갈란타민

갈란타민
갈란타민 구조식 이미지
카스 번호:
357-70-0
한글명:
갈란타민
동의어(한글):
갈란타민
상품명:
Galanthamine
동의어(영문):
GALANTAMINE;Galantamin;Razadyne;Galantamina;Galanthamine-d3 HCl;(4aS,8aS)-4a,5,9,10,11,12-Hexahydro-3-methoxy-11-methyl-6H-benzofuro[3a,3,2-ef][2]benzazepin-6β-ol;Jilkon;ReMinyl;R-113675;Nevalina
CBNumber:
CB8345888
분자식:
C17H21NO3
포뮬러 무게:
287.35
MOL 파일:
357-70-0.mol

갈란타민 속성

녹는점
119-1210C
알파
D20 -118.8° (c = 1.378 in ethanol)
끓는 점
429.65°C (rough estimate)
밀도
1.0662 (rough estimate)
굴절률
1.5022 (estimate)
저장 조건
Sealed in dry,Room Temperature
용해도
≥14.37 mg/mL in DMSO; ≥14.43 mg/mL in H2O with gentle warming; ≥45 mg/mL in EtOH with gentle warming
물리적 상태
가루
산도 계수 (pKa)
pKa 8.32 (Uncertain)
색상
White to off-white
CAS 데이터베이스
357-70-0(CAS DataBase Reference)
NIST
Galantamin(357-70-0)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
유해 물질 데이터 357-70-0(Hazardous Substances Data)
독성 LD50 intraperitoneal in mouse: 10mg/kg
그림문자(GHS): GHS hazard pictogramsGHS hazard pictograms
신호 어: Danger
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H315 피부에 자극을 일으킴 피부부식성 또는 자극성물질 구분 2 경고 GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H317 알레르기성 피부 반응을 일으킬 수 있음 피부 과민성 물질 구분 1 경고 GHS hazard pictograms P261, P272, P280, P302+P352,P333+P313, P321, P363, P501
H319 눈에 심한 자극을 일으킴 심한 눈 손상 또는 자극성 물질 구분 2A 경고 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H373 장기간 또는 반복 노출되면 장기(또는, 영향을 받은 알려진 모든 장기를 명시)에 손상을 일으킬 수 있음 특정 표적장기 독성 - 반복 노출 구분 2 경고 P260, P314, P501
H410 장기적 영향에 의해 수생생물에 매우 유독함 수생 환경유해성 물질 - 만성 구분 1 경고 GHS hazard pictograms P273, P391, P501
예방조치문구:
P260 분진·흄·가스·미스트·증기·...·스프레이를 흡입하지 마시오.
P261 분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P272 작업장 밖으로 오염된 의복을 반출하지 마시오.
P273 환경으로 배출하지 마시오.
P280 보호장갑/보호의/보안경/안면보호구를 착용하시오.
P302+P352 피부에 묻으면 다량의 물로 씻으시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
P314 불편함을 느끼면 의학적인 조치·조언을 구하시오.
P321 (…) 처치를 하시오.
P332+P313 피부 자극이 생기면 의학적인 조치· 조언을 구하시오.
P333+P313 피부자극성 또는 홍반이 나타나면 의학적인 조치·조언를 구하시오.
P362 오염된 의복을 벗고 세척 후에 재사용하기
P363 다시 사용전 오염된 의류는 세척하시오.
P391 누출물을 모으시오.
P501 ...에 내용물 / 용기를 폐기 하시오.

