ADX-47273
Synonym(s):(4-Fluorophenyl)[(3S)-3-[3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl]-1-piperidinyl]methanone;(S)-(4-Fluorophenyl)-{3-[3-(4-fluorophenyl)-[1,2,4]oxadiazol-5-yl]-piperidin-1-yl}-methanone;ADX 47273;ADX47273
- CAS NO.:851881-60-2
- Empirical Formula: C20H17F2N3O2
- Molecular Weight: 369.36
- MDL number: MFCD17167026
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-19 20:33:22
What is ADX-47273?
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.
What are the applications of Application
ADX-47273 is potent and selective metabotropic glutamate receptor 5 allosteric modulator
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.
Properties of ADX-47273
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) |
color | White to off-white |
Safety information for ADX-47273
Computed Descriptors for ADX-47273
New Products
4-Aminotetrahydropyran-4-carbonitrile Hydrochloride (R)-3-Aminobutanenitrile Hydrochloride 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-(Dimethylamino)tetrahydro-2H-pyran-4-carbonitrile 3-((Dimethylamino)methyl)-5-methylhexan-2-one oxalate 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine Nimesulide BP Aceclofenac IP/BP/EP Diclofenac Sodium IP/BP/EP/USP Mefenamic Acid IP/BP/EP/USP Ornidazole IP Diclofenac Potassium SODIUM AAS SOLUTION ZINC AAS SOLUTION BUFFER SOLUTION PH 10.0(BORATE) GOOCH CRUCIBLE SINTERED AQUANIL 5 BERYLLIUM AAS SOLUTION 2-Bromo-1-(bromomethyl)-3-chloro-5-nitrobenzene 2-Bromo-3-nitroaniline N-(3-Hydroxypropyl)-N-methylacetamide 3-Bromo-6-chloropyridazine 4-ethyl-3-nitrobenzoic acidRelated products of tetrahydrofuran
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