포사프레피탄트디메글루민

한글명:포사프레피탄트디메글루민

카스 번호265121-04-8

상품명:Fosaprepitant dimeglumine

CBNumberCB61105364

분자식C30H39F7N5O11P

포뮬러 무게809.63

MOL 파일265121-04-8.mol

동의어(한글)

포사프레피탄트디메글루민

화학적 성질

저장 조건	Sealed in dry,Store in freezer, under -20°C
용해도	≥50.24 mg/mL in DMSO; insoluble in EtOH; ≥13.16 mg/mL in H2O with ultrasonic
물리적 상태	가루
산도 계수 (pKa)	Fosaprepitant dimeglumine has four functional groups which have pKa values of 3.05 ± 0.03, 4.92 ± 0.02, 9.67 ± 0.01 and 10.59 ± 0.03. The pka value of 3.05 corresponds to the morpholinium group, the pka of 4.92 corresponds to the monophosphonate group, the pka of 9.67 corresponds to the meglumine counter ion, and the pka of 10.59 corresponds to the triazolinone NH group.
색상	White to off-white

그림문자(GHS)

포사프레피탄트디메글루민 화학적 특성, 용도, 생산

개요
Fosaprepitant dimeglumine belongs to the group of antiemetics. The active substance inhibits part of the vomiting centre. It is used for the treatment of postoperative or chemotherapyinduced nausea and vomiting.
화학적 성질
Fosaprepitant dimeglumine is a white to off-white amorphous powder. It is freely soluble in water. The pH of a 1.0 g sample of fosaprepitant dimeglumine, dissolved in 25 mL of water, is approximately 8.3. Fosaprepitant, a prodrug of aprepitant, when administered intravenously is rapidly converted to aprepitant.
용도
Fosaprepitant-d4 Dimeglumine is a labeled analogue of Fosaprepitant Dimeglumine (F727305), a selective neurokinin-1 (NK-1) receptor antahonist. Fosaprepitant is an antiemetic drug, a Aprepitant (A729800) prodrug.
Indications
Fosaprepitant dimeglumine is a new drug indicated to prevent nausea and vomiting associated with highly emetogenic cisplatin-based and moderately emetogenic cancer chemotherapy in adults.
정의
ChEBI: Fosaprepitant dimeglumine is an organoammonium salt obtained by reaction of fosaprepitant with two equivalents of 1-deoxy-1-(methylamino)-D-glucitol. A substance P/neurokinin 1 (NK1) receptor antagonist. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting and postoperative nausea and vomiting It has a role as a prodrug, an antiemetic and a neurokinin-1 receptor antagonist. It contains a fosaprepitant(2-).
생물학적 활성
Fosaprepitant dimeglumine acts as a therapeutic agent to treat chemotherapy-induced nausea and vomiting. It also acts as a weak inhibitor of cytochrome P450 3A4 (CYP3A4).
Fosaprepitant dimeglumine is a Substance P/neurokinin-1 (NK1) receptor antagonist. It is a water soluble prodrug of the antiemetic drug aprepitant.
Fosaprepitant dimeglumine is a water-soluble prodrug form of the neurokinin-1 receptor antagonist aprepitant. Formulations containing fosaprepitant dimeglumine have been used to prevent chemotherapy-induced nausea and vomiting.
부작용
Most common adverse reactions in adults (≥2%) are: fatigue, diarrhea, neutropenia, asthenia, anemia, peripheral neuropathy, leukopenia, dyspepsia, urinary tract infection, pain in extremity.
Adverse reactions in pediatrics are similar to adults.

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