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Related Experiment Video

Updated: Mar 24, 2026

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Discovery and Characterization of AMPA Receptor Modulators Selective for TARP-γ8.

Michael P Maher1, Nyantsz Wu2, Suchitra Ravula2

  • 1Janssen Research and Development, LLC, Neuroscience Therapeutic Area, San Diego, California (M.P.M., N.W., S.R., M.K.A., B.M.S., C.L., B.L., R.M.W., J.A.M., C.D., S.Y., A.D.W., N.I.C., T.W.L.); and Janssen Research and Development, a Division of Janssen Pharmaceutica NV, Neuroscience Therapeutic Area, Beerse, Belgium (L.V.D., T.S.) mmaher1@its.jnj.com.

The Journal of Pharmacology and Experimental Therapeutics
|March 19, 2016
PubMed
Summary
This summary is machine-generated.

Novel AMPA receptor modulators targeting TARP-γ8 show therapeutic potential. These compounds, like JNJ-55511118, offer reversible inhibition for anticonvulsant and neuroprotectant applications.

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Area of Science:

  • Neuroscience
  • Pharmacology
  • Molecular Biology

Background:

  • α-amino-3-hydroxyl-5-methyl-4-isoxazole-propionic acid (AMPA) receptors are crucial for fast synaptic transmission in the central nervous system.
  • AMPA receptors are key therapeutic targets for neurological disorders.

Purpose of the Study:

  • To identify and characterize novel AMPA receptor modulators.
  • To investigate the mechanism of action involving the accessory protein CACNG8 (TARP-γ8).

Main Methods:

  • Calcium flux assays
  • Radioligand binding assays
  • Electrophysiological recordings of wild-type and mutant TARP-γ8
  • In vivo rodent models

Main Results:

  • Novel modulators were identified that require TARP-γ8.
  • Compounds demonstrated a partial disruption of TARP-channel subunit interaction.
  • JNJ-55511118 exhibited favorable pharmacokinetics, potent hippocampal inhibition, and anticonvulsant effects.
  • In vivo studies showed EEG changes, transient hyperlocomotion, and mild learning/memory impairment at high doses.

Conclusions:

  • JNJ-55511118 is a novel tool for reversible AMPA receptor inhibition, especially in the hippocampus.
  • This compound has potential as an anticonvulsant or neuroprotectant.
  • Pharmacological targeting of accessory proteins like TARP-γ8 expands the scope of druggable targets.