Lu AF21934

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Lu AF21934 是一种脑渗透性、选择性 mGlu4 受体正变构调节剂（IC50：500 nM，人）。

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.

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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.

Lu AF21934 | Lu AF-21934 | Lu AF 21934

Angiogenesis

ALK

mGluR4

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1445605-23-1

315.2

C14H16Cl12N2O2

>98% (HPLC)

DMSO : ≥ 80 mg/mL. 253.81 mM

C1CC[C@@H]([C@@H](C1)C(=O)N)C(=O)Nc1cc(c(cc1)Cl)Cl

(1S,2R)-N1-(3,4-Dichlorophenyl)cyclohexane-1,2-dicarboxamide

(-20℃)

With Ice Pack

≥ 2 years