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The anti-emetic activity of GK-128 in Suncus murinus.

Abstract
In Suncus murinus, various emetic responses and the anti-emetic activity of a new 5-hydroxytryptamine3 (5-HT3) receptor antagonist, GK-128 (2-[(2-methylimidazol-1-yl) methyl benzo[f]thiochromen-1-one monohydrochloride hemihydrate), were investigated. Cancer chemotherapeutic agents, cisplatin and cyclophosphamide, dose-dependently induced emesis of long-lasting duration. The 5-HT3 receptor agonist, 2-methyl-5-HT, and copper sulfate also induced emesis of short duration. However, another 5-HT3 receptor agonist, m-chlorophenylbiguanide, was not consistently emetic. GK-128 inhibited the emetic responses induced by chemotherapeutic agents and 2-methyl-5-HT with similar potency. The anti-emetic action of GK-128 was more potent than that of ondansetron, Y-25130, granisetron and metoclopramide. The order of potency of these drugs, except granisetron, was consistent with that of their 5-HT3 receptor binding affinity in rat cortex. GK-128 failed to inhibit copper sulfate-induced emesis. These data suggest that GK-128 has a potent inhibitory effect on emesis via the 5-HT3 receptor, and that the 5-HT3 receptor involved in emesis in Suncus murinus may be different from the classically defined 5-HT3 receptor in other animals such as rats, dogs and ferrets.
AuthorsC Ito, Y Isobe, H Kijima, Y Kiuchi, H Ohtsuki, R Kawamura, K Tsuchida, S Higuchi
JournalEuropean journal of pharmacology (Eur J Pharmacol) Vol. 285 Issue 1 Pg. 37-43 (Oct 04 1995) ISSN: 0014-2999 [Print] Netherlands
PMID8846809 (Publication Type: Journal Article)
Chemical References
  • Antiemetics
  • Chromones
  • GK 128
  • Imidazoles
  • Serotonin Antagonists
  • Serotonin
  • 2-methyl-5-HT
  • Copper
  • Cyclophosphamide
  • Copper Sulfate
  • Cisplatin
Topics
  • Animals
  • Antiemetics (pharmacology)
  • Chromones (pharmacology)
  • Cisplatin (toxicity)
  • Copper (toxicity)
  • Copper Sulfate
  • Cyclophosphamide (toxicity)
  • Dose-Response Relationship, Drug
  • Female
  • Imidazoles (pharmacology)
  • Male
  • Serotonin (analogs & derivatives, pharmacology)
  • Serotonin Antagonists (pharmacology)
  • Shrews
  • Species Specificity
  • Vomiting (chemically induced, prevention & control)

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