Ziprasidone Hydrochloride

CP-88059 HCl · CP88059 hydrochloride · CP 88059 hydrochloride · CP-88059 hydrochloride · ZIPRASIDONE HYDROCHLORIDE · Ziprasidone HCl (CP-88059) · Ziprasidone hydrochloride, 10 mM in DMSO · Ziprasidone hydrochloride (CP-88059 hydrochloride

https://huagongshe.com/ko/chemical/219099

식별자 및 물리적 특성

CAS No.	122883-93-6
분자식	C21H22Cl2N4OS
평균 분자량	449.4 g/mol
단동위원소 질량	448.08913768 g/mol
SMILES	Cl.O=C1Cc2cc(CCN3CCN(c4nsc5ccccc45)CC3)c(Cl)cc2N1
InChIKey	NZDBKBRIBJLNNT-UHFFFAOYSA-N
PubChem CID	219099
ChEMBL	CHEMBL1375743
EC No.	602-903-0
DTXSID	DTXSID00153762

화학 및 물리적 성질

극성 표면적	76.7
수소 결합 공여자 수	2
수소 결합 수용자 수	5
회전 가능 결합 수	4
무거운 원자 수	29
형식 전하	0
복잡도	573
Human Drugs	Breast FeedingLactationMilk, HumanAntipsychotic AgentsFDA approved drugs -> Active ingredient
녹는점	>300 °C
저장 조건	Store at -20°C
용해도	Soluble in DMSO > 10 mM
물리적 상태	가루
안정성	흡습성
InChI	1S/C21H21ClN4OS.ClH.H2O/c22-17-13-18-15(12-20(27)23-18)11-14(17)5-6-25-7-9-26(10-8-25)21-16-3-1-2-4-19(16)28-24-21/h1-4,11,13H,5-10,12H2,(H,23,27)
InChIKey	ZCBZSCBNOOIHFP-UHFFFAOYSA-N

안전 및 규제

GHS 분류	This chemical does not meet GHS hazard criteria for 33.3% (1 of 3) of reports.WarningH315 (33.3%): Causes skin irritation [Warning Skin corrosion/irritation]P260, P261, P264, P264+P265, P271, P272, P280, P302+P352, P304+P340, P305+P351+P338, P319, P321, P332+P317, P333+P317, P337+P317, P362+P364, P403+P233, P405, and P501 (click each P-code to see the statement)Aggregated GHS information provided per 3 reports by companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
Hazard Classes and Categories	Skin Irrit. 2 (33.3%)
Drug Induced Liver Injury	Drug Induced Liver Injury Rank (DILIrank 2.0)Ziprasidone hydrochloridevLess-DILI-concern3Adverse reactionsDOI:10.1016/j.drudis.2016.02.015
Effects During Pregnancy and Lactation	◉ Summary of Use during Lactation
수질 위해 등급(WGK)	WGK 2
위험 등급	Acute Tox. 3 DermalAcute Tox. 3 InhalationAcute Tox. 3 OralFlam. Liq. 2STOT SE 1
저장 분류	3 - Flammable liquids

용도

개요

Both p.o. and i.m. formulations of ziprasidone were launched in Sweden for the treatment of schizophrenia and agitated psychoses. It is the sixth marketed atypical antipsychotic after clozapine, risperidone, olanzapine, sertindole and quetiapine. The synthesis of ziprasidone involves a novel one-step process for the preparation of 3-(1- piperazinyl)-1,2-benzisothiazole followed by coupling with a chlorooxindole fragment. Ziprasidone is a very potent 5-HT2A/D2 antagonist with a ratio of about 11 in favor of the serotonin receptor. It also shows very high 5-HT2c antagonistic activity, high 5-HT1A agonistic and 5-HT1D antagonistic activity, as well as moderate antagonism of α1 and H1 receptors and moderate norepinephrine and serotonin reuptake inhibition. Its complex binding profile for serotonin and dopamine receptors resulted during clinical trials in high antipsychotic efficacy with low extrapyramidal side effects and also in antidepressive action with low propensity for weight gain in opposition to other atypical and typical neuroleptics. An intramuscular formulation of ziprasidone was demonstrated to be superior to haloperidol, a conventional neuroleptic, for the short-term treatment of agitation in acutely psychotic patients. When administered orally in the fed state, this well-tolerated agent which strongly binds to plasma proteins shows a bioavailability of about 60% which is almost 2 fold greater than in the fasted state. It is transformed into 4 circulating major metabolites by different enzyme systems. The small QTc prolongation observed with ziprasidone was found to be comparable to other antipsychotic drugs and it is considered to be without significant risk.

용도

Ziprasidone (Geodon, Zeldox) was the fifth atypical antipsychotic to gain FDA approval. In the United States, Ziprasidone is approved for the treatment of schizophrenia, and the intramuscular injection form of ziprasidone is approved for acute agitation i

일반 설명

A Certified Spiking Solution; applicable to use in forensic drug analysis or calibrator preparation by LC/MS or GC/MS. Ziprasidone is sold under the trade names Geodon and Zeldox for treatment of schizophrenia and bipolar disorder. Recent studies have suggested that Ziprasidone may increase the risk of Type II diabetes and hyperglycemia.