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Pamoic acid is a potent agonist of GPR35 orphan receptors (EC50 = 79 nM in a β-arrestin recruitment assay).1 It induces GPR35 translocation from the plasma membrane to the cytoplasm with an EC50 value of 22 nM. Pamoic acid also increases ERK1/2 phosphorylation in a concentration-dependent manner in U20S cells expressing human GPR35a. In vivo, pamoic acid has antinociceptive effects with an ED50 value of 40.5 mg/kg in a mouse abdominal constriction model of visceral pain perception. Pamoate salts, of which pamoic acid is the main constituent, have been used in drug formulations to extend the duration of action.2
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1. Targeting of the orphan receptor GPR35 by pamoic acid: A potent activator of extracellular signal-
2. Mind your salts: When the inactive constituent isn’t. Mol. Pharmacol. 78(4), 558-559 (2010).