Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0042963 (vomiting)
 31,883 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Vomiting may be induced by a variety of agents such as drugs, oncolytics, and provocative motion, as well as being conditioned to occur to environmental stimuli. Such emesis has recently been shown to be blocked by agonists at the 5-HT1A subtype of serotonin receptor. The antiemetic effects of LY228729 [(-)-4-(dipropylamine)-1,3,4,5-tetrahydrobenz-(c,d)indole-6- carboxamide], a 5-HT1A receptor agonist, were tested and compared to the antiemetic effects of the 5-HT3 receptor antagonists ondansetron, tropisetron, and MDL 72222 (3-tropanyl-3,5-dichlorobenzoate). The emetic stimuli tested are known to be blocked by 5-HT3 antagonists in species other than the pigeon. In the pigeon, LY228729 totally abolished vomiting induced by fully emetic doses of cisplatin (10 mg/kg), ipecac (3 ml/kg), emetine (10 mg/kg), and a 5-HT3 agonist, m-(chlorophenyl)-biguanide (1.25 mg/kg). MDL 72222 blocked ipecac-induced vomiting in a dose-related manner and was partially effective in attenuating cisplatin-induced emesis. Ondansetron and tropisetron were partially effective in blocking emetine- and mCPBG-induced vomiting. Ondansetron exhibited an intrinsic emetic response that could not be blocked by MDL 7222, but which was eliminated by LY228729. It was concluded that 5-HT1A agonists are more effective in the pigeon than are 5-HT3 antagonists against these types of emetic stimuli. These results broaden the range of emetic stimuli that are blocked by 5-HT1A agonists in the pigeon.
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PMID:Comparison of the antiemetic effects of a 5-HT1A agonist, LY228729, and 5-HT3 antagonists in the pigeon. 854 76

The aim of this manuscript is to introduce Cryptotis parva (the least shrew) as a new experimental emesis model. The chemotherapeutic agent, cisplatin, caused a dose-dependent increase in the number of animals exhibiting vomiting and retching behaviours with ED50 values of 6.43+/-1 and 7.9+/-1.2 mg/kg, respectively. The frequencies of these parameters were also dose-dependent. Intraperitoneal administration of 5-HT3 receptor antagonists (tropisetron or MDL 72222) prevented cisplatin-induced emesis and retching behaviours in the least shrew by a dose-dependent mechanism with respective ID50 values of 4.28+/-2.8 and 2.05+/-2 for emesis, and 2.71+/-4.5 and 2.52+/-2.59 for retching. Intraperitoneal injection of selective and nonselective 5-HT3 receptor agonists potently, and in a dose-dependent fashion, induced emesis in the least shrew with the following ED50 potency order: 2-methyl 5-HT approximately 5-HT (p > 0.05) <5-HTQ (p < 0.01) <mCPBG (p < 0.001). As with other established experimental animal emesis models, the present data indicate that cisplatin causes emesis by activating 5-HT3 receptors indirectly via release of 5-HT.
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PMID:Serotonin 5-HT3 receptor antagonists prevent cisplatin-induced emesis in Cryptotis parva: a new experimental model of emesis. 992 84