| Identification | Back Directory | [Name]
AZ 12216052 | [CAS]
1290628-31-7 | [Synonyms]
AZ 12216052
AZ12216052 >=98% (HPLC)
2-[[(4-Bromophenyl)methyl]thio]-N-[4-(1-methylpropyl)phenyl]acetamide | [Molecular Formula]
C19H22BrNOS | [MDL Number]
MFCD20926426 | [MOL File]
1290628-31-7.mol | [Molecular Weight]
392.353 |
| Chemical Properties | Back Directory | [Boiling point ]
526.9±45.0 °C(Predicted) | [density ]
1.323±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble | [form ]
A crystalline solid | [pka]
13.70±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8). 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. 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. | [Uses]
AZ 12216052 is a positive allosteric modulator of mGluR8, which are attractive therapeutic targets for anxiety disorders. | [in vivo]
AZ 12216052 (10 mg/kg; i.p.; 2 h prior to testing) reduces measures of anxiety, without affecting the velocity of the mice[3].
AZ12216052 (10 mg/kg; i.p.; single dose) exhibits remaining anxiolytic effects, might involve mGluR4 in mGluR8 / mice, as the mGluR4 PAM (Positive Allosteric Modulator) VU 0155041 also reduces measures of anxiety in wild-type mice[4]. | Animal Model: | WT and Apolipoprotein E-deficient (Apoe?/?) mice (C57BL/6J, 2-month-old) in the elevated zero maze[3] | | Dosage: | 10 mg/kg | | Administration: | Intraperitoneal injection; singel dose, 2 h prior to testing | | Result: | Reduced measures of anxiety in the elevated zero maze without affecting the velocity of the mice.
Reduced the acoustic startle response. |
| [IC 50]
mGlu8 | [References]
[1] ROBERT M. DUVOISIN . Acute pharmacological modulation of mGluR8 reduces measures of anxiety[J]. Behavioural Brain Research, 2010, 212 2: Pages 168-173. DOI: 10.1016/j.bbr.2010.04.006
[2] D. JANTAS . Neuroprotective effects of metabotropic glutamate receptor group II and III activators against MPP(+)-induced cell death in human neuroblastoma SH-SY5Y cells: The impact of cell differentiation state[J]. Neuropharmacology, 2014, 83: Pages 36-53. DOI: 10.1016/j.neuropharm.2014.03.019 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|