Gabapentin
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Gabapentin 속성
- 녹는점
- 162°C
- 끓는 점
- 314.4±15.0 °C(Predicted)
- 밀도
- 1.058±0.06 g/cm3(Predicted)
- 인화점
- 9℃
- 저장 조건
- 2-8°C
- 용해도
- H2O: 10 mg/mL
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 산도 계수 (pKa)
- pKa1 (25°) 3.68; pKa2 10.70
- 색상
- 회백색
- Merck
- 14,4319
- BRN
- 2359739
- BCS Class
- 3
- 안정성
- 제공된 대로 구매일로부터 1년 동안 안정적입니다. 증류수 용액은 -20°C에서 최대 3개월 동안 보관할 수 있습니다.
- InChIKey
- UGJMXCAKCUNAIE-UHFFFAOYSA-N
- CAS 데이터베이스
- 60142-96-3(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험품 표기 | T,Xi,F | ||
---|---|---|---|
위험 카페고리 넘버 | 61-36/37/38-39/23/24/25-23/24/25-11 | ||
안전지침서 | 53-26-36/37/39-45-36-36/37-16 | ||
WGK 독일 | 3 | ||
RTECS 번호 | GU6496000 | ||
위험 등급 | IRRITANT | ||
HS 번호 | 29224999 | ||
유해 물질 데이터 | 60142-96-3(Hazardous Substances Data) |
Gabapentin C화학적 특성, 용도, 생산
개요
Gabapentin was introduced in 1993 in the UK and early 1994 in the USA as an adjunctive therapy in the treatment of refractory partial seizures and secondarily generalized tonic-clonic seizures. Although being a lipophilic analog of the neurotransmitter GABA, gabapentin appears to exert its anticonvulsive function by a GABA receptor independent mechanism, possibly involving the L-system amino acid transporter protein. Gabapentin easily crosses the blood brain barrier and exhibits a favorable pharmacokinetic profile with high tolerability. It does not interfere with the metabolism of other concomitant administered antiepileptic drugs, thus having a low potential for drug interactions. Studies are currently underway for the use of gabapentin as mono-therapy for the treatment of various seizures.화학적 성질
White Crystalline Solid용도
Gabapentin is an Amino acid structurally related to γ-Aminobutyric Acid (GABA), designed to cross the blood brain barrier. Used as an anticonvulsant.정의
ChEBI: A gamma-amino acid that is cyclohexane substituted at position 1 by aminomethyl and carboxymethyl groups. Used for treatment of neuropathic pain and restless legs syndrome.Indications
Gabapentin (Neurontin) significantly decreases pain scores and sleep interference associated with PHN. An initial dose of 300 mg/day is increased over 4 weeks (900, 1,800, 2,400, 3,600 mg/day divided t.i.d.) until efficacy is obtained or side effects become intolerable.Biological Functions
Gabapentin (Neurotonin) was initially designed to be a rigid analogue of GABA. When it was discovered to have antiepileptic properties, it was assumed that this activity was related to a GABAergic mechanism. However, subsequent studies have failed to show any GABAergic activity of gabapentin. Although it has not yet been possible to ascribe any definite mechanism to its antiepileptic activity, there is recent evidence that it may function as an agonist at GABAB receptors in the brain.Gabapentin is recommended as adjunctive therapy in the treatment of partial seizures in adults.When used with other drugs, it appears to be an effective AED; it is usually not effective when employed alone for patients with severe seizures.
Gabapentin is generally well tolerated, with somnolence, dizziness, and ataxia the most commonly reported adverse effects. A low incidence of potentially serious side effects and no significant allergic reactions have been reported.
일반 설명
Gabapentin and its closely related analog pregabalin,(S)-3-isobutyl-GABA, are broad-spectrum anticonvulsantswith multiple mechanisms of action.24,51 Inaddition to modulating calcium influx and stimulateGABA biosynthesis as discussed earlier, they also competefor the biosynthesis of L-glutamic acid because oftheir structural similarity to L-leucine.51 Gabapentin andpregabalin have very little liability for causing metabolicbaseddrug–drug interactions, particularly when used incombination with other AEDs because they are not metabolizedin humans. More than 95% of the drug is excretedunchanged through the kidneys. However, there are somedifferences in their bioavailability. Unlike gabapentin,which exhibits 60% bioavailability when given in lowdoses because of intestinal uptake by a saturable smallneutral L-amino acid transporter, the absorption of pregabalinis almost complete (98%) and exhibits an ideal linear pharmacokinetic profile.24 This high bioavailability of pregabalincan be attributed to its closer structure similarity tothe essential amino acid, L-leucine.생물학적 활성
Anticonvulsant with several possible mechanisms of action. Increases GABA in the brain and binds to a novel site associated with voltage-sensitive Ca 2+ channels. Prevents neuronal death and is antinociceptive and anxiolytic.부작용
Long-Term Side Effects of Gabapentin:- Mood changes.
- Behavioral changes.
- Depression.
- Anxiety.
- Memory loss.
- Weakened muscles.
부작용
Dose-limiting adverse effects include somnolence, dizziness, ataxia, peripheral edema, and infection (22).Gabapentin 준비 용품 및 원자재
원자재
준비 용품
Gabapentin 공급 업체
글로벌( 824)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Sigma Audley | +86-15937194204 +86-18126314766 |
nova@sh-teruiop.com | China | 491 | 58 |
Baoji Guokang Bio-Technology Co., Ltd. | 0917-3909592 13892490616 |
gksales1@gk-bio.com | China | 9316 | 58 |
Hong Kong Excellence Biotechnology Co., Ltd. | |
ada@sh-teruiop.com | China | 882 | 58 |
Guangzhou TongYi biochemistry technology Co.,LTD | +8613073028829 |
mack@tongyon.com | China | 2996 | 58 |
Shaanxi TNJONE Pharmaceutical Co., Ltd | +8618740459177 |
sarah@tnjone.com | China | 1143 | 58 |
Dorne Chemical Technology co. LTD | +86-86-13583358881 +8618560316533 |
Ethan@dornechem.com | China | 3128 | 58 |
hebei hongtan Biotechnology Co., Ltd | +86-86-1913198-3935 +8617331935328 |
sales03@chemcn.cn | China | 973 | 58 |
Shaanxi Xianhe Biotech Co., Ltd | +8617709210191 |
Jerry@xhobio.com | China | 484 | 58 |
Shaanxi Dideu Medichem Co. Ltd | +86-29-81148696 +86-15536356810 |
1022@dideu.com | China | 3878 | 58 |
Sinoway Industrial co., ltd. | 0592-5800732; +8613806035118 |
xie@china-sinoway.com | China | 988 | 58 |
Gabapentin 관련 검색:
메틸사이클로헥산 D-글루코사민 아세트산 에틸사이클로헥산 시트르산 엽산 페닐사이클로헥세인 피리딘 하이드로클로라이드 헥사하이드로니트로벤젠 사이클로헥세인
Glycyl-glycyl-glycine
Cyclohexylacetic acid
Topotecan hydrochloride
Hyaluronic acid
Methoxyammonium chloride
Ascoric Acid
(1-[(9H-FLUOREN-9-YLMETHOXYCARBONYLAMINO)-METHYL]-CYCLOHEXYL)-ACETIC ACID
GABAPENTIN-D6 HYDROCHLORIDE