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VU 0361737 Sale

(Synonyms: ML-128) 目录号 : GC13962

A selective positive allosteric modulator of mGluR4

VU 0361737 Chemical Structure

Cas No.:1161205-04-4

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产品描述

VU0361737 is a selective, positive allosteric modulator and brain-permeable for mGLuR4 (mGlu4 receptor), (EC₅₀ = 240 and 110 nM for human and rat receptors respectively), >50 fold selectivity over other mGluR subtypes. Inactive at mGluR-1, mGluR-2, mGluR-3, mGluR-6 and mGluR-7 receptors and showed weak activity at mGluR-5 and mGluR-8 receptors. [1]

The mGluR (metabotropic glutamate receptor) is a group of G-protein coupled receptors and is active through an indirect metabotropic process. mGLuR4 are invoinved in Parkinson as it decrease GABAerigic transmission at inhibitory striato-pallidal synapse with the basal ganglia.[1][2]

Following the administration of VU0361737 into rat intraperitoneally (10mg/kg), the amount of compound present in brain and plasma was determined at 0.5, 1 and 8 hours. It showed a short half-life (T1/2 20 minutes) and a pronounced brain exposure (brain: plasma ratio = 4.1) [1]

References:
[1] Engers DW, Niswender CM, Weaver CD, Jadhav S, Menon UN, Zamorano R, Conn PJ, Lindsley CW, Hopkins CR.  Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).  J Med Chem. 2009 Jul 23;52(14):4115-8. 
[2] Engers DW, Field JR, Le U, Zhou Y, Bolinger JD, Zamorano R, Blobaum AL, Jones CK, Jadhav S, Weaver CD, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.  Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats.  J Med Chem.  2011 Feb 24;54(4):1106-10.

Chemical Properties

Cas No. 1161205-04-4 SDF
别名 ML-128
化学名 N-(4-chloro-3-methoxyphenyl)pyridine-2-carboxamide
Canonical SMILES COC1=C(C=CC(=C1)NC(=O)C2=CC=CC=N2)Cl
分子式 C13H11ClN2O2 分子量 262.69
溶解度 DMF: 50 mg/ml,DMSO: 50 mg/ml,DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml,Ethanol: 10 mg/ml 储存条件 Store at -20°C
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1 mM 3.8068 mL 19.0338 mL 38.0677 mL
5 mM 0.7614 mL 3.8068 mL 7.6135 mL
10 mM 0.3807 mL 1.9034 mL 3.8068 mL
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