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| Cas No.: | 1445605-23-1 |
| Chemical Name: | Lu AF21934 |
| Synonyms: | Lu AF21934;Lu-AF 21934;(1S,2R)-N1-(3,4-dichlorophenyl)cyclohexane-1,2-dicarboxamide;AM80972;(1R,2S)-2-N-(3,4-dichlorophenyl)cyclohexane-1,2-dicarboxamide |
| SMILES: | ClC1=C(C([H])=C([H])C(=C1[H])N([H])C([C@@]1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(N([H])[H])=O)=O)Cl |
| Formula: | C14H16Cl2N2O2 |
| M.Wt: | 315.1950 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4. |
| In Vivo: | Lu AF21934 treatment shows 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 the basal locomotor activity of mice that are not habituated to activity cages[1]. Lu AF21934 (0.5-5 mg/kg sc) does not influence tremor but at doses of 0.5 and 2.5 mg/kg reverses harmaline-induced hyperactivity. Lu AF21934 at a dose of 2.5 mg/kg potentiates the inhibitory influence of harmaline on the exploratory activity and AP1 during the first 30 min of the measurement and counteracts the harmaline-increased basic activity during the period of 30-90 min[2]. Lu AF21934 (0.1-5 mg/kg) dose-dependently inhibits hyperactivity induced by MK-801 or amphetamine. It also antagonizes head twitches and increases frequency of spontaneous excitatory postsynaptic currents in brain slices, induced by DOI[3]. |