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Lu AF21934

Cat. No. M6071
Lu AF21934 Structure
Size Price Availability Quantity
5mg USD 85 In stock
10mg USD 145 In stock
25mg USD 320 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: 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.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Male Albino Swiss (20–25 g) mice
Formulation
Dosages 0.35 mg/kg
Administration s.c.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 315.2
Formula C14H16Cl2N2O2
CAS Number 1445605-23-1
Purity >99%
Solubility 80 mg/mL in DMSO
Storage at -20°C
References

The antipsychotic-like effects in rodents of the positive allosteric modulator Lu AF21934 involve 5-HT1A receptor signaling: mechanistic studies.
Wierońska JM, et al. Psychopharmacology (Berl). 2015 Jan;232(1):259-73. PMID: 25012236.

Inhibitory actions of mGlu4 receptor ligands on cocaine-, but not nicotine-, induced sensitizing and conditioning locomotor responses in rats.
Zaniewska M, et al. Pharmacol Rep. 2014 Apr;66(2):205-11. PMID: 24911071.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Lu AF21934 supplier, GluR, inhibitors

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