1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. VU0155041

VU0155041 

目录号: HY-14417
产品使用指南

VU0155041 是一种有效,选择性的 mGluR4 混合变构激动剂/正变构调节剂 (PAM),对人和大鼠 mGluR4 的 EC50 值分别为 798 nM 和 693 nM。VU0155041 是 mGluR4 的部分激动剂,可通过与不同于谷氨酸结合位点的位点相互作用来激活受体。

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VU0155041 Chemical Structure

VU0155041 Chemical Structure

CAS No. : 1093757-42-6

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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].

IC50 & Target[1]

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.
Molecular Weight

316.18

Formula

C₁₄H₁₅Cl₂NO₃

CAS No.

1093757-42-6

SMILES

O=C([C@H](CCCC1)[C@H]1C(O)=O)NC2=CC(Cl)=CC(Cl)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

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Keywords:

VU0155041VU 0155041VU-0155041mGluRMetabotropic glutamate receptorsmGluR4partial glutamateInhibitorinhibitorinhibit

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VU0155041
目录号:
HY-14417
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