2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. JNJ-78911118

JNJ-78911118 is a potent, brain-penetrant, selective GluN2A antagonist (IC50 = 44 nM). JNJ-78911118 shows >200-fold selectivity against GluN1/2B, 2C and 2D receptors. JNJ-78911118 functions as a negative allosteric modulator (NAM) by insurmountably suppressing glutamate efficacy and reducing glycine potency at GluN1/2A receptors. JNJ-78911118 produces profound pharmacodynamic effects in vivo. JNJ-78911118 can be used for depression research.

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JNJ-78911118

JNJ-78911118 Chemical Structure

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Description

JNJ-78911118 is a potent, brain-penetrant, selective GluN2A antagonist (IC50 = 44 nM). JNJ-78911118 shows >200-fold selectivity against GluN1/2B, 2C and 2D receptors. JNJ-78911118 functions as a negative allosteric modulator (NAM) by insurmountably suppressing glutamate efficacy and reducing glycine potency at GluN1/2A receptors. JNJ-78911118 produces profound pharmacodynamic effects in vivo. JNJ-78911118 can be used for depression research[1].

IC50 & Target[1]

GluN2A

44 nM (IC50)

In Vitro

JNJ-78911118 (10 pM-10 μM, 2 h) displaces the GluN1/2A interface binding radioligand JNJ-74950343 in hippocampal neuron membranes in a concentration-dependent manner, and does not alter glutamate potency but reduces its efficacy against homomeric GluN1/2A receptors[1].
JNJ-78911118 (10 μM, 24-72 h) promotes neurite outgrowth and synaptogenesis in rat hippocampal neuronal cultures, significantly enhancing multiple measures of dendritic complexity after 72 h[1].
JNJ-78911118 (1-10 μM) shows less than 50 % inhibition against all targets in a custom panel of 77 ion channels, receptors, and transporters, as well as a panel of 373 kinases[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

JNJ-78911118 Related Antibodies
In Vivo

JNJ-78911118 (60 mg/kg, s.c., single dose) mitigates mechanical allodynia in the Complete Freund's adjuvant (CFA, HY-153808) mouse models of inflammatory pain, prevents hippocampal long-term potentiation (LTP) in rats and increases miniature excitatory postsynaptic current (mEPSC) frequency in the rat prefrontal cortex[1].
JNJ-78911118 (50 and 250 mg/kg, p.o., twice daily for 4 days or twice on the same day) is generally well tolerated but produces dose-related haemodynamic effects in rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57BL/6 N mice (8-12 weeks)[1]
Dosage: 60 mg/kg
Administration: s.c., single dose 2 days post-CFA
Result: Partly reversed CFA induced allodynia at 60 mg/kg, while Gabapentin (HY-A0057, 150 mg/kg, p.o.) completely reversed it.
Reduced tactile allodynia at 30 min and 1 h post-administration compared to controls.
Had no effect on paw withdrawal thresholds (PWTs) 24 h post-dosing.
Animal Model: Wild-type C57BL/6J and homozygous Grin2a KO mice[1]
Dosage: 60 mg/kg
Administration: s.c., single dose 2 days post-CFA
Result: Mitigated CFA-induced allodynia in wild type mice at 30 min and 1-h post-administration.
Did not significantly reduce CFA-induced mechanical allodynia in Grin2a KO mice.
Animal Model: Male Sprague-Dawley rats (8-10 weeks)[1]
Dosage: 60 mg/kg
Administration: s.c., single dose 30 min pre-TBS
Result: Did not alter baseline synaptic transmission but completely blocked the induction of LTP by theta burst stimulation (TBS).
The population spike amplitude remained at pre-stimulation levels throughout the recording period (50-60 min post-TBS).
Animal Model: Male Sprague-Dawley rats (6-10 weeks)[1]
Dosage: 60 mg/kg
Administration: s.c., single dose (24 h before recording)
Result: Induced a significant decrease in the inter-event interval of mEPSCs in layer 5 pyramidal neurons in rat medial prefrontal cortex.
Showed no significant changes in mEPSC amplitude.
Animal Model: Male Wistar Han rats [1]
Dosage: 50 and 250 mg/kg
Administration: p.o., twice daily for 4 days
Result: Achieved dose-dependent plasma exposures, with Cmax and AUC increasing less than dose proportionally (80 and 180 %, respectively, and Tmax occurring 1-3 h post-dose.
Minimal activity decreases or minimal hypoactivity were observed 2 h post-dose on days 1-3.
Piloerection was observed in high-dose animals on Day 1 at 3 h post-dose.
Low doses had no effect on body weight, while the high dose caused a transient 3 % decrease in two animals and lower overall body weight gain in all animals.
No meaningful changes were detected in globulin, protein, albumin, chloride, calcium and potassium concentrations, cholesterol level or reticulocyte count.
Produced mild decreases in triglyceride levels.
Showed no Olney's lesions in animals.
Animal Model: Male Sprague-Dawley rats (8-10 weeks)[1]
Dosage: 50 and 250 mg/kg
Administration: p.o., twice on the same day
Result: The low dose increased heart rate and mean arterial pressure.
The high dose caused a transient decrease in heart rate (associated with reduced body temperature) and an increase in blood pressure.
Molecular Weight

419.81

Formula

C19H16ClF2N5O2
SMILES

CC1=NC(C(NCC2=CC=CN=C2)=O)=CN=C1OCC(F)(F)C3=CC(Cl)=CC=N3
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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JNJ-78911118 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JNJ-78911118JNJ78911118JNJ 78911118iGluRIonotropic glutamate receptorsGluN2ANAMdepressionrat hippocampal neuronalTBSCFAInhibitorinhibitorinhibit

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