CLH304a (compound 14) is a selective and noncompetitive negative allosteric modulator (NAM) of the GABA$_B$ receptor. It specifically targets the heptahelical domain of the GB2 subunit, inhibiting receptor activity with inverse agonist properties. CLH304a reduces GABA-induced inositol trisphosphate (IP₃) production with an IC₅₀ of 37.9 μM and does not affect other Class C GPCRs, including mGluR1, mGluR2, and mGluR5, indicating high selectivity.
Additionally, CLH304a inhibits Baclofen-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABA$_B$ receptors, further supporting its function as a negative modulator. This compound is a valuable tool for investigating GABA$_B$ receptor function and holds potential for therapeutic research in neurological disorders involving GABAergic signaling dysregulation.
CLH304a (compound 14) is a selective and noncompetitive negative allosteric modulator (NAM) of the GABA$_B$ receptor. It specifically targets the heptahelical domain of the GB2 subunit, inhibiting receptor activity with inverse agonist properties. CLH304a reduces GABA-induced inositol trisphosphate (IP₃) production with an IC₅₀ of 37.9 μM and does not affect other Class C GPCRs, including mGluR1, mGluR2, and mGluR5, indicating high selectivity.
Additionally, CLH304a inhibits Baclofen-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABA$_B$ receptors, further supporting its function as a negative modulator. This compound is a valuable tool for investigating GABA$_B$ receptor function and holds potential for therapeutic research in neurological disorders involving GABAergic signaling dysregulation.
Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 1 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.
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