Lu AF21934 Property

Boiling point:

577.6±50.0 °C(Predicted)

Density 

1.386±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≥31.5 mg/mL in DMSO; insoluble in H2O; ≥5.03 mg/mL in EtOH with ultrasonic

form 

solid

pka

13.23±0.70(Predicted)

color 

White to off-white

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

Lu AF21934 Chemical Properties,Usage,Production

Biological Activity

ec50: 500 nmlu af21934 is a positive allosteric modulator of mglu4 receptors.the mglu4 receptor subtype of the group iii mglu is mainly a presynaptic auto- or hetero-receptor. its stimulation results in an inhibition of glutamatergic or gabaergic transmission and release

in vitro

lu af21934 has been identified as a brain-penetrating positive allosteric modulator of mglu4 receptors. in broad in-vitro screens, lu af21934 could potentiate the glutamate response at the mglu4 receptor with an emax=120% and a glutamate fold-shift fs=5. lu af21934 did not showed any significant affinity for 70 gpcrs at 10 μm, but acted as a weak positive allosteric modulator of mglu6 receptor, as well as an antagonist of adenosine a2a and 5-ht2b receptors [1].

in vivo

in rats, harmaline triggered tremor as manifested by an increase in the power within 9-15hz band and in the tremor index. harmaline also induced a biphasic effect on mobility, initially inhibiting the exploratory locomotor activity of rats, followed by an increase in their basic activity. lu af21934 at 0.5-5 mg/kg sc did not influence tremor but at doses of 0.5 and 2.5 mg/kg reversed harmaline-induced hyperactivity. mglu4 mrna expression was found to be high in the cerebellar cortex and low in the inferior olive [1].

target

mGlu4 Receptor 500 nM (EC 50 )

References

[1] ossowska k,wardas j,berghauzen-maciejewska 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.