Characterization of ( 3 H)Quipazine Binding to 5‐Hydroxytryptamine 3 Receptors in Rat Brain Membranes

Characterization of ( 3 H)Quipazine Binding to 5‐Hydroxytryptamine 3 Receptors in Rat Brain... Abstract: (3H)Quipazine was used to label binding sites in rat brain membranes that display characteristics of a 5‐hydroxytryptamine3 (5‐HT3) receptor. The radioligand binds with high affinity (KD, 1.2 ± 0.1 nM) to a saturable population of sites (Bmax, 3.0 ± 0.4 pmol/g of tissue) that are differentially located in the brain. Specific (3H)quipazine binding is not affected by guanine or adenine nucleotides. ICS 205–930, BRL 43964, Lilly 278584, and zacopride display less than nanomolar affinity for these sites whereas MDL 72222 is approximately one order of magnitude less potent. The pharmacological profile of the binding site is in excellent agreement with that of 5‐HT3 receptors characterized in peripheral physiological models. We conclude that (3H)quipazine labels a 5‐HT3 receptor in the rat CNS. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Journal of Neurochemistry Wiley

Characterization of ( 3 H)Quipazine Binding to 5‐Hydroxytryptamine 3 Receptors in Rat Brain Membranes

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Publisher
Wiley
Copyright
Copyright © 1989 Wiley Subscription Services, Inc., A Wiley Company
ISSN
0022-3042
eISSN
1471-4159
DOI
10.1111/j.1471-4159.1989.tb07258.x
Publisher site
See Article on Publisher Site

Abstract

Abstract: (3H)Quipazine was used to label binding sites in rat brain membranes that display characteristics of a 5‐hydroxytryptamine3 (5‐HT3) receptor. The radioligand binds with high affinity (KD, 1.2 ± 0.1 nM) to a saturable population of sites (Bmax, 3.0 ± 0.4 pmol/g of tissue) that are differentially located in the brain. Specific (3H)quipazine binding is not affected by guanine or adenine nucleotides. ICS 205–930, BRL 43964, Lilly 278584, and zacopride display less than nanomolar affinity for these sites whereas MDL 72222 is approximately one order of magnitude less potent. The pharmacological profile of the binding site is in excellent agreement with that of 5‐HT3 receptors characterized in peripheral physiological models. We conclude that (3H)quipazine labels a 5‐HT3 receptor in the rat CNS.

Journal

Journal of NeurochemistryWiley

Published: Jun 1, 1989

References

  • Pharmacological characterization of 5‐hydroxytryptamine‐induced depolarization of the rat isolated vagus nerve
    Ireland, Ireland; Tyers, Tyers
  • The potential anxiolytic activity of GR38032F, a 5‐HT 3 receptor antagonist
    Jones, Jones; Costall, Costall; Domeney, Domeney; Kelly, Kelly; Naylor, Naylor; Oakley, Oakley; Tyers, Tyers
  • 5‐Hydroxytryptamine receptor subtypes
    Peroutka, Peroutka
  • Zacopride, a potent 5‐HT 3 antagonist
    Smith, Smith; Sancilio, Sancilio; Owera‐Atepo, Owera‐Atepo; Naylor, Naylor; Lambert, Lambert

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