1093757-42-6

1093757-42-6 structure

Name: VU 0155041
Chemical Name: (1R,2S)-2-[(3,5-dichlorophenyl)carbamoyl]cyclohexane-1-carboxylic acid
CAS Number: 1093757-42-6
Molecular Formula: C₁₄H₁₅Cl₂NO₃
Molecular Weight: 316.18000
Catalog: Signaling Pathways GPCR/G Protein mGluR
Create Date: 2016-03-11 19:19:59
Modify Date: 2024-01-09 15:23:39
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].

Name	(1R,2S)-2-[(3,5-dichlorophenyl)carbamoyl]cyclohexane-1-carboxylic acid
Synonyms	gtpl3323 VU 0155041 VU0155041

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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mGluR Research Areas >> Neurological Disease
Target	Human mGlu4:798 nM (EC50) Rat mGlu4:693 nM (EC50)
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].
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.
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.