Cabergoline

Cabergoline 구조식 이미지
카스 번호:
81409-90-7
상품명:
Cabergoline
동의어(영문):
Dostinex;CG-101;cabergoline powder;Caber;C08187;Dostine;Cabaser;Sogilen;Galastop;FCE-21336
CBNumber:
CB0282495
분자식:
C26H37N5O2
포뮬러 무게:
451.6
MOL 파일:
81409-90-7.mol

Cabergoline 속성

녹는점
102-104°C
밀도
1.156±0.06 g/cm3(Predicted)
저장 조건
2-8°C
용해도
DMSO: ≥10mg/mL
산도 계수 (pKa)
13.05±0.46(Predicted)
물리적 상태
가루
색상
흰색에서 황백색까지
optical activity
[α]/D 61 to 68°, c = 0.5 in dichloromethane
안정성
흡습성
InChIKey
KORNTPPJEAJQIU-KJXAQDMKSA-N
SMILES
[C@]12([H])C[C@H](CN(CC=C)[C@]1([H])CC1=CNC3C=CC=C2C1=3)C(=O)N(CCCN(C)C)C(=O)NCC |&1:0,3,9,r|
CAS 데이터베이스
81409-90-7(CAS DataBase Reference)
안전
  • 위험 및 안전 성명
  • 위험 및 사전주의 사항 (GHS)
위험품 표기 Xi
위험 카페고리 넘버 36/37/38
안전지침서 26-36/37
WGK 독일 3
RTECS 번호 KE6167600
HS 번호 2939690000
독성 Sol in ethyl alcohol, chloroform, DMF; slightly sol in 0.1 N HCl; very slightly sol in n-hexane. Insol in water. LD50 orally in male mice: >400 mg/kg (Brambilla)
그림문자(GHS): GHS hazard pictograms
신호 어: Warning
유해·위험 문구:
암호 유해·위험 문구 위험 등급 범주 신호 어 그림 문자 P- 코드
H302 삼키면 유해함 급성 독성 물질 - 경구 구분 4 경고 GHS hazard pictograms P264, P270, P301+P312, P330, P501
H315 피부에 자극을 일으킴 피부부식성 또는 자극성물질 구분 2 경고 GHS hazard pictograms P264, P280, P302+P352, P321,P332+P313, P362
H319 눈에 심한 자극을 일으킴 심한 눈 손상 또는 자극성 물질 구분 2A 경고 GHS hazard pictograms P264, P280, P305+P351+P338,P337+P313P
H335 호흡 자극성을 일으킬 수 있음 특정 표적장기 독성 - 1회 노출;호흡기계 자극 구분 3 경고 GHS hazard pictograms
예방조치문구:
P261 분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.
P264 취급 후에는 손을 철저히 씻으시오.
P264 취급 후에는 손을 철저히 씻으시오.
P270 이 제품을 사용할 때에는 먹거나, 마시거나 흡연하지 마시오.
P301+P312 삼켜서 불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.
P302+P352 피부에 묻으면 다량의 물로 씻으시오.
P305+P351+P338 눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
NFPA 704
0
3 0

Cabergoline C화학적 특성, 용도, 생산

개요

Cabergoline is a potent, selective, and long-lasting dopamine D2 receptor agonist launched in 1993 in Belgium as a prolactin inhibitor. A single 1 mg dose of cabergoline effectively prevents puerperal lactation for up to 14 days, remarkably superior to other drugs that require a daily regimen. It has a low rate of rebound breast activity and good tolerability. Cabergoline is also in clinical trials for Parkinson's disease, breast cancer, and hyperprolactinaemia.

화학적 성질

White Crystalline Solid

용도

Cabergoline is an ergot derivative and a dopamine D2-receptor agonist (1,2,3). It inhibits the secretion of prolactin and growth hormone.

정의

ChEBI: An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substit ted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia.

일반 설명

Cabergoline, (6aR,9R,10aR)-7-allyl-N-(3-(dimethylamino)propyl)-N-(ethylcarbamoyl)-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline-9-carboxamide (Dostinex), is a white powder soluble inalcohol, chloroform, and N,N-dimethylformamide; slightlysoluble in acidic solutions and in n-hexane; and insoluble inwater. Following oral administration, peak plasma concentrationsare reached within 2 to 3 hours. Cabergoline ismoderately bound to plasma proteins in a concentrationindependentmanner. The absolute bioavailability of cabergolineis unknown. Cabergoline is extensively metabolizedby the liver, predominantly via hydrolysis of the acylureabond of the urea moiety. CYP450 metabolism appears to beminimal. The major metabolites identified thus far do not contribute to the therapeutic effect of cabergoline. Lessthan 4% is excreted unchanged in the urine. Fecal excretionrepresents the main route of cabergoline elimination. Thereare no reports of interactions of cabergoline with other antiparkinsonianagents. Clarithromycin may elevate theplasma concentration of cabergoline by the inhibition ofboth CYP3A4 and P-glycoprotein.Cabergoline is a potentD2 receptor agonist and is indicated for the treatment ofhyperprolactinemic disorders, either idiopathic or causedby pituitary adenomas.

생물학적 활성

Selective D 2 -like dopamine receptor agonist (K i values are 0.7, 1.5, 9.0 and 165 nM for D 2 , D 3 , D 4 and D 5 receptors respectively) that also displays high affinity for several serotonin receptor subtypes (K i = 1.2-20.0 nM for 5-HT 1A , 5-HT 1D , 5-HT 2A and 5-HT 2B ). Inhibits secretion of prolactin and growth hormone and reverses levodopa-induced dyskinesias in Parkinsonian monkeys.

Cabergoline 준비 용품 및 원자재

원자재

준비 용품


Cabergoline 공급 업체

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