AZ 12216052

• CAT Number: I003365
• CAS Number: 1290628-31-7
• Molecular Formula: C19H22BrNOS
• Molecular Weight: 392.35
• Purity: ≥95%
• Synonyms: 2-[(4-bromophenyl)methylsulfanyl]-N-(4-butan-2-ylphenyl)acetamide
• InChI: InChI=1S/C19H22BrNOS/c1-3-14(2)16-6-10-18(11-7-16)21-19(22)13-23-12-15-4-8-17(20)9-5-15/h4-11,14H,3,12-13H2,1-2H3,(H,21,22)
• InChIKey: QKUYZJOTWYRWNF-UHFFFAOYSA-N
• SMILES: CCC(C)C1=CC=C(C=C1)NC(=O)CSCC2=CC=C(C=C2)Br

AZ 12216052 is a mGluR8 positive allosteric modulator, and helps mGluR8 modulate signaling inputing to retinal ganglion cells. AZ 12216052 exhibits antianxiety effect[1][2][3][4].
mGluR8 may modulates the synaptic inputs to retinal ganglion cells[1].
AZ 12216052 (10 μM) enhances the peak excitatory currents of ON-, OFF- currents in ON-OFF-ganglion cells, with a dependent way on the intensity of the light stimuli[1].
AZ 12216052 shows impact of cell differentiation and (0.01-1 μM; 24-48 h) reduces Dox-induced human neuroblastoma SH-SY5Y cell damage partially[2].
AZ 12216052 stimulates proliferation and attenuates staurosporine (St)- and doxorubicin (Dox)-induced toxicity in UN-SH-SY5Y cells[2].
AZ12216052 (10 μM) enhances glutamate activity of human mGluR8b receptor expressed in GHEK cells[3].
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].

Reference

[1]. Reed BT, et al. Differential modulation of retinal ganglion cell light responses by orthosteric and allosteric metabotropic glutamate receptor 8 compounds. Neuropharmacology. 2013 Apr;67:88-94.
 [Content Brief]

[2]. Jantas D, et al. Allosteric and Orthosteric Activators of mGluR8 Differentially Affect the Chemotherapeutic-Induced Human Neuroblastoma SH-SY5Y Cell Damage: The Impact of Cell Differentiation State. Basic Clin Pharmacol Toxicol. 2018 Oct;123(4):443-451.
 [Content Brief]

[3]. Duvoisin RM, et al. Acute pharmacological modulation of mGluR8 reduces measures of anxiety. Behav Brain Res. 2010 Oct 15;212(2):168-73.
 [Content Brief]

[4]. Duvoisin RM, et al. Opposing roles of mGluR8 in measures of anxiety involving non-social and social challenges. Behav Brain Res. 2011 Aug 1;221(1):50-4.
 [Content Brief]