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プレガバリン

プレガバリン 化学構造式
148553-50-8
CAS番号.
148553-50-8
化学名:
プレガバリン
别名:
(S)‐(+)‐プレガバリン‐D4;プレガバリン;プレガバリン 溶液;プレガバリン (JAN)
英語化学名:
Pregabalin
英語别名:
Lyrica;Pregablin;PREGABALIN;Pregabilin;Neugaba 75;Maxgalin 75;APIPregabalin;(R)-Pregabalin;(S)-Pregabalin;xiangxizhiliao
CBNumber:
CB2251105
化学式:
C8H17NO2
分子量:
159.23
MOL File:
148553-50-8.mol

プレガバリン 物理性質

融点 :
194-196°C
比旋光度 :
D23 +10.52° (c = 1.06 in water)
沸点 :
274.0±23.0 °C(Predicted)
比重(密度) :
0.997±0.06 g/cm3(Predicted)
闪点 :
9℃
貯蔵温度 :
Store at RT
溶解性:
deionized water: ≥10mg/mL
酸解離定数(Pka):
4.23±0.10(Predicted)
外見 :
white powder
InChIKey:
AYXYPKUFHZROOJ-ZETCQYMHSA-N
CAS データベース:
148553-50-8(CAS DataBase Reference)
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  Xn,T,F
Rフレーズ  63-48/22-39/23/24/25-23/24/25-11
Sフレーズ  22-36/37-45-16-7
RIDADR  UN1230 - class 3 - PG 2 - Methanol, solution
WGK Germany  3
HSコード  29224999
有毒物質データの 148553-50-8(Hazardous Substances Data)
絵表示(GHS)
注意喚起語 Danger
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
H225 引火性の高い液体および蒸気 引火性液体 2 危険 P210,P233, P240, P241, P242, P243,P280, P303+ P361+P353, P370+P378,P403+P235, P501
H318 重篤な眼の損傷 眼に対する重篤な損傷性/眼刺激 性 1 危険 P280, P305+P351+P338, P310
H361 生殖能または胎児への悪影響のおそれの疑い 生殖毒性 2 警告 P201, P202, P281, P308+P313, P405,P501
H370 臓器の障害 特定標的臓器有害性、単回暴露 1 危険 P260, P264, P270, P307+P311, P321,P405, P501
注意書き
P210 熱/火花/裸火/高温のもののような着火源から遠ざ けること。-禁煙。
P260 粉じん/煙/ガス/ミスト/蒸気/スプレーを吸入しないこ と。
P280 保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。
P301+P310 飲み込んだ場合:直ちに医師に連絡すること。
P305+P351+P338 眼に入った場合:水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。
P311 医師に連絡すること。

プレガバリン 価格 もっと(5)

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
Sigma-Aldrich Japan P-066 プレガバリン 溶液 1.0?mg/mL in methanol, ampule of 1?mL, certified reference material
Pregabalin solution 1.0?mg/mL in methanol, ampule of 1?mL, certified reference material
148553-50-8 1ml ¥46300 2018-12-25 購入
Sigma-Aldrich Japan P-120 プレガバリン 溶液 10.0?mg/mL in water, ampule of 1?mL, certified reference material
Pregabalin solution 10.0?mg/mL in water, ampule of 1?mL, certified reference material
148553-50-8 1ml ¥130300 2018-12-25 購入
Sigma-Aldrich Japan PZ0010 プレガバリン ≥97% (NMR)
Pregabalin ≥97% (NMR)
148553-50-8 25mg ¥97300 2018-12-25 購入
Sigma-Aldrich Japan PZ0010 プレガバリン ≥97% (NMR)
Pregabalin ≥97% (NMR)
148553-50-8 5mg ¥25600 2018-12-25 購入
Sigma-Aldrich Japan Y0001805 プレガバリン EuropePharmacopoeia (EP) Reference Standard
Pregabalin EuropePharmacopoeia (EP) Reference Standard
148553-50-8 y0001805 ¥33600 2018-12-25 購入

プレガバリン 化学特性,用途語,生産方法

用途

末梢性神経障害性疼痛、繊維筋痛症に伴う疼痛。

効能

抗けいれん薬, 疼痛治療

商品名

リリカ (ファイザー)

