>>Signaling Pathways>> GPCR/G protein>> mGluR >>VU0364289

VU0364289

Catalog No.GC70503

VU0364289 는 매우 선택적인 mGlu5 양의 변형 조절제 (PAM) (MPEP 비트와 결합) 이며 EC50은 1.6 µM입니다.

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VU0364289 Chemical Structure

Cas No.: 1242443-29-3

Size 가격 재고 수량
5 mg
US$45.00
재고 있음
10 mg
US$72.00
재고 있음
25 mg
US$135.00
재고 있음
50 mg
US$207.00
재고 있음
100 mg
US$306.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents
VU0364289 is a highly selective mGlu5 positive allosteric modulator (PAM) (binds to the MPEP 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.

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].

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.

리뷰

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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