AZ 12216052

Product NameAZ 12216052
CAS1290628-31-7
MFC19H22BrNOS
MW392.35308
EINECS
MOL File1290628-31-7.mol

Chemical Properties

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

Usage And Synthesis

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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