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Prior work indicated that serotonin transporter (SERT) inhibitors competitively inhibit substrate‐induced [3H]5‐HT release, producing rightward shifts in the substrate‐dose response curve and increasing the EC50 value without altering the Emax. We hypothesized that this finding would not generalize across a number of SERT inhibitors and substrates, and that the functional dissociation constant (Ke)...
The basal (constitutive) activity of G protein‐coupled receptors allows for the measurement of inverse agonist activity. Some competitive antagonists turn into inverse agonists under conditions where receptors are constitutively active. In contrast, neutral antagonists have no inverse agonist activity, and they block both agonist and inverse agonist activity. The μ‐opioid receptor (MOR) demonstrates...
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