Serotonin 5-HT3 receptor antagonist

An important advance in this field has been made by the discovery of selective serotonin (5-HT3) receptor antagonists that are effective inhibitors of cytotoxic drug-induced emesis in laboratory animals. The new agents have been found to be free of the undesirable side-effects associated with dopaminergic blockade and have shown significant protection from emesis in early clinical trials. 

Greenshaw AJ, Silverstone PH. (1997). The non-antiemetic uses of serotonin 5-HT3 receptor antagonists. Clinical pharmacology and therapeutic applications. Drugs. 53(1) 20-39. 

Bell shaped concentration-effect relationships (an Emax curve, followed by a decrease in effect when concentrations are further increased) have been observed for a number of drugs. Concerning serotonin 5-HT3 receptor antagonists, a decrease in effect was reported with increasing doses of tropisetron and dolasetron. This implies a bell shaped concentration-effect relationship, which may be due to the fact... 

Several other drugs have shown efficacy in maintaining abstinence and reducing craving in chronic alcoholism, although none yet has FDA approval for this use. Such drugs include ondansetron, a serotonin 5-HT3-receptor antagonist (see... 

Radulovacki M, Trbovic SM, Carley DW (1998) Serotonin 5-HT3-receptor antagonist GR 38032F suppresses sleep apneas in rats. Sleep 21 131-136... 

Fozard JR. The development and early clinical evaluation of serotonin 5-HT3 receptor antagonists. In Fozard JR, ed., The Peripheral Actions of 5-Hydroxy-tryptamine. Oxford Oxford University Press, 1989 355-376. 

Giordano J, Rogers L (1989) Peripherally administered serotonin 5-HT3 receptor antagonists reduce inflammatory pain in rats. Eur J Pharmacol 170 83-86 GUck SD, Crane LA (1978) Opiate-like and abstinence-like effects of intracerebral histeimine administration in rats. Nature 273 547-549... 

Boess FG, de Vry J, Erb C, Flessner T, Hendrix M, Luithle J et al (2013) Pharmacological and behavioral profile of N-[(3R)-l-azabicyclo[2.2.2]oct-3-yl]-6-chinolincarboxamide (EVP-5141), a novel a7 nicotinic acetylcholine receptor agonist/ serotonin 5-HT3 receptor antagonist. Psychopharmacology (Berl) 227 1-17... 

Ondansetron Alcohol Ondansetron is a serotonin 5-HT3 receptor antagonist, with low affinity for al-adrenergic, 5-HTiB, 5-HTiC, and J-opioid receptors [251]. It is used primarily to treat nausea and vomiting (antiemetic) following chemotherapy. 

Ondansetron, a serotonin (5-HT3)-receptor antagonist (0.15 mg/kg IV with the first dose taken infused every 15 minutes before the start of chemotherapy), is used in the prevention of nansea and vomiting associated with initial and repeat conrses of emetogenic cancer chemotherapy, including high-dose cisplatin (see Figure 73). 

Darmani, N.A. (1998) Serotonin 5-HT3 receptor antagonists prevent cisplatin-induced emesis in Cryptotis parva a new experimental model of emesis, J. Neural Trans. 105 1143-1154. 

Ondansetron is a seleaive serotonin 5-HT3 receptor antagonist. It blocks 5-HT3 receptors in the central CTZ and peripheral vagus nerve resulting in the reduaion of vomiting reflex... 

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