바녹세린디히드로클로라이드

바녹세린디히드로클로라이드
바녹세린디히드로클로라이드 구조식 이미지
카스 번호:
67469-78-7
한글명:
바녹세린디히드로클로라이드
동의어(한글):
바녹세린디히드로클로라이드
상품명:
Vanoxerine dihydrochloride
동의어(영문):
I-893;GBR 12909;Vanoxerine;Boxeprazine;GBR129092HCl;Vanoxerine 2HCl;vanoxerine-GBR-12909;I893 dihydrochloride;GBR 12909 DIHYDROCHLORIDE;GBR 12909 (hydrochloride)
CBNumber:
CB9398144
분자식:
C28H33ClF2N2O
포뮬러 무게:
487.03
MOL 파일:
67469-78-7.mol
MSDS 파일:
SDS

바녹세린디히드로클로라이드 속성

녹는점
221 °C
저장 조건
Sealed in dry,Room Temperature
용해도
DMSO: >5 mg/mL 매일 신선하게 준비된 용액
물리적 상태
고체
물리적 상태
단단한 모양
색상
하얀색
수용성
DMSO에서 50mM까지 용해됩니다. 따뜻해지면 물에 5mM까지 용해됩니다.
안정성
제공된 대로 구매일로부터 2년 동안 안정적입니다. DMSO 또는 증류수 용액은 -20°에서 최대 1개월 동안 보관할 수 있습니다.

안전

WGK 독일 3
HS 번호 2933.59.5300

바녹세린디히드로클로라이드 C화학적 특성, 용도, 생산

개요

Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a potent inhibitor that blocks dopamine uptake (IC50 = 1-51 nM). It is more than 100-fold less effective at blocking serotonin or noradrenaline uptake. GBR 12909 effectively inhibits dopamine uptake in vivo, leading to consequent stimulation of dopamine receptors. GBR 12909 also inhibits pyrilamine binding to the histamine H1 receptor (IC50 = 18 nM) but poorly inhibits ligand binding to dopamine, adrenergic, acetylcholine, serotonin, and γ-aminobutyric acid receptors. It also blocks ligand binding to sigma receptors in rat brain (IC50 = 48 nM).

용도

Vanoxerine dihydrochloride is a Dopamine reuptake inhibitor that is developed for treatment of Parkinson's disease and depression but has no effect on these diseases.

정의

ChEBI: Vanoxerine dihydrochloride is a hydrochloride salt that is obtained by reaction of vanoxerine with two equivalents of hydrogen chloride. Potent, competitive inhibitor of dopamine uptake (Ki = 1 nM for inhibition of striatal dopamine uptake). Has > 100-fold lower affinity for the noradrenalin and 5-HT uptake carriers. Also a potent sigma ligand (IC50 = 48 nM). Centrally active following systemic administration. It has a role as a dopamine uptake inhibitor. It contains a vanoxerine(2+).

일반 설명

Vanoxerine dihydrochloride is a potent inhibitor of dopamine active transporter (DAT, Ki = 1 nM, IC50 = 40 and 51 nM) with >100 fold selectivity over noradrenalin and 5-HT re-uptake transporter. Shown to produce behavioral profile in mice for bipolar mania disease model and ADHD disease models.

위험도

A poison.

생물학적 활성

Potent, competitive inhibitor of dopamine uptake (K i = 1 nM for inhibition of striatal dopamine uptake). Has > 100-fold lower affinity for the noradrenalin and 5-HT uptake carriers. Also a potent sigma ligand (IC 50 = 48 nM). Centrally active following systemic administration.

바녹세린디히드로클로라이드 준비 용품 및 원자재

원자재

준비 용품


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