An mGluR5 PAM; induces calcium mobilization in HEK293 cells expressing human mGluR5 (EC50 = 260 nM); selective for mGluR5 over mGluR1-4 and mGluR6-8 at 10 μM; reverses amphetamine-induced hyperlocomotion in rats (ED50 = 23 mg/kg)

VU0409551 – 1 mg

Brand:
Cayman
CAS:
1363281-27-9
Storage:
-20
UN-No:
Non-Hazardous - /

VU0409551 is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 5 (mGluR5).{29045} It induces calcium mobilization in HEK293 cells expressing human mGluR5 (EC50 = 260 nM). It is selective for mGluR5 over mGluR1-4 and mGluR6-8 at 10 μM. VU0409551 reverses amphetamine-induced hyperlocomotion in rats (ED50 = 23 mg/kg), indicating antipsychotic-like activity.{29045} It increases levels of c-fos and expression of BDNF, Arc/Arg3.1, syntaxin 1A, and post-synaptic density-95 (PSD-95) in the hippocampus in the BACHD mouse model of Huntington’s disease when administered at a dose of 3 mg/kg.{48494} VU0409551 (3 mg/kg) also improves object location memory in the novel object location test and associative memory in the cued fear conditioning test in the BACHD mouse model.  

 

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Description

An mGluR5 PAM; induces calcium mobilization in HEK293 cells expressing human mGluR5 (EC50 = 260 nM); selective for mGluR5 over mGluR1-4 and mGluR6-8 at 10 μM; reverses amphetamine-induced hyperlocomotion in rats (ED50 = 23 mg/kg), indicating antipsychotic-like activity; increases levels of c-fos and expression of BDNF, Arc/Arg3.1, syntaxin 1A, and PSD-95 in the hippocampus in the BACHD mouse model of Huntington’s disease at 3 mg/kg; improves object location memory in the novel object location test and associative memory in the cued fear conditioning test in the BACHD mouse model at 3 mg/kg

Formal name: [6,7-dihydro-2-(phenoxymethyl)oxazolo[5,4-c]pyridin-5(4H)-yl](4-fluorophenyl)-methanone

Synonyms:  JNJ-46778212

Molecular weight: 352.4

CAS: 1363281-27-9

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||Research Area|Neuroscience|Neurodegenerative Disorders|Huntington’s Disease

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