ChemicalBook
Chinese english Germany Korea

プラジカンテル

プラジカンテル 化学構造式
55268-74-1
CAS番号.
55268-74-1
化学名:
プラジカンテル
别名:
ビルトリシド;プラジクアンテル;ドロンシット;エンベイ8440;プラジカンテル;2-(シクロヘキシルカルボニル)-1,3,4,6,7,11b-ヘキサヒドロ-2H-ピラジノ[2,1-a]イソキノリン-4-オン;2-(シクロヘキシルカルボニル)-1,2,3,6,7,11b-ヘキサヒドロ-4H-ピラジノ[2,1-a]イソキノリン-4-オン;ピキトン;プラジカンテル標準品;プラジクアンテル標準品;プラジカンテル (JAN)
英語化学名:
Praziquantel
英語别名:
Cesol;Azinox;droncit;WarMnil;pyquiton;Prazinon;embay8440;Distocide;Cysticide;biltricide
CBNumber:
CB8178956
化学式:
C19H24N2O2
分子量:
312.41
MOL File:
55268-74-1.mol

プラジカンテル 物理性質

融点 :
136-138 C
沸点 :
1377℃
比重(密度) :
1.1209 (rough estimate)
屈折率 :
1.5600 (estimate)
闪点 :
>110°(230°F)
貯蔵温度 :
−20°C
溶解性:
ethanol: soluble5mg/mL
酸解離定数(Pka):
-0.98±0.20(Predicted)
外見 :
powder or crystals
色:
Crystals from EtOAc/hexane
水溶解度 :
Freely soluble in ethanol or dichloromethane. Slightly soluble in water
Merck :
13,7802
BRN :
761557
EPAの化学物質情報:
Praziquantel (55268-74-1)
安全性情報
  • リスクと安全性に関する声明
  • 危険有害性情報のコード(GHS)
主な危険性  F,C
Rフレーズ  11-34
Sフレーズ  16-26-36/37/39-45-24/25
WGK Germany  1
RTECS 番号 UQ4150000
HSコード  29339900
毒性 LD50 in mice, rats (mg/kg): 2000-3000 orally; >3000 s.c. (Muermann)
絵表示(GHS)
注意喚起語
危険有害性情報
コード 危険有害性情報 危険有害性クラス 区分 注意喚起語 シンボル P コード
H303 飲み込むと有害のおそれ 急性毒性、経口 5 P312
注意書き

プラジカンテル 価格 もっと(22)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01FLC358136
2-cyclohexanecarbonyl-1H,2H,3H,4H,6H,7H,11bH-piperazino[2,1-a]isoquinolin-4-one
55268-74-1 10g ¥9200 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01FLC358136
2-cyclohexanecarbonyl-1H,2H,3H,4H,6H,7H,11bH-piperazino[2,1-a]isoquinolin-4-one
55268-74-1 25g ¥17800 2018-12-26 購入
東京化成工業 P2125 プラジカンテル >98.0%(HPLC)(N)
Praziquantel >98.0%(HPLC)(N)
55268-74-1 25g ¥18200 2018-12-04 購入
東京化成工業 P2125 プラジカンテル >98.0%(HPLC)(N)
Praziquantel >98.0%(HPLC)(N)
55268-74-1 5g ¥5200 2018-12-04 購入
関東化学株式会社(KANTO) 49829-48 プラジカンテル標準品
Praziquantel standard
55268-74-1 250mg ¥12000 2018-12-13 購入

プラジカンテル 化学特性,用途語,生産方法

外観

白色, 結晶性粉末〜粉末

溶解性

エタノール及びアセトンに溶け、水にほとんど溶けない。

用途

プラジカンテル (praziquantel) は、吸虫駆除剤の一つである。

効能

駆虫薬 (獣医薬)

商品名

ビルトリシド (バイエル薬品)

化学的特性

White Solid

使用

anthelmintic; EMBAY-8440

使用

Anthelmintic, effective against flatworms.

適応症

The neuromuscular effects of praziquantel (Biltricide) appear to increase parasite motility leading to spastic paralysis. The drug increases calcium permeability through parasite-specific ion channels, so that the tegmental and muscle cells of the parasite accumulate calcium.This action is followed by vacuolization and the exposure of hitherto masked tegmental antigens, lipidanchored protein, and actin. Insertion of the drug into the fluke’s lipid bilayer causes conformational changes, rendering the fluke susceptible to antibody- and complement-mediated assault.

brand name

Biltricide (Bayer).

