Lu AF21934

SKU: orb1223299

Description

Lu AF21934 is a positive allosteric modulator of mGlu4 receptors. Lu AF21934 reduces the harmaline-induced hyperactivity but not tremor in rats. The actions of Lu AF21934 are 5-HT1A receptor-dependent. Activation of the mGlu4 receptor may be a promising mechanism for the development of novel antipsychotic drugs, efficacious toward positive, negative, and cognitive symptoms.

Key Properties

• CAS Number: 1445605-23-1
• MW: 315.2
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₆Cl₁₂N₂O₂
• SMILES: C1CC[C@@H]([C@@H](C1)C(=O)N)C(=O)Nc1cc(c(cc1)Cl)Cl
• Target: ALK
• Solubility: DMSO : ≥ 80 mg/mL. 253.81 mM

Bioactivity

• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Lu AF21934 | Lu AF-21934 | Lu AF 21934

Quick Database Links

Gene Symbol

ALK