rolapitant hydrochloride hydrate

Rolapitant, also known as SCH-619734, is an orally bioavailable, centrally-acting, selective, neurokinin 1 receptor (NK1-receptor) antagonist with potential antiemetic activity. Upon oral administration, rolapitant competitively binds to and blocks the activity of the NK1-receptor in the central nervous system, thereby inhibiting the binding of the endogenous ligand, substance P (SP). This may prevent both SP-induced emesis and chemotherapy-induced nausea and vomiting (CINV). The interaction of SP with the NK1-receptor plays a key role in the induction of nausea and vomiting caused by emetogenic cancer chemotherapy.

Rolapitant (SCH619734) hydrochloride 是一种高效选择性和具有口服活性的神经激肽 1 (NK1) 受体拮抗剂，Ki 值为 0.66 nM。Rolapitant hydrochloride (Rolapitant HCl) 不与 CYP3A4 产生互作。Rolapitant hydrochloride 在雪貂呕吐模型中显示出强效的中枢介导的止吐活性。

Rolapitant (SCH619734) 是一种高效选择性具有口服活性的神经激肽 1 受体抑制剂，Ki 值为0.66 nM。