Dexmedetomidine hydrochloride

한글명:Dexmedetomidine hydrochloride

카스 번호145108-58-3

상품명:Dexmedetomidine hydrochloride

CBNumberCB3838381

분자식C13H17ClN2

포뮬러 무게236.74

MOL 파일145108-58-3.mol

화학적 성질

녹는점	156.5-157.5°
알파	+52.4° (c = 1 in water)
밀도	1.17 g/cm3
저장 조건	2-8°C
용해도	H2O: 용해성20mg/mL, 투명
물리적 상태	가루
색상	흰색에서 베이지색
optical activity	[α]/D +48 to +58°, c = 1 in H2O
Merck	14,2946
안정성	흡습성
InChI	InChI=1/C13H16N2.ClH/c1-9-5-4-6-12(10(9)2)11(3)13-7-14-8-15-13;/h4-8,11H,1-3H3,(H,14,15);1H/t11-;/s3
InChIKey	VPNGEIHDPSLNMU-MERQFXBCSA-N
SMILES	[C@@H](C1NC=NC=1)(C1C=CC=C(C)C=1C)C.Cl \|&1:0,r\|
CAS 데이터베이스	145108-58-3(CAS DataBase Reference)

위험 및 안전 성명

위험품 표기

위험 카페고리 넘버

22-36/37/38

안전지침서

26-36/37/39

WGK 독일

RTECS 번호

NI5156750

HS 번호

2933290000

NFPA 704:

	0
2		0

그림문자(GHS)

Dexmedetomidine hydrochloride 화학적 특성, 용도, 생산

개요
Dexmedetomidine was launched in the US as an i.v. infusion for sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care unit, This imidazole derivative is the (S)-enantiomer of medetomidine that can be obtained via fractional crystallization of the tartrate salt of the racemic mixture. Dexmedetomidine is a full agonist of α2 adrenoceptors with 1300-fold selectivity versus α1 compared to the less selective partial α2 agonist clonidine, a veterinary hypnotic. Dexmedetomidine is unique compared with currently available sedatives in that it provides sedation, analgesia and anxiolysis with the ability of patients to be easily awakened. Besides, it causes minimal respiratory depression unlike other available drugs such as benzodiazepines or opioids. Pharmacological studies in transgenic mice showed that the sedative, anesthetic and analgesic effects of dexmedetomidine are specifically due to the stimulation of the a_2A subtype receptor. Like other α2 adrenoceptor agonists, dexmedetomidine can provoke hypotension and bradycardia probably because of its non-selective action on peripheral a_2B subtype receptors in vascular smooth muscle. Dexmedetomidine is extensively metabolized into methyl and glucuronide conjugates which are mainly eliminated by renal excretion. It was found to be a CYP2D6 inhibitor but less potent than the clinically relevant standard quinidine.
물리적 성질
Dexmedetomidine hydrochloride is a white or almost white powder that is freely soluble in water and has a pKa of 7.1.
용도
Dexmedetomidine hydrochloride has been used to study its effects on primary neonatal rat cardiomyocytes under hypoxic/reoxygenation conditions. It has also been used to study the effects of dexmedetomidine pretreatment on lipopolysaccharide-induced acute lung injury in mice.
benefits
The chemical name of dexmedetomidine hydrochloride is (S) -4- [1- (2,3- 3,5-dimethylphenyl) ethyl] -1H- imidazole hydrochlorides. Dexmedetomidine hydrochloride has an anti-sympathetic town. The effect of quiet and analgesic, compared with U.S. support pyrimidine, with higher selectivity and a short half-life, can be clinically used for Intensive Care Therapy. Start intubation and calmness using a lung ventilator patient during treatment. Meanwhile, the medicine can also reduce narcotic consumption, improve hand incidence of hemodynamic stability, and reduce myocardial ischaemia in art.
생물학적 활성
Active isomer of Medetomide (4-[1-(2,3-Dimethylphenyl)ethyl]-1H-imidazolehydrochloride ), a potent, highly selective α 2 -adrenoceptor agonist (K i values are 1.08 and 1750 nM for α 2 - and α 1 -adrenoceptors respectively). Displays greater selectivity over α 1 -adrenoceptors than clonidine and UK 14,304 (1620-, 220- and 300-fold respectively). Active in vivo ; displays hypotensive, bradycardic, sedative, anxiolytic, hypothermic and analgesic effects.

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