1254979-66-2
Chemical Structure
JNJ-46356479
- CAS No.: 1254979-66-2
- Formula:C22H22F5N5
- Molecular Weight:451.44
IUPAC Name: 3-(cyclopropylmethyl)-7-((4-(2,4-difluorophenyl)piperazin-1-yl)methyl)-8-(trifluoromethyl)-[1,2,4]triazolo[4,3-a]pyridine
InChIKey: BNJUYVSEWGRELC-UHFFFAOYSA-N
SMILES: FC1=CC=C(C(F)=C1)N2CCN(CC2)CC3=C(C4=NN=C(N4C=C3)CC5CC5)C(F)(F)F
Biological Activity: JNJ-46356479 is a blood-brain barrier-penetrant mGluR2/3 allosteric activator. JNJ-46356479 binds to the mGluR2 PAM site to enhance mGluR2 activity, thereby inhibiting presynaptic glutamate release and modulating adenylate cyclase (Adenylate Cyclase), calcium channel (CRAC Channel) activity, and neuronal excitability. JNJ-46356479 exhibits anticonvulsant activity in psychomotor seizures and corneal kindling, and can be used in the study of schizophrenia and epilepsy[1][2][3][4][5].
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JNJ-46356479 | 99.77% | JNJ-46356479 is a blood-brain barrier-penetrant mGluR2/3 allosteric activator. JNJ-46356479 binds to the mGluR2 PAM site to enhance mGluR2 activity, thereby inhibiting presynaptic glutamate release and modulating adenylate cyclase (Adenylate Cyclase), calcium channel (CRAC Channel) activity, and neuronal excitability. JNJ-46356479 exhibits anticonvulsant activity in psychomotor seizures and corneal kindling, and can be used in the study of schizophrenia and epilepsy. | ||||||||||||||||||||
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References
- [1]. Olivares-Berjaga D, et al. Effectiveness of positive allosteric modulators of metabotropic glutamate receptor 2/3 (mGluR2/3) in animal models of schizophrenia. Translational psychiatry. 2025 Jan 14;15(1):11.
- [2]. Leurquin-Sterk G, et al. What We Observe In Vivo Is Not Always What We See In Vitro: Development and Validation of 11C-JNJ-42491293, A Novel Radioligand for mGluR2. Journal of nuclear medicine : official publication, Society of Nuclear Medicine. 2017 Jan;58(1):110-116.
- [3]. Martínez-Pinteño A, et al. Early treatment with JNJ-46356479, a mGluR2 modulator, improves behavioral and neuropathological deficits in a postnatal ketamine mouse model of schizophrenia. Biomedicine & Pharmacotherapy. 2023 Feb 1;158:114079.
- [4]. Martínez-Pinteño A, et al. Effects of JNJ-46356479 and clozapine on VGLUT1 and GAD65/67 brain levels and expression of genes related to glutamate and GABA in mice postnatally exposed to ketamine. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2025 Nov;192:118639.
- [5]. Metcalf CS, et al. Potent and selective pharmacodynamic synergy between the metabotropic glutamate receptor subtype 2-positive allosteric modulator JNJ-46356479 and levetiracetam in the mouse 6-Hz (44-mA) model. Epilepsia. 2018 Mar;59(3):724-735.
