FASORACETAM

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C10H16N2O2
Molecular Weight	196.2462
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O=C([C@H]1CCC(=O)N1)N2CCCCC2

InChI

InChIKey=GOWRRBABHQUJMX-MRVPVSSYSA-N

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

HIDE SMILES / InChI

Description
Sources: http://www.ncbi.nlm.nih.gov/pubmed/9272724
Curator's Comment: description was created based on several sources, including, https://www.nootropics.eu/a-review-on-the-benefits-of-fasoracetam/

Fasoracetam is a cognition enhancer that interacts with GABA(B) receptors, stimulates neuronal ACh receptors and modulates mGlu receptors. The drug is being tested in phase III/II of clinical trials for the treatment of Attention Deficit Disorder With Hyperactivity in people with genetic disorders impacting mGlu receptors and never been approved by FDA. Fasoracetam is also being marketed in the form of capsules for research purposes aimed at investigation of cognition and memory disorders.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
GABA-B receptor 32 Target ID: CHEMBL2111463 Sources: http://www.ncbi.nlm.nih.gov/pubmed/9424016	Antagonist 2849
Acetylcholine receptor 2 Target ID: Acetylcholine receptor Sources: http://www.ncbi.nlm.nih.gov/pubmed/10494996	Agonist 2752
Metabotropic glutamate receptors 2 Target ID: Metabotropic glutamate receptors Sources: http://www.medgenics.com/c/pipeline/	Modulator 846

Conditions

Condition	Modality	Targets	Highest Phase	Product
Attention deficit hyperactivity disorder 70 Sources: https://clinicaltrials.gov/ct2/show/NCT02777931	Primary		Phase III 665	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
3.06 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10450537/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
2.13 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10450537/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1.19 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN
1.72 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN
5.07 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN
10.77 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN
20.52 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
24.6 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10450537/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
14.4 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/10450537/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
6.87 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN
15.68 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN
30.2 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN
58.11 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN
136.46 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
4.44 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN
6.99 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN
4.48 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN
4.11 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	400 mg single, oral dose: 400 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN
4.06 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29339723/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	FASORACETAM plasma	Homo sapiens population: UNHEALTHY age: ADOLESCENT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
400 mg 2 times / day multiple, oral Highest studied dose Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29339723/	unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/29339723/	Sources: https://pubmed.ncbi.nlm.nih.gov/29339723/

PubMed

Title	Date	PubMed
Involvement of cholinergic and GABAergic systems in the reversal of memory disruption by NS-105, a cognition enhancer.	1999-09	10494996
Fasoracetam. LAM 105, NS 105.	1999-08	10820660
Comparison of pharmacokinetics of NS-105, a novel agent for cerebrovascular disease, in elderly and young subjects.	1999	10450537
Effect of a novel cognition enhancer NS-105 on learned helplessness in rats: possible involvement of GABA(B) receptor up-regulation after repeated treatment.	1997-11-12	9424016
A novel cognition enhancer NS-105 modulates adenylate cyclase activity through metabotropic glutamate receptors in primary neuronal culture.	1997-08	9272724
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.	1997-04-18	9134967

Patents

Sample Use Guides

In Vivo Use Guide

100, 200, or 400 mg twice daily as capsules for oral administration.

Route of Administration: Oral

In Vitro Use Guide

Fasoracetam (10(-7) and 10(-6) M) inhibited forskolin-stimulated cyclic AMP formation in cultured neurons of the mouse cerebral cortex. Conversely, in pertussis toxin-pretreated neurons, the drug (10(-7)-10(-5) M) significantly enhanced the forskolin-stimulated cyclic AMP formation, and this action was completely reversed by cholera toxin.

Name

Type

Language

NFC-1 ANHYDROUS

Preferred Name

English

FASORACETAM

Official Name

English

AEVI001

Code

English

(5R)-5-(PIPERIDINE-1-CARBONYL)PYRROLIDIN-2-ONE

Common Name

English

(5R)-5-(1-PIPERIDINYLCARBONYL)-2-PYRROLIDINONE

Common Name

English

LAM105 ANHYDROUS

Code

English

NFC1 ANHYDROUS

Code

English

LAM-105 ANHYDROUS

Code

English

NS-105

Code

English

(+)-1-(((R)-5-OXO-2-PYRROLIDINYL)CARBONYL)PIPERIDINE

Systematic Name

English

2-PYRROLIDINONE, 5-(1-PIPERIDINYLCARBONYL)-, (5R)-

Systematic Name

English

NS105

Code

English

fasoracetam [INN]

Common Name

English

AEVI-001

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C1509