptores GABA b después de una aplicación crónica, produciendo efectos a largo plazo ansiolíticos, de mejora de la atención y antidepresivos.[9]​



Referencias



  1. ↑ Número CAS


  2. ↑ «5-oxo-D-prolinepiperidinamide monohydrate - Compound Summary». Consultado el 21 de julio de 2013. 


  3. ↑ ab «Drug Profile Fasoracetam». 


  4. ↑ «Phase I Single Dose, Open-label, Pharmacokinetic Study Followed by Single-blind, Placebo-controlled Dose Escalation Study to Evaluate the Safety, Tolerability, Plasma Concentration Profiles, and Targeted Efficacy of NFC-1 in Adolescents (12-17 Years of Age) With Attention-Deficit Hyperactivity Disorder and Genetic Disruption Impacting Metabotropic Glutamate Receptor Genes (NFC1-GREAT)». 


  5. ↑ «Phase Ib dose-escalation trial of fasoracetam [NFC-1] in mGluR network mutation positive adolescents with attention deficit hyperactivity disorder». 


  6. ↑ «Phase II/III trial of fasoracetam [NFC-1] in mGluR network mutation positive patients with attention deficit hyperactivity disorder and neuropsychiatric symptoms resulting from 22q11.2 deletion syndrome (22q11.2 DS)». 


  7. ↑ ab «A novel cognition enhancer NS-105 modulates adenylate cyclase activity through metabotropic glutamate receptors in primary neuronal culture.». 


  8. ↑ ab «Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer.». 


  9. ↑ ab «Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of GABA(B) receptor up-regulation after repeated treatment.». 


  10. ↑ «Copia archivada». Archivado desde el original el 4 de marzo de 2016. Consultado el 12 de julio de 2015. 








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