갈란타민 C화학적 특성, 용도, 생산

개요

Galantamine is an Amaryllidaceae alkaloid which is first obtained from the plant of snowdrop (Galanthus nivalis), and nowadays, it’s extracted from the plants of Narcissus and Galanthus species or obtained from chemosynthesis. In many areas in Europe such as Bulgaria, eastern Turkey, and the Caucasus, the plants of Galanthus are native species. But its earliest pharmaceutical applications are seldom known. Plaitakis and Duvoisin hypothesized that “moly” in ancient Homer’s epic might be snowdrops. In Homer’s epic Odyssey, “moly” was used as an antidote by Odysseus against Circe’s poisonous drugs. To be used as an antidote may be the plants of Galanthus’ oldest medicinal records. But there is not much evidence for that. There is little evidence of the traditional application of the plants of Galanthus, and it is certain that until the Second World War, the plants of Galanthus and other genera of Amaryllidaceae were not frequently used in European drugs
Italian scholar Iannello studied Pancratium illyricum L., an Amaryllidaceae species endemic to Sardinia, and isolated a new galantamine-type alkaloid in its leaves. This new galantamine-type compound exhibited a pronounced in?vitro AChE inhibitory activity (IC50? =? 3.5±1.1? μM) in comparison with the reference standard galantamine hydrobromide (IC50?=?1.5±0.2?μM)

화학적 성질

Off-White Solid

물리적 성질

Hydrobromide of galantamine can be used as drug although galantamine can’t be used as drugs
Appearance: an almost white powder. Solubility: soluble in water; slightly soluble in alcohol; and insoluble in acetone, trichloromethane, and diethyl ether. Melting point: 269–270?°C. Specific optical rotation: ?90 to ?100°.

출처

Galanthamine is a bulb plant found throughout the world.

역사

In the early 1950s, Soviet Union’s scientists started modern medicine research of galantamine. In 1951, the Soviet Union’s pharmacologist Mashkovsky and Kruglikova-Lvova firstly proved its AChE-inhibiting properties, which was published in the paper. In 1957, the Bulgarian pharmacologist Paskov et?al. found that the plants of Galanthus were the richest sources of galantamine, which opened a way for its commercial development by the company Sopharma in Bulgaria. Galantamine hydrobromide was launched into market under the trade name Nivalin. Initially, Nivalin was used in anesthesia to antagonize the effects of non-depolarizing muscle relaxants, and since then, it was rapidly introduced in other areas of medicine
Galantamine hydrobromide was launched into market for the indication of mild to moderate Alzheimer’s disease firstly in 1995, developed by Sanochemia Pharmaceuticals. In the United States, galantamine hydrobromide was developed by Janssen Pharmaceuticals, a subsidiary of Johnson & Johnson, and was listed under the trade name Razadyne in 2001. So far, galantamine hydrobromide has been marketed in more than 20 countries and regions, such as the United States, Europe, and Japan.

용도

A selective acetylcholinesterase inhibitor. Useful for the treatment of Alzheimer's disease.

Indications

Its formulation includes capsule, tablet, and oral solution. It is used in the symptomatic treatment of mild to moderately severe dementia in Alzheimer’s disease.

정의

ChEBI: A natural product found in Crinum asiaticum var. sinicum.

일반 설명

Galantamine, 4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-6H-benzofuro-[3a,3,2,ef][2]-benzazepin-6-ol (Nivalin, Reminyl), is an alkaloid extractedfrom the tuberous plant Leucojum aestivum (L.) belongingto the Amaryllidaceae family and from the bulbs of thedaffodil, Narcissus pseudonarcissus. It is a reversiblecholinesterase inhibitor that appears to have no effect on butyrylcholinesterase.In addition, it acts at allosteric nicotinicsites, further enhancing its cholinergic activity. Galantamineundergoes slow and minor biotransformation with approximately5% to 6% undergoing demethylation. It is primarilyexcreted in the urine.

Clinical Use

Before the 1990s, galantamine was mainly used to treat poliomyelitis sequelae, muscle atrophy, postoperative intestinal muscle paralysis, urinary retention, and myasthenia gravis. In the 1990s, it was found that galantamine had improved memory impairment in mice, suggesting that it might be effective for central cholinergic disorders in Alzheimer’s disease
In a 3–6?months’ well-designed clinical trial, recipients of galantamine achieved significant improvements in cognitive symptoms compared to placebo recipients. Galantamine also improved activities of daily living in these patients and significantly reduced the requirement for caregiver assistance with activities of daily living. Clinical development of new indications of galanthamine is currently underway, such as smoking cessation and improving cognitive impairment in schizophrenia and mania.

갈란타민 준비 용품 및 원자재

원자재

준비 용품


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