Paliperidone
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Paliperidone 속성
- 녹는점
- 158-160°C
- 끓는 점
- 612.3±65.0 °C(Predicted)
- 밀도
- 1.45±0.1 g/cm3(Predicted)
- 인화점
- 9℃
- 저장 조건
- 2-8°C
- 용해도
- DMSO: 용해성2mg/mL, 투명(가온)
- 산도 계수 (pKa)
- 13.00±0.60(Predicted)
- 물리적 상태
- 가루
- 색상
- 흰색에서 갈색으로
- 안정성
- 제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO의 솔루션은 -20°에서 최대 2개월 동안 보관할 수 있습니다.
- InChI
- InChI=1S/C23H27FN4O3/c1-14-17(23(30)28-9-2-3-19(29)22(28)25-14)8-12-27-10-6-15(7-11-27)21-18-5-4-16(24)13-20(18)31-26-21/h4-5,13,15,19,29H,2-3,6-12H2,1H3
- InChIKey
- PMXMIIMHBWHSKN-UHFFFAOYSA-N
- SMILES
- C12C(O)CCCN1C(=O)C(CCN1CCC(C3C4=C(ON=3)C=C(F)C=C4)CC1)=C(C)N=2
- CAS 데이터베이스
- 144598-75-4(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험품 표기 | T,F | ||
---|---|---|---|
위험 카페고리 넘버 | 25-39/23/24/25-23/24/25-11 | ||
안전지침서 | 45-36/37-16 | ||
유엔번호(UN No.) | UN 2811 6.1/PG 3 | ||
WGK 독일 | 3 | ||
RTECS 번호 | UV1164720 | ||
위험 등급 | 6.1 | ||
포장분류 | III | ||
HS 번호 | 29349990 | ||
유해 물질 데이터 | 144598-75-4(Hazardous Substances Data) | ||
독성 | rat,LD50,oral,65mg/kg (65mg/kg),Drug Development Research. Vol. 33, Pg. 399, 1994. |
Paliperidone C화학적 특성, 용도, 생산
개요
Paliperidone, the C-9 hydroxylated active metabolite of the antipsychotic agent risperidone, is the newest atypical antipsychotic to join the market following the introductions of olanzapine (ZyprexaTM), risperidone (RisperdalTM), quetiapine(SeroquelTM), and ziprasidone (GeodonTM). Compared to its parent, paliperidone has improved PK properties and a reduced potential for drug interactions. In terms of receptor affinity, the two drugs are equipotent.화학적 성질
Off White to Light Orange Coloured Solid용도
Paliperidone(Invega) is an atypical antipsychotic. Chemically, paliperidone is the primary active metabolite of the older atypical antipsychotic risperidone. It is indicated for the acute and maintenance treatment of schizophrenia일반 설명
Paliperidone, (±)-3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one(Invega), is essentially insoluble in water and is available asextended-release tablets. Paliperidone is delivered at a constantrate using an osmotic drug release device (OsmoticRelease Oral Systems [OROS]). The absolute bioavailabilityof paliperidone is 28%, and studies in healthy subjects on ahigh-fat, high-calorie meal showed an increase in AUC.Paliperidone is 74% bound to plasma proteins. After a single,1-mg dose of C-paliperidone, 59% of the dose was excretedin the urine as unchanged drug, and 32% of the dose was recoveredas metabolites. Most of the drug (80%) is excreted bythe kidneys. Paliperidone is metabolized by dealkylation, hydroxylation,dehydrogenation, and scission of the benzoxazolering. None of these metabolic pathways account for morethan 10% of the dose. The terminal elimination half-life ofpaliperidone is 23 hours.부작용
The most common adverse events included tachycardia, QTc prolongation, headache, anxiety, dizziness, tremors, and insomnia along with the dose-related events of somnolence, orthostatic hypotension, salivary hypersecretion, and extrapyrimidal disorder. Weight gain was also observed in 6–9% of patients which may be attributable to paliperidone’s lower affinity for H1-histaminergic and a1- and a2-adrenergic receptors. Patients with renal impairment require dose adjustments since elimination of paliperidone is altered. Paliperidone is contraindicated in patients with a hypersensitivity to risperidone. Concomitant use of class III antiarrhythmic agents should be avoided since this may result in additive QT interval prolongation. Also, loss of levodopa efficacy is expected with this D2 antagonist.참고 문헌
1) Beijsterveldt?et al.?(1994),?Regional brain distribution of risperidone and its active metabolite 9-hydroxy-risperidone in the rat; Psychopharmacology,?114?53 DOI:10.1007/BF022454442) Leysen?et al. (1994),?Risperidone: a novel antipsychotic with balanced serotonin-dopamine antagonism, receptor occupancy profile, and pharmacologic activity; J. Clin. Psychiatry,?55?suppl: 5 PMID: 7520908
3) Schotte?et al.?(1996),?Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding; Psychopharmacology (Berl.),?124?57 DOI:10.1007/BF02245606
Paliperidone 준비 용품 및 원자재
원자재
준비 용품
Paliperidone 공급 업체
글로벌( 548)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Jewim Pharmaceutical (Shandong) Co., Ltd. | +86-15552509998 +86-15621883869 |
liutf@jewim.com.cn | China | 251 | 58 |
Aceschem Inc. | +1-817863-6948 +1-(817)863-6948 |
sales@aceschem.com | United States | 19639 | 58 |
Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +8617865335152 |
Mandy@hangyubiotech.com | China | 11013 | 58 |
Sinoway Industrial co., ltd. | 0592-5800732; +8613806035118 |
xie@china-sinoway.com | China | 992 | 58 |
Shaanxi TNJONE Pharmaceutical Co., Ltd | +8618740459177 |
sarah@tnjone.com | China | 1142 | 58 |
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 |
sales@capotchem.com | China | 29797 | 60 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21688 | 55 |
Hangzhou FandaChem Co.,Ltd. | 008657128800458; +8615858145714 |
fandachem@gmail.com | China | 9341 | 55 |
Nanjing ChemLin Chemical Industry Co., Ltd. | 025-83697070 |
product@chemlin.com.cn | CHINA | 3012 | 60 |
Lianyungang happen teng technology co., LTD | 15950718863 |
wang666xt@163.com | CHINA | 295 | 58 |
Paliperidone 관련 검색:
술파메톡사졸 1-히드록시에틸리덴-1,1-디포스포닌산 리스페리돈 2,2,6,6-사메틸-4-피페리디놀 이소옥사졸 메틸에틸케톤
Risperidone Impurity 2
9-Keto Risperidone
Paliperidone Palmitate
Paliperidone N-Oxide
Paliperidone Palmitate N-Oxide
Oxiracetam
ILOPERIDONE
(2-Methoxyethyl)benzene
2,2,6,6-Tetramethylpiperidinooxy
4-Ethyl-5-fluoro-6-hydroxypyrimidine
6-Fluoro-3-(4-piperidinyl)benzisoxazole hydrochloride (Paliperidone)
3-(2-Chloroethyl)-2-methyl-9-benzyloxy-4H-pyrido[1,2-a]pyrimidin-4-one (Paliperidone)