Lu AF21934

Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor.

Product information

CAS Number: 1445605-23-1

Molecular Weight: 315.20

Formula: C14H16Cl2N2O2

Chemical Name: (1S,2R)-N1-(3,4-dichlorophenyl)cyclohexane-1,2-dicarboxamide

Smiles: NC(=O)[C@@H]1CCCC[C@@H]1C(=O)NC1=CC=C(Cl)C(Cl)=C1

InChiKey: AVKZWCJNDWOBAM-ZJUUUORDSA-N

InChi: InChI=1S/C14H16Cl2N2O2/c15-11-6-5-8(7-12(11)16)18-14(20)10-4-2-1-3-9(10)13(17)19/h5-7,9-10H,1-4H2,(H2,17,19)(H,18,20)/t9-,10+/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 80 mg/mL (253.81 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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. 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.

References:

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.

Products are for research use only. Not for human use.