EMANA 76272-56-5 For Granisetron

EMANA is an intermediate of Granisetron which as one of the most important means of cancer treatment with positive effect, chemotherapy dose have many adverse reactions, among which vomiting is one of the most serious. The purpose of antiemetic therapy is to prevent or reduce the frequency and intensity of nausea and vomiting associated induced by chemotherapy. Early antiemetic drugs used in clinical practice have severe nerve center inhibition or extrapyramidal adverse reactions. Therefore, a variety of highly selective 5-ht3 receptor blockers have been developed since the 1980s and gradually develops into the mainstream drugs for the treatment of nausea and vomiting caused by chemotherapy. Based on the mechanism antiemetic drugs can be divided into dopamine blockers, vomiting central inhibitors, antihistamines, corticosteroids, 5-ht3 receptor blockers, and nk-1 receptor blockers.

Since the launch of the first generation highly selective 5 - HT3 receptor blockers Ondansetron, a series of 5 - HT3 receptor blockers derivatives with determined curative effect and less adverse reaction have been used clinically, such as Granisetron, Navoban, Azasetron.

Mechanisms: the mechanism of chemotherapy induced nausea and vomiting is very complex which mainly includes the following aspects: the majority of cytotoxic drugs can stimulate the gastrointestinal mucosa causing mucosa damage and lead the chromaffin cells on mucous membrane, especially from the stomach to the ileal mucosa to release 5-HT which combines 5 - HT3 receptor to generate nerve impulses spreading to vomiting center forming vomiting; chemotherapeutic drugs and the metabolites stimulate and activate the vomiting center to form vomit; the various toxic substances in blood can act on the vomiting center unprotected by blood-brain barrier and the signal can be passed to vomiting center causing vomiting, the vomiting center reacts to a variety of stimuli which are activated through a series of receptors (dopamine receptors, histamine receptors, muscarine receptors, 5-HT3 receptors). Most antiemetic drugs also play a role in acting on one or more receptors. 5-HT is an important central transmitter in the human body. Its receptor is divided into 4 types,5-HT1, 5-HT2, 5-HT3, 5-HT4 and several subtypes. 5 - HT3 receptor blockers can be applied to the 5-HT3 receptors on vagus nerve to inhibit the excitement of vagal into fibers and inhibit the activation of AP and NTS 5 - HT3 by acting on the receptors, thus blocking afferent impulse to the vomiting center and inhibiting vomiting.