1363281-27-9

1363281-27-9 structure

Name: JNJ-46778212
Chemical Name: VU 0409551
CAS Number: 1363281-27-9
Molecular Formula: C₂₀H₁₇FN₂O₃
Molecular Weight: 352.36
Catalog: Signaling Pathways GPCR/G Protein mGluR
Create Date: 2018-06-14 03:15:02
Modify Date: 2024-01-13 16:39:04
JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.

Name	VU 0409551
Synonyms	JNJ-46778212

Description	JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mGluR Research Areas >> Neurological Disease
Target	EC50: 260 nM (mGlu5)[1]
In Vivo	In oral brain/plasma studies, JNJ-46778212 displays excellent CNS penetration[1]. JNJ-46778212 enhances NMDAR function and rescues long-term potentiation in hippocampal slices obtained from SR−/− mice. The administration of JNJ-46778212 to SR−/− mice reverses their deficits in several neuroplasticity signaling pathways and improves their contextual fear memory[2].
Animal Admin	Mice[1] SR−/− mice receive once daily, intraperitoneal (i.p.) injections of vehicle (20% hydroxypropyl β-cyclodextran) or VU0409551 for 5 days at a volume of 10 mL/kg. For the in vivo pharmacokinetic and dose-finding experiments, WT mice (n=5–6/dose) receive vehicle or VU0409551 (10 and 30 mg/kg). For the SR−/− mice reversal studies, WT mice receive vehicle and SR−/− mice receive either vehicle or VU0409551 (30 mg/kg). All mice are killed 2 h after the last injection on day 5[1].
References	[1]. Conde-Ceide S, et al. Discovery of VU0409551/JNJ-46778212: An mGlu5 Positive Allosteric Modulator Clinical Candidate Targeting Schizophrenia. ACS Med Chem Lett. 2015 May 20;6(6):716-20.