Azasteron is mostly administered by i.v and orally (approximately 60-70%) and excreted in the urine as an unmetabolized form. Orally-administered azasetron is shown to be absorbed and secreted by the saturable transport mechanism in the small intestine, resulting in good bioavailability as approximately 90%.
產品描述
A Potent Blocker of Serotonin-Gated Channels
產品形式
Y-25130 hydrochloride (Azasetron hydrochloride) is a potent 5-HT3 receptor antagonist. It selectively and competitively binds to 5-HT3 receptors thereby blocking the serotonin binding site. Azasetron is classified as a derivative of benzamide. It has a different chemical structure from other 5-HT3 receptor blockers. The significant difference is found in the pharmacokinetic profiles resulting in a longer duration of action and a higher affinity for the 5HT3 receptor. Azasetron has an IC50 value ~ 4.9x10-10 M4 and half life of 5.4 hours.
