Ziprasidone

한글명:Ziprasidone

카스 번호146939-27-7

상품명:Ziprasidone

CBNumberCB6167417

분자식C21H21ClN4OS

포뮬러 무게412.94

MOL 파일146939-27-7.mol

화학적 성질

녹는점	213-215°C
끓는 점	554.8±50.0 °C(Predicted)
밀도	1.369±0.06 g/cm3(Predicted)
저장 조건	Sealed in dry,Room Temperature
용해도	DMSO(약간 용해됨), 메탄올(약간 용해됨)
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	13.34±0.20(Predicted)
색상	갈색에서 진한 갈색까지
Merck	14,10171
CAS 데이터베이스	146939-27-7(CAS DataBase Reference)

위험 및 안전 성명

위험품 표기	F,T
위험 카페고리 넘버	60-61-11-19-38
안전지침서	53-45
RTECS 번호	NM3241000
HS 번호	2934.20.8000
유해 물질 데이터	146939-27-7(Hazardous Substances Data)

그림문자(GHS)

Ziprasidone 화학적 특성, 용도, 생산

화학적 성질
Tan Solid
용도
Labelled Ziprasidone, which is used as an antipsychotic. Combined serotonin (5HT2) and dopamine (D2) receptor antagonist.
정의
ChEBI: A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.
Biological Functions
"Ziprasidone is chemically similar to risperidone but with a substitution of piperzinyl and benzisothiazole for piperidinyl and benzisoxazole and with minor aromatic modification. Like risperidone, ziprasidone is a high-affinity antagonist at 5-HT2A/C and D2 receptors as well as at adrenergic α1/α2 and histamine H1 receptors. Moreover, ziprasidone can activate 5-HT1A receptors that regulate dopaminergic neurotransmission in brain regions involved in critical cognitive functions. Thus, in addition to D2 partial agonism, 5-HT1A agonism is now thought to be an important pharmacological property for atypical antipsychotic drug efficacy.
일반 설명
Ziprasidone (Geodon, a benzisothiazolpiprazinylindolonederivative) also has the structuralfeatures of a hybrid molecule between a butyrophenone antipsychoticand a trazodone-like antidepressant. It is highlymetabolized to four major metabolites, only one of which, Smethyldihydroziprasidone,likely contributes to its clinical activity. In humans, less than 5% of the dose isexcreted unchanged. Reduction by aldehyde oxidase accountsfor about 66% of ziprasidone metabolism; two oxidative pathwaysinvolving hepatic CYP3A4 account for the remainder.
Mechanism of action
Ziprasidone (half-life, 6 hours) has an oral bioavailability of approximately 60%, which can be enhanced in the presence of fatty foods. It is extensively metabolized (<5% excreted unchanged) by aldehyde oxidase, which results in reductive cleavage of the S–N bond, and then by S-methylation. Ziprasidone also can undergo CYP3A4-catalyzed N-dealkylation and S-oxidation.

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