Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: 2-(4-(2-(Benzyloxy)acetyl)piperazin-1-yl)benzonitrile
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Purity: 98.0%
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1242443-29-3

1242443-29-3 structure

Name: VU0364289
Chemical Name: vu0364289
CAS Number: 1242443-29-3
Molecular Formula: C₂₀H₂₁N₃O₂
Molecular Weight: 335.40000
Catalog: Signaling Pathways GPCR/G Protein mGluR
Create Date: 2018-06-03 08:48:00
Modify Date: 2024-03-07 18:29:56
VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 µM. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research[1][2][3].

Name	vu0364289

Description	VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP (HY-14609A) site), with an EC50 of 1.6 µM. VU0364289 can reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, which can be used for schizophrenia and other psychiatric research[1][2][3].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mGluR Research Areas >> Neurological Disease
Target	mGlu5:1.6 μM (EC50)
In Vivo	VU0364289 (10, 30, 56.6, 100 mg/kg ; i.p.; once) reverse amphetamine-induced hyperlocomotion in a dose-dependent manner, and (56.6, 100 mg/kg) shows significantly fewer ambulations[1]. VU0364289 (10 mg/kg; i.p.; once) is rapidly and significantly absorbed in rats, and shows excellent central nervous system penetration[1]. Animal Model: Adult male Sprague-Dawley rats (250-275 g)[1]. Dosage: 10, 30, 56.6, 100 mg/kg Administration: Intraperitoneal injection; once. Result: Showed activity of reversing the hyperlocomotion induced by amphetamine, and can also significantly fewer ambulations in rats when dose up to 56.6 mg/kg. Animal Model: Adult male Sprague-Dawley rats (250-275 g)[1]. Dosage: 10 mg/kg Administration: Intraperitoneal injection; once. Result: 1.19Pharmacokinetic Parameters of VU0364289 in male Sprague-Dawley rats[1]. Tmax (h) Cmax (ng/mL) Plasma protein binding Rat Fu (free fraction) IP (10 mg/kg) 0.25 1280 94% (h); 90% (r) 0.10
References	[1]. Gregory KJ, et al. N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement. J Pharmacol Exp Ther. 2013 Nov;347(2):438-57. [2]. Ya Zhou, et al. Discovery of N-Aryl Piperazines as Selective mGluR5Potentiators with Improved In Vivo Utility. ACS medicinal chemistry letters, 2010, 1(8): 433-438. [3]. Psychosis Models[M]//Melatonin, Neuroprotective Agents and Antidepressant Therapy. Springer, New Delhi, 2016: 731-750.

Molecular Formula	C₂₀H₂₁N₃O₂
Molecular Weight	335.40000
Exact Mass	335.16300
PSA	56.57000
LogP	2.42658

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