A positive allosteric modulator of mGluR8; potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM); inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells at 0.001-1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM; increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response

AZ 12216052 – 5 mg

Brand:
Cayman
CAS:
1290628-31-7
Storage:
-20
UN-No:
De Minimis - 3077 / 9

AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8).{53273} It potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). In a cell-based model of Parkinson’s disease, AZ 12216052 inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM.{53274} AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively.{53273}  

 

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Description

A positive allosteric modulator of mGluR8; potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM); inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells at 0.001-1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM; increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response, avoidable and unavoidable anxiogenic stimuli, respectively, in mice at 10 mg/kg

Formal name: 2-[[(4-bromophenyl)methyl]thio]-N-[4-(1-methylpropyl)phenyl]-acetamide

Synonyms: 

Molecular weight: 392.4

CAS: 1290628-31-7

Purity: ≥98%

Formulation: A crystalline solid

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