VU0155041||VU0155041|mGlu4 modulator

Cas No.:	1093757-42-6
Chemical Name:	cis-2-[[(3,5-Dichlorophenyl)amino]carbonyl]cyclohexanecarboxylic acid
Synonyms:	VU0155041,VU-0155041
SMILES:	O=C([C@H](CCCC1)[C@H]1C(O)=O)NC2=CC(Cl)=CC(Cl)=C2
Formula:	C₁₄H₁₅Cl₂NO₃
M.Wt:	316.18
Purity:	>98%
Sotrage:	4°C for 1 year, -20°C for more than 2 years

Description:	VU0155041 is a potent, selective and mixed allosteric agonist/positive allosteric modulator (PAM) of mGluR4, with EC50s of 798 nM and 693 nM for human and rat mGluR4, respectively. VU0155041 is a partial agonist of mGluR4 that activates the receptor by interacting with a site that is distinct from the glutamate binding site[1].
Target:	Human mGlu4:798 nM (EC50) Rat mGlu4:693 nM (EC50)
In Vivo:	VU0155041 (31 nM, 93 nM; i.c.v.) reverses catalepsy induced by the dopamine D2 receptor antagonist haloperidol in rats[1]. VU0155041 (93 nM , 316 nM; i.c.v.) reverses reserpine-induced akinesia in rats[1]. Animal Model: Third ventricle cannulated (TVC) Male Sprague-Dawley rats (225-255 g)[1] Dosage: 31 nM, 93 nM Administration: Intracerebroventrical injection, after the haloperidol (1.5 mg/kg) treatment 2 hours Result: Decreased the cataleptic effects of haloperidol, and the effects still presented 30 min after infusion.
In Vitro:	VU0155041 (30 μM) causes 6.4-fold and 4.7-fold leftward shifts in the glutamate CRC at human and rat mGluR4, respectively[1]. VU0155041 (10 μM) does not affect NMDA receptor currents in striatal medium spiny neurons[1].
References:	[1]. Niswender CM, et, al. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol Pharmacol. 2008 Nov; 74(5): 1345-58.

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