ADX-47273 is a novel, potent and selective metabotropic glutamate receptor 5 allosteric modulator with an EC50 of 170 nM in human embryonic kidney 293 cells expressing rat mGlu5. ADX-47273 shifted mGlu5 receptor glutamate response curve to the left (9-fold at 1 μM) and competed for binding of [3H]2-methyl-6- (phenylethynyl) pyridine with a Ki of 4.3 μM in a dose-dependent manner, but not [3H]quisqualate. In vivo, ADX-47273 elevated extracellular signal-regulated kinase and cAMP-responsive element-binding protein phosphorylation in hippocampus and prefrontal cortex. In models sensitive to antipsychotic compound treatment, ADX-47273 decreased rat-conditioned avoidance responding [minimal effective dose (MED) = 30 mg/kg i.p.] and reduced mouse apomorphine-induced climbing (MED = 100 mg/kg i.p.), with little effect on stereotypy or catalepsy. Furthermore, ADX-47273 inhibited phencyclidine, apomorphine, and amphetamine-induced locomotor activities in mice and reduced extracellular levels of dopamine in the nucleus accumbens, but not in the striatum, in rats. In cognition models, ADX-47273 improved novel object recognition (MED = 1 mg/kg i.p.) and decreased impulsivity in the five-choice serial reaction time test (MED = 10 mg/kg i.p.) in rats.
Cell Experiment | |
---|---|
Cell lines | |
Preparation method | |
Concentrations | |
Incubation time |
Animal Experiment | |
---|---|
Animal models | male Long-Evans rats |
Formulation | sterile 0.9% sodium chloride solution |
Dosages | 10 mg/kg |
Administration | Inject intraperitoneally at a single dose30 min before sacrifice |
Molecular Weight | 369.36 |
Formula | C20H17F2N3O2 |
CAS Number | 851881-60-2 |
Solubility (25°C) | DMSO 70 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related GluR Products |
---|
PDZ1 Domain inhibitor peptide
PDZ1 Domain inhibitor peptide, a cyclic peptide, incorporates a β-Ala lactam side chain linker and targets the PDZ1 domains of the postsynaptic density protein 95 (PSD-95). |
CALP1
CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca2+-binding site. |
NT 13
NT 13 (TPPT) is a tetrapeptide having the amino acid sequence L-threonyl-L-prolyl-L-prolyl-L-threonine amide. |
Tat-NR2Baa
Tat-NR2BAA is the control peptide of Tat-NR2B9c, inactive. |
VSGLNPSLWSIFGLQFILLWLVSGSRHYLW
VSGLNPSLWSIFGLQFILLWLVSGSRHYLW is a 30-amino-acid peptide mimicking the C-terminal domain of α2δ-1, termed as α2δ-1Tat peptide. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.