5‐HT 3 receptor antagonists injected into the area postrema inhibit cisplatin‐induced emesis in the ferret

5‐HT 3 receptor antagonists injected into the area postrema inhibit cisplatin‐induced emesis... 1 The purpose of the present study was to identify and investigate the role of 5‐hydroxytryptamine3 (5‐HT3) receptors in the area postrema in the control of cisplatin‐induced emesis in the ferret. 2 Homogenate binding and autoradiography experiments using the high affinity 5‐HT3 receptor ligand, (3H)‐GR65630, identified the presence of a high concentration of 5‐HT3 receptors in the area postrema of the ferret. 3 Intraperitoneal injection of the 5‐HT3 receptor antagonists, GR38032F, GR65630A and MDL72222, at doses of 1, 0.1 and 1 mg kg−1 respectively, inhibited emesis induced by cisplatin, 9 mg kg−1 i.p. 4 Discrete injection of low doses of the 5‐HT3 receptor antagonists directly into the area postrema region also inhibited cisplatin‐induced (9 mg kg−1 i.p.) emesis. The dose ranges used were: GR38032F, 0.01–1 μg; GR65630A, 0.001–0.1 μg; MDL72222, 0.1–10 μg. 5 Cisplatin‐induced emesis was not inhibited by discrete injection of ketanserin (30 μg) or methiothepin (30 μg) into the area postrema. Injection of the 5‐HT3 receptor agonist, 2‐methyl‐5‐HT, directly into the area postrema produced an incomplete emetic response. 6 These results confirm a role of 5‐HT, and in particular 5‐HT3 receptors, in the control of cisplatin‐induced emesis, and show that at least one functional site for these receptors in modulating the emetic response is the area postrema, the locus of the chemoreceptor trigger zone. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png British Journal of Pharmacology Wiley

5‐HT 3 receptor antagonists injected into the area postrema inhibit cisplatin‐induced emesis in the ferret

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Publisher
Wiley
Copyright
1989 British Pharmacological Society
ISSN
0007-1188
eISSN
1476-5381
DOI
10.1111/j.1476-5381.1989.tb11948.x
Publisher site
See Article on Publisher Site

Abstract

1 The purpose of the present study was to identify and investigate the role of 5‐hydroxytryptamine3 (5‐HT3) receptors in the area postrema in the control of cisplatin‐induced emesis in the ferret. 2 Homogenate binding and autoradiography experiments using the high affinity 5‐HT3 receptor ligand, (3H)‐GR65630, identified the presence of a high concentration of 5‐HT3 receptors in the area postrema of the ferret. 3 Intraperitoneal injection of the 5‐HT3 receptor antagonists, GR38032F, GR65630A and MDL72222, at doses of 1, 0.1 and 1 mg kg−1 respectively, inhibited emesis induced by cisplatin, 9 mg kg−1 i.p. 4 Discrete injection of low doses of the 5‐HT3 receptor antagonists directly into the area postrema region also inhibited cisplatin‐induced (9 mg kg−1 i.p.) emesis. The dose ranges used were: GR38032F, 0.01–1 μg; GR65630A, 0.001–0.1 μg; MDL72222, 0.1–10 μg. 5 Cisplatin‐induced emesis was not inhibited by discrete injection of ketanserin (30 μg) or methiothepin (30 μg) into the area postrema. Injection of the 5‐HT3 receptor agonist, 2‐methyl‐5‐HT, directly into the area postrema produced an incomplete emetic response. 6 These results confirm a role of 5‐HT, and in particular 5‐HT3 receptors, in the control of cisplatin‐induced emesis, and show that at least one functional site for these receptors in modulating the emetic response is the area postrema, the locus of the chemoreceptor trigger zone.

Journal

British Journal of PharmacologyWiley

Published: May 1, 1989

References

  • Pharmacological properties of GR38032F, a novel antagonist at 5‐HT 3 receptors
    Butler, Butler; Hill, Hill; Ireland, Ireland; Jordan, Jordan; Tyers, Tyers
  • Inhibition of cisplatin‐induced vomiting by selective 5‐hydroxytryptamine M‐receptor antagonism
    Miner, Miner; Sanger, Sanger
  • Fundamental studies with cisplatin
    Rosenberg, Rosenberg
  • The emetic activity of centrally administered cisplatin in cats and its antagonism by zacopride
    Smith, Smith; Callahan, Callahan; Alphin, Alphin

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