Name | 2-[(4-Bromobenzyl)sulfanyl]-N-(4-sec-butylphenyl)acetamide |
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Description | 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]. |
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Related Catalog | |
Target |
mGlu8 |
In Vitro | 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]. Cell Viability Assay[2] Cell Line: UN- and RA-SH-SY5Y cells Concentration: 0.01-1 μM Incubation Time: 48 hours Result: Increased cell viability at 0.1 μM, and protected undifferentiated neuroblastoma cells against damaging effects of Iri or Cis. |
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. |
References |
Molecular Formula | C19H22BrNOS |
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Molecular Weight | 392.35300 |
Exact Mass | 391.06100 |
PSA | 54.40000 |
LogP | 5.90750 |
Symbol |
![]() GHS09 |
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Signal Word | Warning |
Hazard Statements | H410 |
Precautionary Statements | P273-P391-P501 |
RIDADR | UN 3077 9 / PGIII |