trans-3-(4-Methoxyphenyl)-N-(pentan-3-yl)acrylamide, commonly referred as TMPPAA, is a allosteric agonist and positive allosteric modulator (PAM) of 5-HT3 receptor. It has the molecular formula . TMPPAA behaves as both an agonist and a PAM at 5-HT3A receptors, not via binding at the orthosteric site.
Pharmacology and mechanism of action It is a synthetic compound that functions as an allosteric agonist and positive allosteric modulator of the 5-HT3 serotonin receptor. While traditional ligands bind to the extracellular orthosteric site, chimeric and mutational studies indicate that TMPPAA interacts directly with the receptor's transmembrane domain. Electrophysiological experiments show that the compound exhibits distinct desensitization kinetics and causes a progressive current run-down, demonstrating a mechanism of activation separate from serotonin.
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