Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C13H14N2 |
Molecular Weight | 198.2637 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
N[C@@H](CC1=CC=CC=N1)C2=CC=CC=C2
InChI
InChIKey=FWUQWDCOOWEXRY-ZDUSSCGKSA-N
InChI=1S/C13H14N2/c14-13(11-6-2-1-3-7-11)10-12-8-4-5-9-15-12/h1-9,13H,10,14H2/t13-/m0/s1
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/23206319
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23206319
Lanicemine is a low-trapping NMDA channel blocker, which was developed by Fisons Pharmaceuticals and later by AstraZeneca for the treatment of the major depressive disorder. The development was terminated in phase II as the drug did not meet the primary endpoint.
CNS Activity
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL2094124 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23206319 |
0.56 µM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
1.3 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25259653/ |
150 mg single, intravenous dose: 150 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
LANICEMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
17.9 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25259653/ |
150 mg single, intravenous dose: 150 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
LANICEMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
16.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25259653/ |
150 mg single, intravenous dose: 150 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
LANICEMINE plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
PubMed
Title | Date | PubMed |
---|---|---|
Tolerability of the low-affinity, use-dependent NMDA antagonist AR-R15896AR in stroke patients: a dose-ranging study. | 2001 Feb |
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Structural modifications to an N-methyl-D-aspartate receptor antagonist result in large differences in trapping block. | 2001 Jun |
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Assessment of cognitive and motor deficits in a marmoset model of stroke. | 2003 |
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Comparison of the neuroprotective effect of clomethiazole, AR-R15896AR and NXY-059 in a primate model of stroke using histological and behavioural measures. | 2003 May 16 |
|
NXY-059: a hopeful sign in the treatment of stroke. | 2006 Oct |
Patents
Sample Use Guides
50-150 mg of the drug is given as a single intravenous (iv) infusion over 60 minutes.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/7595504
Rat cortical neurons were exposed to NMDA (50 uM) or glutamate (50 uM) for 15 min, the treatment resulted in the death of 85-95% of the neurons during the next 24 h. Lanicemine inhibited the neurotoxicity at 50 uM, prevented the loss of membrane-associated protein kinase C activity and reduced by approximately 35% the magnitude of NMDA-triggered increases in intracellular free Ca2+ concentration in the cortical cultures.
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C1509
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ACTIVE MOIETY
SALT/SOLVATE (PARENT)