A positive allosteric modulator of mGluR5 (EC50s = 0.17 and 0.23 μM for potentiation of glutamate activity in HEK293 cells expressing rat mGluR5 and primary astrocyte cultures

ADX-47273 – 10 mg

Brand:
Cayman
CAS:
851881-60-2
Storage:
-20
UN-No:
De Minimis - 3077 / 9

ADX-47273 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) with EC50 values of 0.17 and 0.23 μM for potentiation of glutamate activity in HEK293 cells expressing rat mGluR5 and primary astrocyte cultures, respectively.{37446} It is selective for mGluR5 over rat mGluR1 and human mGluR1 and mGluR4 when used at concentrations up to 10 μM. In vivo, ADX-47273 (1 and 10 mg/kg, i.p.) increases ERK and CREB phosphorylation in the hippocampus and prefrontal cortex in rats. It decreases the conditioned avoidance response, apomorphine-induced climbing, as well as PCP-, apomorphine-, and amphetamine-induced locomotor activity in rats in a dose-dependent manner, indicating antipsychotic-like activity. ADX-47273 (0.1-50 mg/kg, i.p) improves recall in a novel object recognition test and reduces impulsivity in the 5-choice serial reaction time task (5CSRTT). It also enhances reversal learning in mice in the Morris water maze test.{37447}  

 

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Description

A positive allosteric modulator of mGluR5 (EC50s = 0.17 and 0.23 μM for potentiation of glutamate activity in HEK293 cells expressing rat mGluR5 and primary astrocyte cultures, respectively); selective for mGluR5 over rat mGluR1 and human mGluR1 and mGluR4 at 10 μM; decreases the conditioned avoidance response, apomorphine-induced climbing, as well as PCP-, apomorphine-, and amphetamine-induced locomotor activity in rats in a dose-dependent manner; improves recall in a novel object recognition test and reduces impulsivity in the 5CSRTT from 0.1-50 mg/kg; enhances reversal learning in mice in the Morris water maze test,

Formal name: (4-fluorophenyl)[(3S)-3-[3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl]-1-piperidinyl]-methanone

Synonyms: 

Molecular weight: 369.4

CAS: 851881-60-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Allosteric Modulators||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Behavioral Neuroscience|Schizophrenia & Psychosis

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