| Identification | Back Directory | [Name]
VU0155041 | [CAS]
1093757-42-6 | [Synonyms]
VU0155041
UV0155041
VU0155041;VU-0155041
(±)-cis-2-(3,5-DichlorophenylcarbaMoy)cyclohexanecarboxylic Acid
(±)-cis-2-(3,5-Dicholorphenylcarbamoyl)cyclohexanecarboxylic acid
(1S,2R)-2-((3,5-DICHLOROPHENYL)CARBAMOYL)CYCLOHEXANECARBOXYLIC ACID
cis-2-[[(3,5-Dichlorophenyl)amino]carbonyl]cyclohexanecarboxylicacid
(1R,2S)-2-[(3,5-dichlorophenyl)carbamoyl]cyclohexane-1-carboxylic acid
rel-(1R,2S)-2-[[(3,5-Dichlorophenyl)amino]carbonyl]cyclohexanecarboxylic acid
Cyclohexanecarboxylic acid, 2-[[(3,5-dichlorophenyl)amino]carbonyl]-, (1R,2S)-rel- | [Molecular Formula]
C14H15Cl2NO3 | [MDL Number]
MFCD03544581 | [MOL File]
1093757-42-6.mol | [Molecular Weight]
316.18 |
| Chemical Properties | Back Directory | [Boiling point ]
540.2±50.0 °C(Predicted) | [density ]
1.429±0.06 g/cm3(Predicted) | [storage temp. ]
Store at RT | [solubility ]
Soluble to 100 mM in 1eq. NaOH and to 100 mM in DMSO | [form ]
white powder | [pka]
4.48±0.44(Predicted) | [color ]
Pale purple to purple |
| Hazard Information | Back Directory | [Uses]
Acts as an allosteric modulator (PAM) of mGluR4, part of the class of receptors influencing Parkinson’s disease and it’s expression. | [Biological Activity]
VU0155041 is a mixed allosteric agonist/positive allosteric modulator (PAM) of mGluR4. VU0155041 is approximately 8-fold more potent than PHCCC and does not show any significant potentiator or antagonist activity at other mGluR subtypes. It is soluble in an aqueous vehicle and intracerebroventricular administration of 31-316 nmol of VU0155041 dose-dependently decreased haloperidol-induced catalepsy and reserpine-induced akinesia in rats. VU0155041 exhibits selectivity for mGluR4 relative to 67 different targets and does not affect the function of striatal NMDA receptors.''VU0155041 is a positive allosteric modulator of the metabotropic glutamate receptor subtype 4. It also shows some direct agonist activitybut at a site different from the glutamate binding site. /VU0155041 is approximately 8-fold more potent than PHCCC and enhances the activity of glutamate also about 8-fold. It shows promising anti-Parkinsonian effects in animal models of Parkinsonμs disease. | [in vivo]
VU0155041 (31 nmol, 93 nmol; i.c.v.) reverses catalepsy induced by the dopamine D2 receptor antagonist Haloperidol (1.5 mg/kg, i.p.) in rats[1].
VU0155041 (93 nnmol, 316 nmol; i.c.v.) reverses Reserpine (HY-N0480)-induced akinesia in rats[1].
| Animal Model: | Third ventricle cannulated (TVC) Male Sprague-Dawley rats (225-255 g)[1] | | Dosage: | 31 nmol, 93 nmol (10 μL) | | 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. |
| [IC 50]
Human mGlu4: 798 nM (EC50); Rat mGlu4: 693 nM (EC50) |
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