ADX-47273

Bezeichnung:ADX-47273

CAS-Nr851881-60-2

Englisch Name:ADX-47273

CBNumberCB72546765

SummenformelC20H17F2N3O2

Molgewicht369.36

MOL-Datei851881-60-2.mol

ADX-47273 physikalisch-chemischer Eigenschaften

Siedepunkt	540.8±60.0 °C(Predicted)
Dichte	1.311
storage temp.	Store at -20°C
Löslichkeit	Soluble in DMSO
Aggregatzustand	Powder
pka	-0.83±0.44(Predicted)
Farbe	White to off-white

Gefahreninformationscode (GHS)

ADX-47273 Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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]
Einzelnachweise
[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.

ADX-47273 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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