獲得抵抗性

There is evidence that resistance to praziquantel is emerging in schistosomes, although there is debate as to whether treatment failures are due to resistance or innate tolerance.

応用例(製薬)

A synthetic pyrazinoquinoline formulated for oral administration. It is stable in the dry state, but hygroscopic.

作用機序

Praziquantel is readily absorbed (80% in 24 hours) after oral administration, with serum concentrations being maximal in 1 to 3 hours; the drug has a half-life of 0.8 to 1.5 hours. Its bioavailability is reduced by phenytoin or carbamazepine and increased by cimetidine. Dexamethasone decreases plasma praziquantel levels by 50%. Praziquantel is excreted by the kidneys.

薬物動態学

Oral absorption: >80%
Cmax 50 mg/kg oral: 1 mg/L after 1–2 h
Plasma half-life: parent drug: 1–1.5 h
metabolites: 4–6h
Plasma protein binding: 80%
Praziquantel is rapidly absorbed when given orally, but it undergoes extensive first-pass biotransformation and the concentration of unchanged drug in plasma is low. The major metabolite, a 4-hydroxy derivative, retains little to no antiparasitic activity. About 80% of the oral dose, as parent drug and its metabolites, is excreted in the urine by the fourth day post-treatment, 90% of this in 24 h. A higher peak plasma concentration is achieved in infected people, but other pharmacokinetic values are unchanged.

臨床応用

2-(Cyclohexylcarbonyl)-1,2,3,6,7, 11b-hexahydro-4Hpyrazino[2,1-a]isoquinolin-4-one (Biltricide) is a broadspectrumagent that is effective against various trematodes (flukes). It has become the agent of choice for the treatmentof infections caused by schistosomes (blood flukes).
The drug also provides effective treatment for fasciolopsiasis(intestinal fluke), clonorchiasis (Chinese liver fluke),fascioliasis (sheep liver fluke), opisthorchosis (liver fluke),and paragonimiasis (lung fluke). Praziquantel increases cellmembrane permeability of susceptible worms, resulting inthe loss of extracellular calcium. Massive contractions andultimate paralysis of the fluke musculature occurs, followedby phagocytosis of the parasite.
Following oral administration, about 80% of the doseis absorbed. Maximal plasma concentrations are achievedin 1 to 3 hours. The drug is rapidly metabolized in theliver in the first-pass. It is likely that some of the metabolitesare also active. Praziquantel occurs as a white crystallinesolid that is insoluble in water. It is available as600-mg film-coated tablets. The drug is generally welltolerated.

臨床応用

Praziquantel is an extremely active broad-spectrum anthelmintic that is well tolerated. It is the most effective of the drugs used in the treatment of schistosomiasis, possessing activity against male and female adults and immature stages. Unlike other agents, it is active against all three major species (S. haematobium, S. mansoni, and S. japonicum). In addition, it has activity against other flukes, such as C. sinensis, Paragonimus westermani, O. viverrini, and the tapeworms (D. latum, H. nana, T. saginata, and T. solium). It is not as effective against F. hepatica. It is used effectively in the treatment of clonorchiasis and paragonimiasis and is an effective alternative agent to niclosamide in the treatment of tapeworm infestations.

臨床応用

Schistosomiasis
Other trematode infections (except F. hepatica)
Tapeworm infection, including cerebral cysticercosis
Treatment may need to be prolonged in cerebral cysticercosis.

副作用

Very few side effects have been reported. In the treatment of cerebral cysticercosis the death of cysts in the brain may cause local inflammation and edema, but this usually subsides quickly. Ocular cysticercosis should not be treated with this drug, because parasite destruction in the eye can lead to irreparable lesions. Adverse events seen in the treatment of schistosomiasis, including abdominal pain, nausea, anorexia, diarrhea and mild neurological effects, are almost certainly due to the death and disintegration of the large adult worms.

副作用

Adverse reactions tend to occur within a few hours of administration. They include gastrointestinal intolerance with nausea, vomiting, and abdominal discomfort. This may be due to the liberation of helminth proteins from dead worms rather than any direct effect of the drug.

安全性プロファイル

Poison by intraperitoneal route.Moderately toxic by ingestion and other routes. Humanmutation data reported. When heated to decomposition itemits toxic fumes of NOx.

