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| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2 , with an EC 50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1 , 3, 4, 5, 6, 7, and 8 subtypes.
In Vitro
AZD-8529 potentiates the effects of glutamate at mGluR2 with an EC 50 of 195 nM. AZD-8529 does not elicit antagonist responses on mGluRs at 25 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AZD-8529 (0.3-mg/kg, i.m.) reduces nicotine priming-induced and cue-induced reinstatement in squirrel monkeys . AZD-8529 (30 mg/kg; i.p.) decreases the increased extracellular dopamine induced by nicotine in accumbens shell of freely-moving rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sprague-Dawley rats Dosage: 10 mg/kg, 30 mg/kg Administration: Intraperitoneal injection; 2 hours before nicotine injections Result: Decreased the increased extracellular dopamine induced by nicotine (0.4 mg/kg, s.c.) in accumbens shell of freely-moving rats.
Form:Oil
IC50& Target:mGluR2 285 nM (EC 50 )
Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| Classe | Isoindoles and derivatives |
| Subclass | Isoindolines |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Isoindolones |
| Alternative Parents | Isoindoles Phenol ethers Phenoxy compounds Aralkylamines N-alkylpiperazines Heteroaromatic compounds 1,2,4-oxadiazoles Tertiary carboxylic acid amides Lactams Trihalomethanes Amino acids and derivatives Trialkylamines Oxacyclic compounds Dialkylamines Azacyclic compounds Organooxygen compounds Organofluorides Organic oxides Alkyl fluorides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Isoindolone - Isoindole - Phenoxy compound - Phenol ether - N-alkylpiperazine - Aralkylamine - Monocyclic benzene moiety - 1,4-diazinane - Piperazine - Benzenoid - 1,2,4-oxadiazole - Azole - Oxadiazole - Tertiary carboxylic acid amide - Heteroaromatic compound - Tertiary amine - Amino acid or derivatives - Tertiary aliphatic amine - Carboxamide group - Lactam - Trihalomethane - Secondary amine - Azacycle - Oxacycle - Carboxylic acid derivative - Secondary aliphatic amine - Hydrocarbon derivative - Organic oxide - Organic oxygen compound - Organohalogen compound - Organofluoride - Organonitrogen compound - Organic nitrogen compound - Alkyl fluoride - Amine - Organooxygen compound - Alkyl halide - Halomethane - Aromatic heteropolycyclic compound |
| Descrizione | This compound belongs to the class of organic compounds known as isoindolones. These are aromatic polycyclic compounds that an isoindole bearing a ketone. |
| External Descriptors | Not available |
| Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
|---|
| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
|---|
| Solubilità | DMSO : 62.5 mg/mL (128.21 mM; Need ultrasonic) |
|---|---|
| Peso molecolare | 487.500 g/mol |
| XLogP3 | 3.100 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 10 |
| Rotatable Bond Count | 6 |
| Exact Mass | 487.183 Da |
| Monoisotopic Mass | 487.183 Da |
| Topological Polar Surface Area | 83.700 Ų |
| Heavy Atom Count | 35 |
| Formal Charge | 0 |
| Complexity | 730.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 1 |
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