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质量水平
方案
≥98% (HPLC)
表单
solid
储存条件
desiccated
颜色
white
溶解性
ethanol: 0.91 mg/mL
H2O: 20 mg/mL
SMILES字符串
Cl[H].Oc1noc2CNCCc12
InChI
1S/C6H8N2O2.ClH/c9-6-4-1-2-7-3-5(4)10-8-6;/h7H,1-3H2,(H,8,9);1H
InChI key
ZDZDSZQYRBZPNN-UHFFFAOYSA-N
基因信息
human ... GABRA1(2554) , GABRA2(2555) , GABRA3(2556) , GABRA4(2557) , GABRA5(2558) , GABRA6(2559) , GABRB1(2560) , GABRB2(2561) , GABRB3(2562)
一般描述
加波沙朵,也称为4,5,6,7-四氢异恶唑并(5,4-c)吡啶-3-醇(THIP),是一种GABA位点激动剂。它对突触外高亲和力GABAA受体的δ 亚基具有很强的亲和力。 加波沙朵最初被用于治疗精神分裂症、癫痫、原发性失眠症 和亨廷顿病。它很容易穿过血脑屏障,并迅速被人体吸收。
应用
盐酸加波沙朵已被用于细胞迁移和侵袭测定以评估肝癌细胞的迁移。
生化/生理作用
GABAA 受体激动剂。
注意
光敏
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
Eyeshields, Gloves, type N95 (US)
从最新的版本中选择一种:
分析证书(COA)
GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic.
Biochemical Pharmacology, 68(8), 1573-1580 (2004)
Journal of medicinal chemistry, 26(6), 895-900 (1983-06-01)
The thio analogues of the GABA (gamma-aminobutyric acid) agonist THIP (4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol), the GABA uptake inhibitor THPO (4,5,6,7-tetrahydroisoxazolo[4,5-c]pyridin-3-ol), and the glycine antagonist THAZ (5,6,7,8-tetrahydro-4H-isoxazolo[4,5-d]azepin-3-ol) have been synthesized and tested biologically on single neurons in the cat spinal cord and in vitro
Frontiers in neural circuits, 7, 203-203 (2014-01-07)
We have made use of the δ subunit-selective allosteric modulator DS2 (4-chloro-N-[2-(2-thienyl)imidazo[1,2-a]pyridine-3-yl benzamide) to assay the contribution of δ-GABAARs to tonic and phasic conductance changes in the cerebellum, thalamus and neocortex. In cerebellar granule cells, an enhancement of the tonic
GABA Site Agonist Gaboxadol Induces Addiction-Predicting Persistent Changes in Ventral Tegmental Area Dopamine Neurons But Is Not Rewarding in Mice or Baboons
The Journal of Neuroscience, 32(15), 5310-5320 (2012)
TEXTBOOK OF GERIATRIC MEDICINE INTERNATIONAL (2011)
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