NMDA receptor antagonist 2

价格询价

品牌MedChemExpress(MCE)
产地美国
货号HY-136459
更新日期2025年07月11日

MedChemExpress LLC

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NMDA receptor antagonist 2

CAS No. : 875898-41-2

MCE 国际站：NMDA receptor antagonist 2

产品活性：NMDA receptor antagonist 2 是一种有效的口服 NR2B 亚型选择性 NMDA 拮抗剂，其 IC₅₀ 和 K_i 分别为 1.0 nM 和 0.88 nM。NMDA receptor antagonist 2 用于神经性疼痛与帕金森病的研究。

研究领域：Membrane Transporter/Ion Channel | Neuronal Signaling

作用靶点：iGluR

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.
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.

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.
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.
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.
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.
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.