Rapid communicationAnti-emetic profile of a non-peptide neurokinin NK1 receptor antagonist, CP-99,994, in ferrets
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Selectivity of 5-HT3 receptor antagonists and anti-emetic mechanisms of action
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Cited by (155)
Strategies to mitigate the toxicity of cancer therapeutics
2022, Advances in Cancer ResearchPerioperative use of centrally acting angiotensin-converting enzyme inhibitor may increase patients' risk for postoperative nausea and vomiting
2016, Medical HypothesesCitation Excerpt :SP induces vomiting by binding to NK-1 receptors, which are expressed in the abdominal vagus, the NTS and the AP [16]. Further evidence of the role of SP in vomiting was provided by investigating the antiemetic effect of SP antagonists (SPAs) in animal models [17–20]. Of note, only SPAs that could penetrate into the brain were effective [21].
The differential antiemetic properties of GLP-1 receptor antagonist, exendin (9-39) in Suncus murinus (house musk shrew)
2014, NeuropharmacologyCitation Excerpt :It also antagonises lithium chloride-induced conditioned gaping (a putative model of nausea) in rats when combined with a subthreshold dose of cannabidiolic acid (Rock and Parker, 2013). Tachykinin NK1 receptor antagonists have broad spectrum anti-emetic activity against various emetic stimuli including cisplatin, radiation, copper sulphate, ipecacuanha, morphine (Bountra et al., 1993; Gardner et al., 1995, 1996), apomorphine (Watson et al., 1995), loperamide (Watson et al., 1995), and motion (Lucot et al., 1997). Previous studies in our laboratories have shown that subcutaneous administration of CP-99,994 significantly reduced emesis induced by cisplatin and nicotine (Lau et al., 2005; Rudd et al., 1999b).
Molecular mechanisms of 5-HT<inf>3</inf> and NK<inf>1</inf> receptor antagonists in prevention of emesis
2014, European Journal of PharmacologyCitation Excerpt :NK1 receptor antagonists were shown to be effective against emesis induced by a variety of emetogens, including cisplatin in animal models of emesis. The results paved the way for NK1 receptor antagonists to be recognized as new therapeutic agents for the treatment of CINV in cancer patients (Bountra et al., 1993). The first NK1 receptor antagonists were developed in the 1980s; they were peptides (Engberg et al., 1981) or peptidomimetics (Quartara and Maggi, 1997a) based on SP.
Broad-spectrum antiemetic potential of the L-type calcium channel antagonist nifedipine and evidence for its additive antiemetic interaction with the 5-HT<inf>3</inf> receptor antagonist palonosetron in the least shrew (Cryptotis parva)
2014, European Journal of PharmacologyCitation Excerpt :More recent research effort in antiemetic drug development has focused on producing receptor-selective antagonists that could have broad-spectrum antiemetic potential with fewer side-effects. In fact the development of NK1 receptor antagonists in the early 1990s introduced the notion of a universal antiemetic in the realm of frequently used emesis models such as the ferret (Bountra et al., 1993). However, such observed broad-spectrum antiemetic efficacy of selective NK1 receptor antagonists in larger species unfortunately failed to fully translate either in the clinic for patients, or in the laboratory for the smaller species, the least shrew.
Rolapitant (SCH 619734): A potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets
2012, Pharmacology Biochemistry and BehaviorCitation Excerpt :Neurokinin NK1 receptors have been shown to play a role in a variety of behavioral responses in both animals and humans which has lead to the development of selective antagonists for this receptor (for review see Duffy, 2004). Principal among the properties of NK1 antagonists is their inhibitory effects against emesis induced by a variety of emetogenic stimuli (Bountra et al., 1993; Tattersall et al., 1993) resulting in the NK1 antagonist aprepitant (Emend®) being approved and marketed for the treatment of chemotherapy-induced nausea and vomiting (CINV) and post-operative nausea and vomiting (PONV) (Diemunsch et al., 2009; Rupniak and Kramer, 1999; Diemunsch and Grelot, 2000). A variety of NK1 antagonists have been consistently shown to demonstrate a robust, dose-related, anti-emetic profile across a diverse range of animal models (Watson et al., 1995; Rudd et al., 1996, 1999; Tattersall et al., 1994, 1996; Gardner et al., 1995, 1996; Singh et al., 1997).