AQW-051

Names

[ Name ]:
AQW-051

[Synonym ]:
JQH481R778
1-Azabicyclo[2.2.2]octane, 3-[[6-(4-methylphenyl)-3-pyridinyl]oxy]-, (3R)-
MFCD28502153
AQW051
(3R)-3-{[6-(4-Methylphenyl)-3-pyridinyl]oxy}quinuclidine

Biological Activity

[Description]:

VQW-765 (AQW-051) is a selective and orally active alpha-7 nicotinic acetylcholine receptor (α7-nAChR) agonist with a pKD value of 7.56 to recombinantly expressed human α7-nAChR. VQW-765 shows anxiolytic-like effect in vivo. VQW-765 can be used for the research of anxiety disorder and acute performance anxiety[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR

Signaling Pathways >> Neuronal Signaling >> nAChR

Research Areas >> Neurological Disease

[In Vitro]

VQW-765 对重组表达的人 α7-nACh 受体的 pKD 值为 7.56[1]。 VQW-765 在 GH3-ha7-22 细胞中重组表达的人 α7-nACh 受体刺激后，显示出对钙瞬态的强大激动活性，pEC50 值为 7.41[1]。

[In Vivo]

VQW-765 (0.03 和 0.3 mg/kg；口服，一次) 增加小鼠的认知和学习、记忆表现[1]。 VQW-765 (1 mg/kg；口服，一次) 显示出抗焦虑作用，增加大鼠的社会探索时间，持续时间至少6小时[1]。 Animal Model: OF1/IC strain adult mice[1] Dosage: 0.03 and 0.3 mg/kg Administration: Oral administration; 0.03 and 0.3 mg/kg once Result: Increased the learning/memory performance with more time to scrutinize the novel partner than the familiar partner during the re-test trial at 24 h. Showed cognitive-enhancing effects in mice by the object recognition test (ORT).

[References]

[1]. Feuerbach D, et al. AQW051, a novel, potent and selective α7 nicotinic ACh receptor partial agonist: pharmacological characterization and phase I evaluation. Br J Pharmacol. 2015 Mar;172(5):1292-304.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
443.8±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₉H₂₂N₂O

[ Molecular Weight ]:
294.391

[ Flash Point ]:
222.2±28.7 °C

[ Exact Mass ]:
294.173218

[ LogP ]:
3.69

[ Vapour Pressure ]:
0.0±1.1 mmHg at 25°C

[ Index of Refraction ]:
1.622

[ Storage condition ]:
store at -20℃ for one year（Powder）

Related Compounds

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