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Delineation of the functional properties and the mechanism of action of TMPPAA, an allosteric agonist and positive allosteric modulator of 5-HT<inf>3</inf> receptors
2016, Biochemical PharmacologyCitation Excerpt :These values are in good agreement with previously reported binding affinities and antagonist potencies for the compounds [19,20,25,36]. Metoclopramide exhibited an IC50 of 4.0 μM, which is in the high end of the considerable range of functional IC50 values displayed by the antagonist at 5-HT3ARs in previous studies [31,32,37,38]. Finally, the 5-HT3R NAMs PU02 and propofol displayed antagonist potencies in agreement with previously reported values [26,39,40], whereas the channel blocker picrotoxin displayed a ∼10-fold lower IC50 value at the h5-HT3AR in this assay than those reported from previous studies in oocytes [41,42].
The 5-HT<inf>3</inf> receptor - the relationship between structure and function
2009, NeuropharmacologyCitation Excerpt :The 5-HT3A(b) isoform lacks 6 (mouse and guinea pig), or 5 (rat) amino acid residues within the large intracellular loop linking M3 and M4. Differences in the efficacy of certain 5-HT3 receptor agonists at the two isoforms have been noted along with differential modulation by activators of protein kinase A (PKA) and protein kinase C (PKC) (Downie et al., 1994; van Hooft et al., 1997; Niemeyer & Lummis, 1999; Hubbard et al., 2000). The human isoform corresponds to the 5-HT3A(b) subunit (Belelli et al., 1995; Miyake et al., 1995).
Investigation of the effects of YM-31636, a novel 5-HT<inf>3</inf> receptor agonist, on defecation in normal and constipated ferrets
2001, European Journal of PharmacologyPharmacological profile of YM-31636, a novel 5-HT<inf>3</inf> receptor agonist, in vitro
2000, European Journal of PharmacologyFunctional differences between splice variants of the murine 5-HT(3A) receptor: Possible role for phosphorylation
2000, Molecular Brain ResearchCloning, expression, and characterization of ferret 5-HT<inf>3</inf> receptor subunit
2000, European Journal of Pharmacology