Zatosetron Explained

Zatosetron (LY-277,359) is a drug which acts as an antagonist at the 5HT₃ receptor^[1] It is orally active and has a long duration of action, producing antinauseant effects but without stimulating the rate of gastrointestinal transport.^{[2] [3]} It is also an effective anxiolytic in both animal studies and human trials,^[4] although with some side effects at higher doses.^{[5] [6]}

See also

• Ondansetron
• Bemesetron
• Granisetron
• Ricasetron
• Tropanserin
• Tropisetron

Notes and References

1. Cohen ML, Bloomquist W, Gidda JS, Lacefield W . LY277359 maleate: a potent and selective 5-HT3 receptor antagonist without gastroprokinetic activity . The Journal of Pharmacology and Experimental Therapeutics . 254 . 1 . 350–5 . July 1990 . 2366187 .
2. Robertson DW, Lacefield WB, Bloomquist W, Pfeifer W, Simon RL, Cohen ML . Zatosetron, a potent, selective, and long-acting 5HT3 receptor antagonist: synthesis and structure-activity relationships . Journal of Medicinal Chemistry . 35 . 2 . 310–9 . January 1992 . 1732548 . 10.1021/jm00080a016 .
3. Schwartz SM, Goldberg MJ, Gidda JS, Cerimele BJ . Effect of zatosetron on ipecac-induced emesis in dogs and healthy men . Journal of Clinical Pharmacology . 34 . 3 . 250–4 . March 1994 . 7517409 . 10.1002/j.1552-4604.1994.tb03994.x . 23486859 .
4. Smith WT, Londborg PD, Blomgren SL, Tollefson GD, Sayler ME . Pilot study of zatosetron (LY277359) maleate, a 5-hydroxytryptamine-3 antagonist, in the treatment of anxiety . Journal of Clinical Psychopharmacology . 19 . 2 . 125–31 . April 1999 . 10211913 . 10.1097/00004714-199904000-00006 .
5. Williams PD, Calligaro DO, Colbert WE, Helton DR, Shetler T, Turk JA, Jordan WH . General pharmacology of a new potent 5-hydroxytryptamine antagonist . Arzneimittel-Forschung . 41 . 3 . 189–95 . March 1991 . 1867653 .
6. Bendele A, Means J, Shoufler J, Schmalz C, Hanasono G, Symanowski J, Adams E . Chronic toxicity of zatosetron, a 5-HT3 receptor antagonist, in rhesus monkeys . Drug and Chemical Toxicology . 18 . 1 . 61–82 . February 1995 . 7768200 . 10.3109/01480549509017858 .