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Cat. No.: HY-136459

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NMDA receptor antagonist 2

NMDA receptor antagonist 2 is a potent and orally active NR2B subtype-selective NMDA antagonist with an IC₅₀ and a K_i of 1.0 nM and 0.88 nM, respectively. NMDA receptor antagonist 2 is used for the study of neuropathic pain and Parkinson’s disease.

For research use only. We do not sell to patients.

CAS No.: 875898-41-2
Formula: C₂₀H₂₁N₇O
Molecular Weight:375.43

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

NMDA receptor antagonist 2 Chemical Structure

CAS No.: 875898-41-2

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vivo
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

NMDA Receptor

All iGluR Isoforms :

In Vitro

NMDA receptor antagonist 2 leads to excellent potency at NR2B (K_i=0.88 nM) and selectivity over hERG binding (IP=20000 nM). NMDA receptor antagonist 2 is evaluated in a functional assay measuring Ca₂₊ flux in cells expressing recombinant NR1/NR2B receptors. Selectivity over the hERG-channel is evaluated in an MK-499-binding assay^[1].
NMDA receptor antagonist 2 is highly potent in a functional assay using cells expressing NR2B (IC₅₀=1.0 nM) and remains equipotent in a binding assay using a sample of homogenized human temporal cortex (K_i=0.81 nM). In an electrophysiology assay using NR2B receptors, Compound 22 shows full blockade of ion flux with K_D=0.35 nM. Compound 22 also exhibits high levels of selectivity over NR2A (IC₅₀=200 μM), hERG binding (IP=20 μM), α-adrenergic receptors based on Prazosin binding (IC₅₀>100 μM), and CYP P450s including CYP3A4, 2C9, and 2D6^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In pharmacokinetic studies with higher species, NMDA receptor antagonist 2 shows excellent oral bioavailability (F=83%), half-life (T_1/2=7.5 hours) and clearance (CL=3.6 mL/min/kg) in dog. And it exhibits moderate clearance (CL=12 mL/min/kg) and oral bioavailability (F=17%) in rhesus, the half-life (T_1/2) is 1.5 hours^[1].
In a rat pharmacokinetic study, NMDA receptor antagonist 2 shows oral bioavailability (F=23 %), half-life (T_1/2=0.7 hours) and clearance (CL=24 mL/min/kg), the receptor occupancy ED₅₀ with oral administration is 4.8 mg/kg in rat^[1].
In the spinal nerve ligation model of neuropathic pain in rats, surgical ligation of two lumbar nerves in the spinal column induces a state of mechanical allodynia^[1].
NMDA receptor antagonist 2 (oral administration; 3-30 mg/kg) inhibits tactile allodynia in a dose-dependent manner after oral administration at 10 and 30 mg/kg. It produces an average improvement in the maximal possible effect of 15% (3 mg/kg), 41% (10 mg/kg), and 69% (30 mg/kg) compared to vehicle treated animals^[1].
NMDA receptor antagonist 2 (oral administration; 3-30 mg/kg) is efficacious in an acute rodent model of Parkinson’s disease. Haloperidol (HY-14538) is administered at a dose previously shown to elicit an acute cataleptic response in rats, compound 22 reduces catalepsy scores in a dose-dependent manner, producing average improvements of 34% (3 mg/kg), 86% (10 mg/kg), and 92% (30 mg/kg) when it compares to vehicle group^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 875898-41-2
Molecular Weight 375.43
Formula C₂₀H₂₁N₇O
SMILES

CC1=CC=C(CC2=NOC([C@@H]3C[C@@H](NC4=C5C(NN=C5)=NC=N4)CC3)=N2)C=C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

View the Complete Stock Solution Preparation Table

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

Compound?22?is dissolved in 1% methylcellulose and orally administered via gavage^[1].

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Mark E Layton, et al. Discovery of 3-substituted Aminocyclopentanes as Potent and Orally Bioavailable NR2B Subtype-Selective NMDA Antagonists. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vivo
Purity & Documentation
References

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NMDA receptor antagonist 2

All iGluR Isoforms