| Identification | Back Directory | [Name]
2-(4-(2-(Benzyloxy)acetyl)piperazin-1-yl)benzonitrile | [CAS]
1242443-29-3 | [Synonyms]
104251
VU0364289
VU-0364289; VU 0364289
2-(4-(2-(Benzyloxy)acetyl)piperazin-1-yl)benzonitrile | [Molecular Formula]
C20H21N3O2 | [MDL Number]
MFCD26097260 | [MOL File]
1242443-29-3.mol | [Molecular Weight]
335.4 |
| Chemical Properties | Back Directory | [Boiling point ]
552.0±50.0 °C(Predicted) | [density ]
1.23±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
1.30±0.10(Predicted) | [color ]
Yellow to brown |
| Hazard Information | Back Directory | [Description]
VU0364289 is a novel N-aryl piperazine mGlu5 positive allosteric modulator. | [Uses]
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]. | [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 |
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| [IC 50]
mGlu5: 1.6 μM (EC50) | [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. DOI:10.1124/jpet.113.206623
[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. |
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