A positive allosteric modulator of mGluR4
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Lu AF21934

Item No. 27045

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N1-(3,4-dichlorophenyl)-1S,2R-cyclohexanedicarboxamide
CAS Number
1445605-23-1
Molecular Formula
C14H16Cl2N2O2
Formula Weight
315.2
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml
λmax
211, 252 nm
SMILES
O=C(NC1=CC(Cl)=C(Cl)C=C1)[C@@H]2[C@H](C(N)=O)CCCC2
InChi Code
InChI=1S/C14H16Cl2N2O2/c15-11-6-5-8(7-12(11)16)18-14(20)10-4-2-1-3-9(10)13(17)19/h5-7,9-10H,1-4H2,(H2,17,19)(H,18,20)/t9-,10+/m1/s1
InChi Key
AVKZWCJNDWOBAM-ZJUUUORDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $130

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    10 mg

    $236

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    25 mg

    $527

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    Product Description

    Lu AF21934 is a positive allosteric modulator (PAM) of metabotropic glutamate receptor 4 (mGluR4; EC50 = 500 nM for the human receptor in a FLIPR assay).1 It is selective for mGluR4 over mGluR6 (EC50 = 7 μM) and a panel of 73 CNS ion channels, G protein-coupled receptors (GPCRs), and enzymes at 10 μM. Lu AF21934 (12 mg/kg) reduces marble burying behavior and stress-induced hyperthermia in mice, indicating anxiolytic-like activity, but also reduces locomotor activity. It inhibits MK-801- and amphetamine-induced hyperactivity in mice and prevents MK-801-induced decreases in social interaction in rats.2 Lu AF21934 (0.5 and 2.5 mg/kg) also reduces harmaline-induced hyperactivity, but not tremor, in rats.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Sławińska, A., Wierońska, J.M., Stachowicz, K., et al. Anxiolytic- but not antidepressant-like activity of Lu AF21934, a novel, selective positive allosteric modulator of the mGlu4 receptor. Neuropharmacology 66, 225-235 (2013).

    2. Sławińska, A., Wierońska, J.M., Stachowicz, K., et al. The antipsychotic-like effects of positive allosteric modulators of metabotropic glutamate mGlu4 receptors in rodents. Br. J. Pharmacol. 169(8), 1824-1839 (2013).

    3. 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 83, 28-35 (2014).