1198309-73-7
Chemical Structure
AZD-8418
- CAS No.: 1198309-73-7
- Formula:C19H20ClN3O3
- Molecular Weight:373.84
IUPAC Name: (S)-5-(7-chloro-2-(1-cyclopropylethyl)-1-oxoisoindolin-5-yl)-N,N-dimethylisoxazole-3-carboxamide
InChIKey: MCPBSUCAISQZQK-JTQLQIEISA-N
SMILES: O=C1C=2C(CN1[C@@H](C)C3CC3)=CC(=CC2Cl)C4=CC(C(N(C)C)=O)=NO4
Biological Activity: AZD-8418 is an orally active positive allosteric modulator of metabotropic glutamate receptor 2 (mGluR2), with an EC50 of 0.86 μM for rat mGlu2 receptors. AZD-8418 reduces the in vitro binding level of [3H]AZ12559322 in prefrontal cortex brain tissues of non-human primates. AZD8418 enhances the inhibitory effect of the mGlu2/3 agonist DCG-IV (HY-101335) on field excitatory postsynaptic potentials (fEPSP) in rat hippocampal brain slices. AZD-8418 reduces nicotine self-administration behavior in rats, and blocks cue-induced reinstatement of nicotine-seeking and food-seeking behaviors. The attenuating effect on nicotine self-administration behavior develops rapid tolerance, while inhibition of food self-administration behavior requires chronic administration. AZD-8418 can be used in research related to nicotine dependence and neuropsychiatric disorders[1][2].
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AZD-8418 | AZD-8418 is an orally active positive allosteric modulator of metabotropic glutamate receptor 2 (mGluR2), with an EC50 of 0.86 μM for rat mGlu2 receptors. AZD-8418 reduces the in vitro binding level of [3H]AZ12559322 in prefrontal cortex brain tissues of non-human primates. AZD8418 enhances the inhibitory effect of the mGlu2/3 agonist DCG-IV (HY-101335) on field excitatory postsynaptic potentials (fEPSP) in rat hippocampal brain slices. AZD-8418 reduces nicotine self-administration behavior in rats, and blocks cue-induced reinstatement of nicotine-seeking and food-seeking behaviors. The attenuating effect on nicotine self-administration behavior develops rapid tolerance, while inhibition of food self-administration behavior requires chronic administration. AZD-8418 can be used in research related to nicotine dependence and neuropsychiatric disorders. | |||||||||||||||||||||
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- [1]. Li Y, et al. Radiosynthesis and Evaluation of 11C-Labeled Isoindolone-Based Positive Allosteric Modulators for Positron Emission Tomography Imaging of Metabotropic Glutamate Receptor 2. ACS pharmacology & translational science. 2024 Aug 09;7(8):2414-2423. [Content Brief]
- [2]. Li X, et al. Attenuation of nicotine-taking and nicotine-seeking behavior by the mGlu2 receptor positive allosteric modulators AZD8418 and AZD8529 in rats. Psychopharmacology. 2016 May;233(10):1801-14.
Keywords
