| Identification | Back Directory | [Name]
Lu AF21934 | [CAS]
1445605-23-1 | [Synonyms]
CS-2215
Lu AF21934
LuAF21934, >98%
LU-AF 21934;LU AF 21934
LU AF-21934;LU AF 21934;LU-AF21934;LU-AF-21934
(1S,2R)-N1-(3,4-Dichlorophenyl)-1,2-cyclohexanedicarboxamide
1,2-Cyclohexanedicarboxamide, N1-(3,4-dichlorophenyl)-, (1S,2R)-
2-PYRIMIDINAMINE,4-METHYL-N-[5-METHYL-4-(1H-PYRAZOL-4-YL)-2-THIAZOLYL]-, >98% | [Molecular Formula]
C14H16Cl2N2O2 | [MDL Number]
MFCD22576450 | [MOL File]
1445605-23-1.mol | [Molecular Weight]
315.2 |
| Chemical Properties | Back Directory | [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 Information | Back Directory | [Uses]
Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM for mGlu4 receptor[1]. | [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 ) | | [IC 50]
mGlu4 Receptor: 500 nM (EC50) | [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. |
|
|