( 3 H)Zacopride: Ligand for the Identification of 5‐HT 3 Recognition Sites

( 3 H)Zacopride: Ligand for the Identification of 5‐HT 3 Recognition Sites 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. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Journal of Pharmacy and Pharmacology: An International Journal of Pharmaceutical Science Wiley

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Publisher
Wiley
Copyright
1988 Royal Pharmaceutical Society of Great Britain
ISSN
0022-3573
eISSN
2042-7158
DOI
10.1111/j.2042-7158.1988.tb05300.x
Publisher site
See Article on Publisher Site

Abstract

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

Journal of Pharmacy and Pharmacology: An International Journal of Pharmaceutical ScienceWiley

Published: Aug 1, 1988

References

  • Zacopride: anxiolytic profile in rodent and primate models of anxiety
    Costall, Costall; Domeney, Domeney; Gerrard, Gerrard; Kelly, Kelly; Naylor, Naylor
  • Zacopride: a potent 5‐HT 3 antagonist
    Smith, Smith; Sancilio, Sancilio; Owera‐Atepo, Owera‐Atepo; Naylor, Naylor; Lambert, Lambert

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