Literature DB >> 2964267

Antiemetic properties of the 5HT3-receptor antagonist, GR38032F.

R Stables1, P L Andrews, H E Bailey, B Costall, S J Gunning, J Hawthorn, R J Naylor, M B Tyers.   

Abstract

GR38032F is a highly selective 5HT3-receptor antagonist which inhibits vomiting induced by cisplatin, cyclophosphamide or X-radiation in the ferret. Since cisplatin selectively increased the levels of 5HT and 5HIAA in the intestinal mucosa, a possible site of the antiemetic action of GR38032F may be on 5HT3-receptors on vagal afferents in the small intestine. The potent antiemetic action of GR38032F should be of clinical value in reducing the nausea and vomiting associated with radiotherapy or chemotherapy of cancer.

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Year:  1987        PMID: 2964267     DOI: 10.1016/0305-7372(87)90026-0

Source DB:  PubMed          Journal:  Cancer Treat Rev        ISSN: 0305-7372            Impact factor:   12.111


  24 in total

1.  Serotonin and emesis--from animals to humans: a discussion of Professor Naylor's paper.

Authors:  L Cubeddu; I Hoffmann; N Fuenmayor
Journal:  Br J Cancer Suppl       Date:  1992-12

Review 2.  Neuropharmacology of emesis in relation to clinical response.

Authors:  B Costall; R J Naylor
Journal:  Br J Cancer Suppl       Date:  1992-12

3.  Differential interactions of traditional and novel antiemetics with dopamine D2 and 5-hydroxytryptamine3 receptors.

Authors:  A Hamik; S J Peroutka
Journal:  Cancer Chemother Pharmacol       Date:  1989       Impact factor: 3.333

4.  Antidepressant-like effects of SR 57227A, a 5-HT3 receptor agonist, in rodents.

Authors:  M Poncelet; A Perio; J Simiand; G Gout; P Soubrie; G Le Fur
Journal:  J Neural Transm Gen Sect       Date:  1995

5.  The effects of gamma-radiation on intestinal motor activity and faecal pellet expulsion in the guinea pig.

Authors:  A Krantis; K Rana; R K Harding
Journal:  Dig Dis Sci       Date:  1996-12       Impact factor: 3.199

6.  A phase I study of a new 5HT3-receptor antagonist, BRL43694A, an agent for the prevention of chemotherapy-induced nausea and vomiting.

Authors:  G Falkson; A J van Zyl
Journal:  Cancer Chemother Pharmacol       Date:  1989       Impact factor: 3.333

7.  Stimulation of gastrointestinal motility by cisplatin in the ferret: activation of an intrinsic cholinergic mechanism dissociated from emesis.

Authors:  H I Davidson; P L Andrews
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1993-05       Impact factor: 3.000

8.  Peptide YY3-36 and 5-hydroxytryptamine mediate emesis induction by trichothecene deoxynivalenol (vomitoxin).

Authors:  Wenda Wu; Melissa A Bates; Steven J Bursian; Brenna Flannery; Hui-Ren Zhou; Jane E Link; Haibin Zhang; James J Pestka
Journal:  Toxicol Sci       Date:  2013-03-01       Impact factor: 4.849

9.  5-HT3 receptor antagonists injected into the area postrema inhibit cisplatin-induced emesis in the ferret.

Authors:  G A Higgins; G J Kilpatrick; K T Bunce; B J Jones; M B Tyers
Journal:  Br J Pharmacol       Date:  1989-05       Impact factor: 8.739

10.  The role of serotonin as a mediator of emesis induced by different stimuli.

Authors:  A du Bois; H Kriesinger-Schroeder; H G Meerpohl
Journal:  Support Care Cancer       Date:  1995-09       Impact factor: 3.603

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