| Bioactivity | Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor[1]. | ||||||||||||
| 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]. | ||||||||||||
| Name | Lu AF21934 | ||||||||||||
| CAS | 1445605-23-1 | ||||||||||||
| Formula | C14H16Cl2N2O2 | ||||||||||||
| Molar Mass | 315.20 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Anna Sławińska, et al. Anxiolytic- but not antidepressant-like activity of Lu AF21934, a novel, selective positive allosteric modulator of the mGlu? receptor. Neuropharmacology. 2013 Mar;66:225-35. [2]. Ossowska K, et al. Lu AF21934, a positive allosteric modulator of mGlu4 receptors, reduces the harmaline-induced hyperactivity but not tremor in rats. Neuropharmacology. 2014 Aug;83:28-35. [3]. Anna Sławińska, et al. The antipsychotic-like effects of positive allosteric modulators of metabotropic glutamate mGlu4 receptors in rodents. Br J Pharmacol. 2013 Aug;169(8):1824-39. |
Lu AF21934
CAS: 1445605-23-1 F: C14H16Cl2N2O2 W: 315.20
Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mG
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