Bretazenil

Bretazenil C화학적 특성, 용도, 생산

개요

Bretazenil is an imidazobenzodiazepine partial agonist and a potent anxiolytic. It is rapidly absorbed and has a half-life of 2.5 hours. Animal work has shown that, even after long-term administration of bretazenil, there are no changes in GABA receptor binding or function, and tolerance does not occur. Studies in humans have also suggested that bretazenil has a low abuse potential (Sellers et al. 1991). In terms of clinical effects, bretazenil has demonstrated anxiolytic efficacy in both generalized anxiety disorder and panic disorder (Katschnig et al. 1991), but no controlled study has compared bretazenil with a classic full agonist.

용도

Anti-anxiety agent.
Bretazenil potentiated GABA responses on α4β3γ2 cells.
Bretazenil is a partial benzodiazepine receptor agonist. Benzodiazepines, mainly diazepam, are commonly used as anticonvulsants in the treatment of organophosphate casualties. Bretazenil has been used to determine non-specific binding due to its affinity to bind to a variety of γ-aminobutyric acid type A (GABAA) receptor subtypes (α1-3;5). It has also been used as a GABAA receptor partial agonist in the subcutaneous Alzet minipumps to treat obese agouti related protein (AgRP) ablated and lean naive mice to study its effect on them.

생물학적 활성

Bretazenil is a positive allosteric modulator of GABAA receptors with anticonvulsant and anxiolytic activity. It potentiates GABA-gated chloride currents in rat cortical neurons and in HEK293 cells expressing α1β1γ2 subunit-containing GABAA receptors (EC50s = 60 and 10 nM, respectively). Bretazenil inhibits binding of the benzodiazepine diazepam to rat cerebral cortex homogenates (IC50 = 2.2 nM). It inhibits tonic convulsions induced by pentylenetetrazol (PTZ; Item No. 18682) and maximal electroshock (MES) in rats (ED50s = 0.07 and 0.48 mg/kg, respectively). Bretazenil (5-30 mg/kg) increases the number of open arm entries and percentage of time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity.

Pharmacology

Bretazenil exhibits an ticonflflict and anticonvulsant properties. Only mild sedation appears at doses needed to produce anticonvulsant or anxiolytic effects, and potentiation of ethanol-induced sedation is less pronounced than with diazepam.

Bretazenil 준비 용품 및 원자재

원자재

준비 용품

Bretazenil 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Shanghai Synchem Pharma Co., Ltd	+86-61984905-1 +86-18016477331	synchempharma@aliyun.com	China	95	58
Zhejiang J&C Biological Technology Co.,Limited	+1-2135480471 +1-2135480471	sales@sarms4muscle.com	China	10523	58
Henan Bao Enluo International TradeCo.，LTD	+86-17331933971 +86-17331933971	deasea125996@gmail.com	China	2503	58
Hebei Yanxi Chemical Co., Ltd.	+8617531190177	peter@yan-xi.com	China	6011	58
Dorne Chemical Technology co. LTD	+86-13583358881 +86-18560316533	Ethan@dornechem.com	China	299	58
Xiamen Wonderful Bio Technology Co., Ltd.	+8613043004613	Sara@xmwonderfulbio.com	China	305	58
Shandong Huisheng Import & Export Co., Ltd.	+86-13176845580 +86-13176845580	da@zhongda-biotech.com	China	248	58
Anhui Ruihan Technology Co., Ltd	+8617756083858	daisy@anhuiruihan.com	China	994	58
CONTIDE BIOTECH CO.,LTD	+852-53358525	xena@healthtide-api.com	China	619	58
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21689	55

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