MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

NMDA receptor antagonist 2

CAS No. : 875898-41-2

MCE 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.

相关产品：Dizocilpine maleate  |  D-AP5  |  NMDA  |  CNQX  |  NBQX  |  Ifenprodil tartrate  |  L-Phenylalanine  |  Ibotenic acid  |  Kynurenic acid  |  Memantine hydrochloride  |  L-Glutamic acid monosodium salt  |  Quinolinic acid  |  Glycine  |  Ro 25-6981 Maleate  |  DNQX  |  D-Cycloserine  |  PEAQX tetrasodium hydrate  |  Transcrocetin  |  CX546  |  Traxoprodil  |  ZL006  |  Flupirtine Maleate  |  Cycloleucine  |  MDL-29951  |  Topiramate  |  (-)-Huperzine A  |  (S)-Willardiine  |  24-Hydroxycholesterol  |  Philanthotoxin 74 dihydrochloride

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。