ArticleBritish journal of pharmacology1995
The broad-spectrum anti-emetic activity of the novel non-peptide tachykinin NK1 receptor antagonist GR203040.
Article in British journal of pharmacology, 1995. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers, 1 of them a synthesis that pooled it.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
16 citing papers in PubMed, 1 synthesis or guideline pooled it, 122 citations in OpenAlex.
- Cisplatin-induced emesis: systematic review and meta-analysis of the ferret model and the effects of 5-HT₃ receptor antagonists.Cancer chemotherapy and pharmacology · 2011Pooled it
- Comparative efficacy of metoclopramide, ondansetron and maropitant in preventing parvoviral enteritis-induced emesis in dogs.Journal of veterinary pharmacology and therapeutics · 2017Trial
- Pharmacological characterization and preclinical evaluation of 11h: a novel, brain-penetrant PDE4 inhibitor for neurological disorders.Frontiers in pharmacology · 2025Article
- Anti-emetic Action of the Brain-Penetrating New Ghrelin Agonist, HM01, Alone and in Combination With the 5-HTFrontiers in pharmacology · 2018Article
- Profile of Antiemetic Activity of Netupitant Alone or in Combination with Palonosetron and Dexamethasone in Ferrets and Suncus murinus (House Musk Shrew).Frontiers in pharmacology · 2016Article
- A Dunnione Compound MB12662 Improves Cisplatin-Induced Tissue Injury and Emesis.Biomolecules & therapeutics · 2015Article
- Recent advances in pharmacotherapy of chemotherapy-induced nausea and vomiting.Journal of advanced pharmaceutical technology & research · 2012Article
- Computerized detection and analysis of cancer chemotherapy-induced emesis in a small animal model, musk shrew.Journal of neuroscience methods · 2011Article
- Casopitant: a novel NK(1)-receptor antagonist in the prevention of chemotherapy-induced nausea and vomiting.Therapeutics and clinical risk management · 2009Article
- A multinational study to measure the value that patients with cancer place on improved emesis control following cisplatin chemotherapy.PharmacoEconomics · 2001Article
- Review
- Review
- The action of the NK1 tachykinin receptor antagonist, CP 99,994, in antagonizing the acute and delayed emesis induced by cisplatin in the ferret.British journal of pharmacology · 1996Article
- New perspectives in antiemetic treatment.Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer · 1996Review
- The pharmacology of GR203040, a novel, potent and selective non-peptide tachykinin NK1 receptor antagonist.British journal of pharmacology · 1995Article
- The involvement of TRPV1 in emesis and anti-emesis.Temperature (Austin, Tex.)Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. Following our earlier observations that the tachykinin NK1 receptor antagonist CP-99,994 is an effective anti-emetic in ferrets, we have examined the anti-emetic effects of a more potent and novel NK1 receptor antagonist, GR203040, against various emetic stimuli in the ferret, dog and house musk shrew (Suncus murinus). 2. In ferrets, GR203040 (0.1 mg kg-1 s.c. or i.v.) is effective against emesis induced by radiation, cisplatin, cyclophosphamide, copper sulphate, ipecacuanha or morphine. 3. In animals in which emesis had been established with cisplatin, GR203040 (1 mg kg-1 s.c.) was fully effective as an interventional treatment. No further emesis was seen in animals treated with GR203040 whilst saline-treated animals continued to vomit. 4. GR203040 (0.1 mg kg-1 s.c.) retains anti-emetic efficacy in the ferret, even when given as a 6 h pretreatment, indicating that this compound has a long duration of action. The compound is also effective orally at the same dose, when given as a 90 min pretreatment. 5. GR203040 (0.1 mg kg-1 i.v.) is fully effective against ipecacuanha-induced emesis in the dog. 6. GR203040 is effective against motion- and cisplatin-induced emesis in Suncus murinus. These effects were seen at doses an order of magnitude greater than those shown to be effective against cisplatin in the ferret. 7. In conclusion, GR203040 is a novel anti-emetic agent, and the broad spectrum of anti-emetic activity, together with activity observed in three species, suggests that this compound is worthy of clinical investigation.
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Registered trials
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