A potent agonist of mGluR2 and mGluR3 (Kis = 149 and 62 nM

LY404039 – 25 mg

Brand:
Cayman
CAS:
635318-11-5
Storage:
-20
UN-No:
Non-Hazardous - /

LY404039 is a potent agonist of metabotropic glutamate (mGlu) group II receptors mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively, for recombinant human isoforms).{32438} It displays 100-fold selectivity for mGluR2/3 over ionotropic glutamate receptors, glutamate transporters, and several other receptors targeted by known anxiolytic and antipsychotic medications.{32438} LY404039 inhibits the binding of domperidone (Item No. 18875) by 15.5% to dopamine D2 receptors (Kd = ~10 nM in vitro), indicating interaction with this receptor.{32439} LY404039 is orally bioavailable and demonstrates antipsychotic and anxiolytic efficacy in several animal models.{32437}  

 

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Description

A potent agonist of mGluR2 and mGluR3 (Kis = 149 and 62 nM, respectively); demonstrates antipsychotic and anxiolytic efficacy in several animal models

Formal name: (1R,​4S,​5S,​6S)​-4-​amino-2-​thiabicyclo[3.1.0]​hexane-​4,​6-​dicarboxylic acid 2,​2-​dioxide

Synonyms: 

Molecular weight: 235.2

CAS: 635318-11-5

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience|Behavioral Neuroscience|Anxiety||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis

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