ChemicalBook CAS DataBase List 1242443-29-3

1242443-29-3

Name	2-(4-(2-(Benzyloxy)acetyl)piperazin-1-yl)benzonitrile
CAS	1242443-29-3
Molecular Formula	C20H21N3O2
MDL Number	MFCD26097260
Molecular Weight	335.4
MOL File	1242443-29-3.mol

Chemical Properties

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

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].

	T_max (h)	C_max (ng/mL)	Plasma protein binding	Rat Fu (free fraction)
IP (10 mg/kg)	0.25	1280	94% (h); 90% (r)	0.10

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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