5‐HT3 receptor antagonists injected into the area postrema inhibit cisplatin‐induced emesis in the ferret

@article{Higgins19895HT3RA,
  title={5‐HT3 receptor antagonists injected into the area postrema inhibit cisplatin‐induced emesis in the ferret},
  author={Guy A Higgins and Gavin Kilpatrick and Keith Thomas Bunce and Brian J. Jones and Michael Brian Tyers},
  journal={British Journal of Pharmacology},
  year={1989},
  volume={97}
}
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… Expand
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  • N. Darmani
  • Biology, Medicine
  • Journal of Neural Transmission
  • 1998
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TLDR
The results indicate that stimulation of abdominal vagal afferent nerves via peripheral 5-HT3 receptors is important for triggering cisplatin- and m-chlorophenylbiguanide-induced emesis in ferrets. Expand
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TLDR
The residual or delayed phase of cisplatin-induced emesis may involve a 5-HT-independent mechanism, compared to the problem of acute and delayed emesis in man. Expand
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TLDR
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TLDR
It is concluded that non-NMDA antagonists effectively inhibit cisplatin-induced emesis in ferrets and are potential antiemetic compounds, alone or in combination with 5-HT3 antagonists or other more conventional drugs of choice. Expand
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TLDR
The involvement of 5-hydroxytryptamine (5-HT) with cisplatin-induced emesis in the ferret was investigated using reserpine, para-chlorophenylalanine and fenfluramine and other treatments reduced levels of dopamine and noradrenaline. Expand
Pharmacological properties of GR38032F, a novel antagonist at 5‐HT3 receptors
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R,S‐GR38032F is highly selective for 5‐HT3 receptors, and at concentrations of 3 × 10‐6‐3 × 10−5m, had negligible agonist or antagonist activity on other 5‐ HT or non‐5‐HT receptor‐containing tissues on which it was tested. Expand
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TLDR
Five‐HT, PBG and 2‐methyl‐5‐HT had no demonstrable agonist effects at non‐5-HT receptors on the rat vagus nerve, and Tropacaine and m‐chlorophenylpiperazine were found to behave as reversible competitive antagonists of 5‐HT‐induced depolarization of thevagus nerve. Expand
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TLDR
Direct evidence for the existence of 5-HT3 receptors in rat brain tissue and their distribution is reported, based on high affinity binding of the potent 5- HT3 receptor antagonist 3H-GR65630 to homogenates of rat entorhinal cortex. Expand
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MDL 72222, the selective 5‐hydroxytryptamine (5‐HT) M‐receptor antagonist, prevented or reduced cisplatin‐induced emesis in ferrets. It is suggested that cisplatin‐induced, and possibly otherExpand
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TLDR
It is demonstrated that the area postrema, the anatomic site of the chemoreceptor trigger zone for emesis, is essential for cisplatin-induced vomiting, which suggests a possible mechanism for other emetogenic anticancer agents. Expand
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TLDR
It is demonstrated that the area postrema, the anatomic site of the chemoreceptor trigger zone for emesis, is essential for cisplatin-induced vomiting, which suggests a possible mechanism for other emetogenic anticancer agents. Expand
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TLDR
The potent antiemetic action of GR38032F should be of clinical value in reducing the nausea and vomiting associated with radiotherapy or chemotherapy of cancer. Expand
PREVENTION OF EMESIS IN PATIENTS RECEIVING CYTOTOXIC DRUGS BY GR38032F, A SELECTIVE 5-HT3 RECEPTOR ANTAGONIST
15 patients receiving cytotoxic drugs (other than cisplatin) that had previously produced nausea and vomiting refractory to first-line antiemetics were given a selective 5-HT3 receptor antagonistExpand
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