| Identification | Back Directory | [Name]
rolapitant hydrochloride (anhydrous) | [CAS]
858102-79-1 | [Synonyms]
rolapitant hydrochloride (anhydrous) | [Molecular Formula]
C25H27ClF6N2O2 | [MDL Number]
MFCD22572774 | [MOL File]
858102-79-1.mol | [Molecular Weight]
536.937 |
| Hazard Information | Back Directory | [Uses]
Rolapitant is an NK1 receptor antagonist that is used in the treatment of chemotherapy-induced nausea and vomiting. | [Definition]
ChEBI: Rolapitant hydrochloride (anhydrous) is a hydrochloride obtained by combining irinotecan with one molar equivalent of hydrochloric acid. Used (in the form of the hydrate) for the prevention of delayed nausea and vomiting associated with initial and repeat courses of emetogenic cancer chemotherapy. It has a role as an antiemetic and a neurokinin-1 receptor antagonist. It contains a rolapitant(1+). | [in vivo]
Rolapitant (0.03-1 mg/kg for PO, 0.3-1 mg/kg for IV; single dosage) attenuates the GR-73632-induced foot-tapping response in Mongolian Gerbils[1].
Rolapitant (0.03-1 mg/kg; PO; single dosage; observed for 72 h) blocks acute emesis induced by both apomorphine and cisplatin in ferrets[1]. | Animal Model: | Female Mongolian Gerbils (30-60 g; anesthetized by inhalation of an oxygen:isofluorane mixture after 4 h PO or immediately after IV, then injected with 5 μl of 3 pmol solution of GR-73632 via ICV)[1] | | Dosage: | 0.03, 0.1, 0.3 and 1 mg/kg for PO, 0.3 and 1 mg/kg for IV | | Administration: | PO or IV, single dosage | | Result: | Attenuated dose-dependently the GR-73632-induced foot-tapping response when administered PO 4 h before testing, with an ID90 of 0.3 mg/kg, and the inhibition in foot tapping for at least 24 h.
Blocked dose-dependently the foot tapping induced by GR-73632 when administered IV, with complete blockade observed at 1 mg/kg. |
| Animal Model: | Ferrets (treated with subcutaneous administration of 0.125 mg/kg apomorphine or intraperitoneal administration of 10 mg/kg cisplatin)[1] | | Dosage: | 0.03, 0.1, 0.3 and 1 mg/kg | | Administration: | PO; single dosage; observed for 72 h | | Result: | Blocked dose-dependently acute emesis induced by both apomorphine and cisplatin in ferrets.
Produced a robust decrease in retches and vomits in ferrets that was maintained throughout the 72 h observation period. |
| [IC 50]
human NK1: 0.66 (Ki); gerbil NK1: 0.13 (Ki); guinea pig NK1: 0.72 (Ki); monkey NK1: 2.5 (Ki); rabbit NK1: 31.7 (Ki); rat NK1: 78.6 (Ki); mouse NK1: 60.4 (Ki) |
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cjbscvictory
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13348960310 13348960310 |
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https://www.weikeqi-biotech.com/ |
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