Synthesis and Development of Indole Based 5-HT3 Receptor Antagonists as Anti-Emetic Drugs in Oncology: An Update

Abstract

: An important group of anti-emetic drugs used in the treatment of nausea and vomiting after chemotherapy contains an indole moiety in their structures, working as 5-hydroxytryptamine type 3 serotonin receptor antagonist (5-HT3). This revision is focused on compounds bearing an indole core that present a 5-HT3 receptor antagonist activity that has been successfully used as anti-emetic drugs, reducing chemotherapy adverse secondary effects during cancer treatment. Their synthesis, biological activities, and some outstanding characteristics are discussed, affording a general outlook towards the development of more efficient anti-emetic drugs.

Therapeutic potential of pyrrole and pyrrolidine analogs: an update

“…Serotonin receptors were also responsible for aggression, anxiety, memory, learning, nausea, mood, and sleep [ 71 , 72 ]. Among such antagonists, tropisetron, a fused pyrrole, an indole analog blocks the action of serotonin at 5HT3 receptors, resulting in control of nausea and vomiting induced by chemotherapy and radiotherapy [ 73 , 74 ].…”

Evaluating Aprepitant single-dose plus granisetron and dexamethasone in children receiving highly emetogenic chemotherapy for the prevention of chemotherapy-induced nausea and vomiting: A triple-blinded randomized clinical trial

“… 6 Granisetron (Kytril) is a selective 5-HT 3 receptor antagonist which is recommended by clinical practice guidelines as an effective and potent antiemetic drug. 7 Application of antagonists of receptor 5-HT 3 , along (Shouldn't this be “prolonged”???) with DEX, can improve CINV in the acute stage, but the delayed CINV has remained an important clinical issue.…”