説明

As a follow-up to its g-aminobutyric acid (GABA) agonist gabapentin, Pfizer has developed and launched pregabalin for the treatment of epilepsy and neuropathic pain. Although pregabalin is a structural analog of GABA, it does not interact with GABA-A or GABA-B receptors or influence GABA uptake. The exact mechanism of action is unclear, but pregabalin may reduce excitatory neurotransmitter release by binding to the α2-δ protein subunit of voltage-gated calcium channels. The resulting inhibition of excess neuronal activity is believed to be the basis for pregabalin’s efficacy in epilepsy and neuropathic pain alleviation. Since the activity is attributed to the (S′)-enantiomer alone, an efficient asymmetric synthesis is employed for commercial production. The key step is the asymmetric hydrogenation of 3-cyano-5-methyl-3-hexenoic acid using a chiral rhodium catalyst to afford an intermediate that is enriched in the (S′)-enantiomer. The cyano group is ultimately reduced by routine hydrogenation with a nickel catalyst. Further enrichment of the final product is realized by selective recrystallization with (S′)-mandelic acid or simply recrystallizing from water/isopropanol. Compared to gabapentin, pregabalin is 2- to 10-fold more potent in various animal models. For example, in preventing maximal electroshock seizures (MES) in mice, pregabalin has an ED50 of 20 mg/kg p.o. versus 87 mg/kg for gabapentin. A comparable increase in potency is also observed in the rat MES model (ED50=1.8mg=kg p.o. for pregabalin versus 10.3 mg/kg for gabapentin). In addition, pregabalin’s linear pharmacokinetics (Cmax relates to dose) translates to better predictability of pharmacological effects. It has 90% oral bioavailability, with an elimination half-life of approximately 6 h. The primary route of excretion is via the renal system with negligible metabolism. Furthermore, its lack of activity at the cytochrome P450 enzymes was reflected in an absence of pharmacokinetic drug-drug interactions in relevant studies. In a placebocontrolled, fixed dose (up to 600mg/day) trial with pregabalin as an adjunctive therapy for epilepsy, 14 to 51% of patients showed at least a 50% decrease in seizure frequency with a clear dose-response relationship. In a flexible dosing group, (150 mg/day to 600 mg/day), the seizure reduction rate was 35.4%compared to 40.3% for a fixed dose of 600mg/day and 10.6% for placebo. The most common side effects were dizziness (29%) and somnolence (21%). In addition, weight gain (equal to or more than 7% increase from baseline) occurred in 40% of patients in the 12-week study; however, there was no affect on male fertility or efficacy of oral contraceptives in women. Regarding the use of pregabalin in treating painful diabetic peripheral neuropathy, oral administration of 300 and 600 mg/day t.i.d. was superior to placebo (39–48% compared to 15–18% with placebo) in relieving pain and improving pain-related sleep interference. While pregabalin was originally developed as an anticonvulsant for epilepsy, its success in treating neuropathic pain has led to its exploration in treating other CNS disorders, such as, anxiety, social phobia, and fibromyalgia.

化学的特性

Off-White Solid

Originator

Warner-Lambert (US)

使用

S-Enantiomer of Pregabalin. A GABA analogue used as an anticonvulsant. Anxiolytic analgesic used to treat peripheral neuropathic pain and fibromyalgia.

使用

Pregabalin is an anticonvulsant drug used for neuropathic pain, as an adjunct therapy for partial seizures, and in generalized anxiety disorder. It was designed as a more potent successor to gabapentin. Pregabalin is marketed by Pfizer under the trade nam

brand name

Lyrica (CP).

プレガバリン 上流と下流の製品情報

原材料

準備製品


プレガバリン 生産企業

Global( 446)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
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales04@yibaibiotech.com CHINA 420 58
Cangzhou Wanyou New Material Technology Co.,Ltd
18631714998
sales@czwytech.com CHINA 914 58
-
18292830413 029-86107037-8014
sales7@konochemical.com CHINA 3000 58
Hebei Huanhao Biotechnology Co., Ltd.
+8618034552304
86-0311-83975816 cathylee@hbhuanhao.com CHINA 861 58
Hebei Xibaijie Biotechnology Co., Ltd.
0086 15203217809
sales@hbxibaijie.com CHINA 544 58
Casorganics US Corp
+17326109938
sales@casorganics.com CHINA 175 58
Jinan Jianfeng Chemical Co., Ltd
15562555968
info@pharmachemm.com CHINA 304 58
Hebei shuoxi biotechnology co. LTD
+8613081092107
whatsapp:+8613081092107 julia@hbshuoxi.com CHINA 973 58
Shijiazhuang Suking Biotechnology Co .,Ltd. Co., Ltd.
18732196011
18732196011 sales2@sxbiology.com CHINA 307 58
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 19929 60

148553-50-8(プレガバリン)キーワード:


  • 148553-50-8
  • Pregabalin Manufacturer
  • Pregabalin SynonyMs 3-(AMinoMethyl)-5-Methyl-hexanoic acid
  • Pregabalin 3-(Aminomethyl)-5-methyl-hexanoic acid
  • Pregabaline ada@tuskwei.com whatsapp
  • (S)-3-(Aminomethyl)-5-methylhexanoic acid (Pregabalin)
  • Pregabalin solution
  • Hexanoic acid, 3-(aminomethyl)-5-methyl-, (3S)-
  • Pregabalin and Intermediates
  • 3(S)-(AMINOMETHYL)-5-METHYLHEXANOIC ACID
  • (3S)-3-(AMINOMETHYL)-5-METHYLHEXANOIC ACID
  • PREDNISOLONESODIUMPHOSPHATE
  • (R)-Pregabalin
  • (S)-Pregabalin
  • (S)-3-(Ammoniomethyl)-5-methylhexanoate
  • Lyrica
  • PREGABALIN
  • Pregablin
  • 3(S)-(AMINOMETHYL)-5
  • LYRICA (pregabalin)
  • Pregabalin-13C3 RaceMic
  • PREGABALINE (S)-(+)-3-AMinoMethyl-5-Methylhexanoic acid
  • (S)-(+)-Pregabalin-d4
  • xiangxizhiliao
  • Pregabalin (S)-(+)-3-AMinoMethyl-5-Methylhexanoic acid
  • (S)-Pregabalin (1.0 Mg/ML in Methanol)
  • Pregabalin kf-wang(at)kf-chem.com
  • API Pregabalin 148553-50-8 wickr alinalee
  • Pregabalin cas148553-50-8(whatsapp:+8618830163278)
  • Maxgalin 75
  • ACTIVE PHARMACEUTICALS INGRADIENTS : PRE GABALIN 3-( AMINOMETHYL)-5-METHYL-HEXANO IC ACID (OTHER) [TAX I
  • (S)‐(+)‐プレガバリン‐D4
  • プレガバリン
  • プレガバリン 溶液
  • プレガバリン (JAN)
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