| Name | Lu AF21934 |
| Description | Lu AF21934 is a brain-penetrant and selective mGlu4 receptor positive allosteric modulator (IC50: 500 nM, human). |
| Kinase Assay | The receptor-expressing CHO cells are seeded into 24-well plates at a density of 4×104 cells/well and cultured for 1 day. The cells are then incubated with [5,6,8,9,11,12,14,15-3H]arachidonic acid (11 kBq/well) for 1 day and ished with DMEM supplemented with 20 mM HEPES and 0.2% BSA. The cells are then preincubated with the compounds (Sufugolix) at 37 °C for 60 min and the reaction is started by addition of LHRH (1 nM). After incubation at37 °C for 40 min, radioactivity in the medium is measured with a liquid scintillation counter[1]. |
| In vivo | Lu AF21934 treatment exhibits a dose-dependent anxiolytic-like effect in the stress-induced hyperthermia, four-plate, and marble-burying tests. The anti-hyperthermic effect of Lu AF21934 (5 mg/kg) in the SIH test is inhibited by the benzodiazepine receptor antagonist flumazenil (10 mg/kg) and is not serotonin-dependent. Lu AF21934 does not produce antidepressant-like effects in the tail suspension test in mice; however, it decreases basal locomotor activity in mice not habituated to activity cages. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.35 mM), Sonication is recommended.
DMSO : 16.67 mg/mL (52.89 mM), Sonication is recommended.
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| Keywords | mGluR4 | mGluR | Metabotropic glutamate receptors | Lu AF-21934 | Lu AF21934 | Lu AF 21934 | Inhibitor | inhibit |
| Inhibitors Related | S-Sulfo-L-cysteine sodium salt | IDRA-21 | Urethane | Decanoic Acid | DCB | L-Cysteic acid monohydrate | Evans blue | L-Glutamine | Direct Blue 1 | L-Glutamic acid monosodium salt | Memantine hydrochloride | O-Phospho-L-serine |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Glutamine Metabolism Compound Library | Neurotransmitter Receptor Compound Library | NO PAINS Compound Library | Bioactive Compounds Library Max |
United States
