Abstract— (3H)Zacopride displayed saturable binding to homogenates of the rat entorhinal cortex as measured by the inclusion of the 5‐HT3 receptor antagonist BRL 43694 in the incubation media. Scatchard analysis indicated a single high affinity binding site (KD 0.76 ± 0.08 nM, Bmax 77.5 ±6.5 fmol (mg protein)−1) with a Hill slope close to unity. Other 5‐HT3 receptor antagonists (zacopride, ICS 205–930, GR38032F, GR65630, metoclopramide and cocaine) also competed for the binding site displacing 60% of the total (3H)zacopride binding. 5‐HT and 2‐methyl‐5‐HT also were competitive antagonists for (3H)zacopride binding whereas 5‐HT1/5‐HT2 agonists and antagonists, and agents acting on other neurotransmitter receptors had Ki values greater than 10−5 M. It is concluded that (3H)zacopride may prove a useful ligand for the study of 5‐HT3 recognition sites.
Journal of Pharmacy and Pharmacology: An International Journal of Pharmaceutical Science – Wiley
Published: Aug 1, 1988
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