Lanicemine (Synonyms: AZD 6765,AR-R 15896AR) |
| Catalog No.GC11124 |
voltage-dependent NMDA channel blocker
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 153322-05-5
Sample solution is provided at 25 µL, 10mM.
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IC50: 4-7 μM
Lanicemine is a NMDA channel blocker.
NMDA receptors, glutamate-gated cation channels with high calcium permeability, play critical roles in various aspects of the biology. They are important for the development of the CNS, generation of rhythms, and the processes underlying memory, learning, and neuroplasticity.
In vitro: Previous study with lanicemine and ketamine found that both compounds could bind with low-to-moderate affinity to sites within the NMDA channel pore, exhibit strong voltage dependence, and have similar lack of NR2A vs NR2B subunit selectivity [1].
In vivo: In animal study, cortical EEG recordings were obtained from rats trained to perform an auditory detection task for food reward. Results showed that both lanicemine and ketamine produced pronounced dose-dependent elevations in spontaneous gamma-band EEG, but only gamma changes for ketamine were tightly coupled to increases in locomotor activity, indicating that lanicemine not only engaged brain circuits involved in the generation of gamma-EEG, but also influenced these networks independent of the broader systemslevel disruptions typical of ketamine [1].
Clinical trial: A qEEG crossover study was conducted in healthy volunteers but was stopped earlier than planned following two serious adverse events occurring during ketamine infusion. Significant increases in gamma-band EEG were found for both lanicemine and ketamine, and baseline-corrected gamma-EEG following lanicemine treatment was statistically indistinguishable from ketamine. Moreover, both lanicemine and ketamine produced significant reductions in prefrontal theta-cordance. Furthermore, no serious adverse events were observed associated with lanicemine [1].
Reference:
[1] G. Sanacora, M. A. Smith, S. Pathak, et al. Lanicemine: A low-trapping NMDA channel blocker produces sustained antidepressant efficacy with minimal psychotomimetic adverse effects. Molecular Psychiatry 19(9), 978-985 (2014).
| Cas No. | 153322-05-5 | SDF | |
| Synonyms | AZD 6765,AR-R 15896AR | ||
| Chemical Name | (αS)-phenyl-2-pyridineethanamine | ||
| Canonical SMILES | N[C@H](C1=CC=CC=C1)CC2=CC=CC=N2 | ||
| Formula | C13H14N2 | M.Wt | 198.3 |
| Solubility | ≤20mg/ml in ethanol;30mg/ml in DMSO;5mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 5.0429 mL | 25.2143 mL | 50.4286 mL |
| 5 mM | 1.0086 mL | 5.0429 mL | 10.0857 mL |
| 10 mM | 0.5043 mL | 2.5214 mL | 5.0429 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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