A group II mGluR agonist (Kis = 99 and 94 nM

LY354740 – 10 mg

Brand:
Cayman
CAS:
176199-48-7
Storage:
-20
UN-No:
Non-Hazardous - /

LY354740 is an agonist of the group II metabotropic glutamate receptor (mGluR) subtypes mGluR2 and mGluR3 (Kis = 99 and 94 nM, respectively).{32438} It inhibits forskolin-stimulated cAMP accumulation in cells expressing human mGluR2 and mGluR3 (EC50s = 5.1 and 24.3 nM, respectively) and is selective for mGluR2 and mGluR3 over mGluR4, mGluR7, mGluR1a, and mGluR5a (EC50s = >100 µM).{38897,34626} LY354740 suppresses electrically stimulated excitatory postsynaptic potentials (EPSPs) in rat striatal neurons (EC50 = 20 nM) and excitatory postsynaptic currents (EPSCs) induced by serotonin (Item No. 14332) in rat medial prefrontal cortex in vitro (EC50 = 89.1 nM).{32438,38898} LY354740 (5 mM) iontophoretically ejected into the ventrobasal thalamus of rats reduces sensory inhibition by 20% compared to control in an alternating test, condition-test paradigm.{31730} It attenuates the effects of PCP on working memory, stereotypy, locomotion, and cortical glutamate efflux in a rat model of schizophrenia when administered at a dose of 10 mg/kg.{38899} LY354740 also shows efficacy in animal models of anxiety, epilepsy, and withdrawal from nicotine and morphine.{32438,21635}  

 

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Description

A group II mGluR agonist (Kis = 99 and 94 nM, respectively); inhibits forskolin-stimulated cAMP accumulation in cells expressing human mGluR2 and mGluR3 (EC50s = 5.1 and 24.3 nM, respectively); highly selective for mGluR2 and mGluR3 over mGluR4, mGluR7, mGluR1a, and mGluR5a (EC50s = >100 µM); suppresses electrically stimulated EPSPs in rat striatal neurons in vitro (EC50 = 20 nM); suppresses serotonin-induced EPSCs in rat medial prefrontal cortex in vitro (EC50 = 89.1 nM); attenuates the effects of PCP on working memory, stereotypy, locomotion, and cortical glutamate efflux in a rat model of schizophrenia (10 mg/kg); shows efficacy in animal models of anxiety, epilepsy, and withdrawal from nicotine and morphine

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

Synonyms: 

Molecular weight: 185.2

CAS: 176199-48-7

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||Research Area|Neuroscience|Seizure Disorders

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