Veterinary Drugs and Treatments

Praziquantel is indicated for (approved labeling) for the treatment of Dipylidium caninum, Taenia pisiformis, and Echinococcus granulosis in dogs, and Dipylidium caninum and Taenia taeniaeformis in cats. Fasting is not required nor recommended before dosing. A single dose is usually effective, but measures should be taken to prevent reinfection, particularly against D. caninum. Praziquantel can also be used for treating Alaria spp. in dogs and cats and Spirometra mansonoides infections in cats.
Praziquantel has been used in birds and other animals, but it is usually not economically feasible to use in large animals. In humans, praziquantel is used for schistosomiasis, other trematodes (lung, liver, intestinal flukes) and tapeworms. It is not routinely effective in treating F. hepatica infections in humans.
Combination products can give a wide spectrum of internal parasite control in a variety of species.

プラジカンテル 上流と下流の製品情報

原材料

準備製品


プラジカンテル 生産企業

Global( 392)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
Frapp's ChemicalNFTZ Co., Ltd.
+86 (576) 8169-6106
+86 (576) 8169-6105 sales@frappschem.com China 886 50
Capot Chemical Co.,Ltd.
+86-571-85586718
+86-571-85864795 sales@capotchem.com China 19920 60
Beijing Cooperate Pharmaceutical Co.,Ltd.
+86-10-60279497 +86(0)15646567669
+86-10-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22631 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070
product@chemlin.com.cn CHINA 3015 60
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 739 60
Hubei XinRunde Chemical Co., Ltd.
+8615102730682
02783214688 bruce@xrdchem.cn CHINA 569 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24687 60
Hefei TNJ Chemical Industry Co.,Ltd.
86-0551-65418684 18949823763
86-0551-65418684 info@tnjchem.com China 1892 55
Hebei Chisure Biotechnology Co., Ltd.
+8613292890173
0311 66567340 luna@speedgainpharma.com CHINA 1012 58

55268-74-1(プラジカンテル)キーワード:


  • 55268-74-1
  • embay8440
  • praz,quantel
  • pyquiton
  • PRAZIQUANTEL
  • 2-(CYCLOHEXYLCARBONYL)-1,2,3,6,7-11BETA-HEXAHYDRO-4H-PYRAZINO[2,1A] ISOQUINOLIN-4-ONE
  • 2-[CYCLOHEXYLCARBONYL]-1,2,3,6,7-11B-HEXAHYDRO-4H-PYRAZINO[2,1A]ISOQUINOLIN-4-ONE
  • 2-cyclohexyl-carbonyl-1,3,4,6,7,11b-hexahydro-2h-pyrazine(2,1-a)isoquinoline-4-one
  • PRAZIQUANTEL BP 98
  • PRAZIQUANTEL F&D VERSION
  • PRAZIQUANTEL VETRANAL, 250 MG
  • PraziquantelUsp25
  • 4H-Pyrazino[2,1-a]isoquinolin-4-one, 2-(cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro- (9CI)
  • Azinox
  • Cesol
  • 1-a]-isoquinolin-4-one,2-(cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-4H-pyrazino-[2
  • 2-cyclohexylcarbonyl-1,2,3,6,7,11b-hexahydro-4h-pyrazino(2,1-a)isoquinolin-4
  • 4h-pyrazino(2,1-a)isoquinolin-4-one,2-(cyclohexylcarbonyl)-1,2,3,6,7,11b-hexah
  • 4H-pyrazino-[2,1-a]-isoquinolin-4-one,2-(cyclohexylcarbonyl)-1,2,3,6,7,11b-hexahydro-
  • biltricide
  • droncit
  • Praziquintel (FDA)
  • 2-(Cyclohexanecarbonyl)-1,3,4,6,7,11b-hexahydro-4H-pyrazino[2,1-α]isoquinolin-4-one
  • Usnea diffract
  • Praziquantel (200 mg)
  • (11bS)-2-cyclohexanecarbonyl-1H,2H,3H,4H,6H,7H,11bH-piperazino[2,1-a]isoquinolin-4-one
  • Praziquantel, Pyquiton
  • Distocide
  • Prazinon
  • Praziguantel
  • Prazichantel
  • ビルトリシド
  • プラジクアンテル
  • ドロンシット
  • エンベイ8440
  • プラジカンテル
  • 2-(シクロヘキシルカルボニル)-1,3,4,6,7,11b-ヘキサヒドロ-2H-ピラジノ[2,1-a]イソキノリン-4-オン
  • 2-(シクロヘキシルカルボニル)-1,2,3,6,7,11b-ヘキサヒドロ-4H-ピラジノ[2,1-a]イソキノリン-4-オン
  • ピキトン
  • プラジカンテル標準品
  • プラジクアンテル標準品
  • プラジカンテル (JAN)
  • 駆虫薬
Copyright 2017 © ChemicalBook. All rights reserved