ADX-47273 Property

Boiling point:

540.8±60.0 °C(Predicted)

Density 

1.311

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

form 

Powder

pka

-0.83±0.44(Predicted)

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

ADX-47273 Chemical Properties,Usage,Production

Description

ADX-47273 is a positive allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) with EC₅₀ values of 0.17 and 0.23 μM for potentiation of glutamate activity in HEK293 cells expressing rat mGluR5 and primary astrocyte cultures, respectively. It is selective for mGluR5 over rat mGluR1 and human mGluR1 and mGluR4 when used at concentrations up to 10 μM. In vivo, ADX-47273 (1 and 10 mg/kg, i.p.) increases ERK and CREB phosphorylation in the hippocampus and prefrontal cortex in rats. It decreases the conditioned avoidance response, apomorphine-induced climbing, as well as PCP-, apomorphine-, and amphetamine-induced locomotor activity in rats in a dose-dependent manner, indicating antipsychotic-like activity. ADX-47273 (0.1-50 mg/kg, i.p) improves recall in a novel object recognition test and reduces impulsivity in the 5-choice serial reaction time task (5CSRTT). It also enhances reversal learning in mice in the Morris water maze test.

in vivo

adx47273 increased erk (extracellular signal-regulated kinase) and creb (camp-responsive element-binding protein) phosphorylation in rat hippocampus and prefrontal cortex. in rat and mouse models that sensitive to antipsychotic treatment, adx47273 decreased rat conditioned avoidance responding (minimal effective dose = 30 mg/kg i.p.) and reduced mouse ampomorphine-activated climbing (minimal effective dose = 100 mg/kg i.p.) [1]

References

[1] liu f, grauer s, kelley c, navarra r, graf r, zhang g, atkinson pj, popiolek m, wantuch c, khawaja x, smith d, olsen m, kouranova e, lai m, pruthi f, pulicicchio c, day m, gilbert a, pausch mh, brandon nj, beyer ce, comery ta, logue s, rosenzweig-lipson s, marquis kl. adx47273 [s-(4-fluoro-phenyl)-{3-[3-(4-fluoro-phenyl)-[1,2,4]-oxadiazol-5-yl]-piperidin-1-yl}-methanone]: a novel metabotropic glutamate receptor 5-selective positive allosteric modulator with preclinical antipsychotic-like and precognitive activities. j pharmacol exp ther. 2008 dec;327(3):827-39.