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品質水準
アッセイ
≥96% (HPLC)
形状
solid
色
white
溶解性
DMSO: 24 mg/mL
H2O: insoluble
オーガナイザー
Roche
保管温度
2-8°C
SMILES記法
[H][C@@]12CCCN1C(=O)c3c(Br)cccc3-n4cnc(C(=O)OC(C)(C)C)c24
InChI
1S/C19H20BrN3O3/c1-19(2,3)26-18(25)15-16-13-8-5-9-22(13)17(24)14-11(20)6-4-7-12(14)23(16)10-21-15/h4,6-7,10,13H,5,8-9H2,1-3H3/t13-/m0/s1
InChI Key
LWUDDYHYYNNIQI-ZDUSSCGKSA-N
詳細
Bretazenil, a tetracyclic imidazocarboxylic ester, is an anxi-olytic/anticonvulsant agent. It possesses a half-life of 2.5 hours and is quickly absorbed.
アプリケーション
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.
生物化学的／生理学的作用
Bretazenil is capable of binding to γ-aminobutyric acid type A (GABAA) receptors that are sensitive and insensitive to diazepam. This compound possesses negligible sedative or muscle relaxant effects.
ブレタゼニルはベンゾジアゼピンの部分アゴニストです。
特徴および利点
This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by Roche. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
保管分類コード
11 - Combustible Solids
WGK
WGK 3
引火点(°F)
Not applicable
引火点(℃)
Not applicable
個人用保護具 (PPE)
Eyeshields, Gloves, type N95 (US)
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
Jan Code
B6434-VAR:
B6434-5MG:
B6434-BULK:
B6434-25MG:
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。
Elisabetta Cagetti et al.
Molecular pharmacology, 63(1), 53-64 (2002-12-19)
One of the pharmacological targets of ethanol is the GABAA receptor (GABAR), whose function and expression are altered after chronic administration of ethanol. The details of the changes differ between experimental models. In the chronic intermittent ethanol (CIE) model for
A L van Steveninck et al.
British journal of clinical pharmacology, 41(6), 565-573 (1996-06-01)
1. Interaction between alcohol and bretazenil (a benzodiazepine partial agonist in animals) was studied with diazepam as a comparator in a randomized, double-blind, placebo controlled six-way cross over experiment in 12 healthy volunteers, aged 19-26 years. 2. Bretazenil (0.5 mg)
M Nazar et al.
Journal of neural transmission (Vienna, Austria : 1996), 106(5-6), 369-381 (1999-08-12)
The effects of an intrahippocampal administering of a nonselective full (midazolam), a partial benzodiazepine (BDZ) receptor agonist (bretazenil), and a BDZ1 selective (zolpidem) receptor ligand were examined in the open field test (OFT) of neophobia and Vogel's test (VT) of
N Brown et al.
British journal of pharmacology, 136(7), 965-974 (2002-07-30)
1: The pharmacology of the stable cell line expressing human alpha(4)beta(3)delta GABA(A) receptor was investigated using whole-cell patch-clamp techniques. 2: alpha(4)beta(3)delta receptors exhibited increased sensitivity to GABA when compared to alpha(4)beta(3)gamma(2) receptors, with EC(50)'s of 0.50 (0.46, 0.53) microM and
M R Guscott et al.
Behavioural pharmacology, 11(6), 495-504 (2000-12-05)
In the rat, fear-potentiated startle (FPS) test animals are first trained to associate brief light presentations with a mild electric footshock and then tested for startle responses to acoustic stimuli, delivered either in darkness (i.e. baseline startle) or after the
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