T101
加波沙朵 盐酸盐
solid, ≥98% (HPLC)
别名:
4,5,6,7-四氢异噁唑[5,4-c]吡啶-3-醇 盐酸盐, THIP 盐酸盐
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关于此项目
经验公式（希尔记法）:
C6H8N2O2 · HCl
化学文摘社编号:
分子量:
176.60
NACRES:
NA.22
PubChem Substance ID:
UNSPSC Code:
12352100
EC Number:
285-687-7
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
InChI key
ZDZDSZQYRBZPNN-UHFFFAOYSA-N
InChI
1S/C6H8N2O2.ClH/c9-6-4-1-2-7-3-5(4)10-8-6;/h7H,1-3H2,(H,8,9);1H
SMILES string
Cl[H].Oc1noc2CNCCc12
assay
≥98% (HPLC)
form
solid
storage condition
desiccated
color
white
solubility
ethanol: 0.91 mg/mL, H2O: 20 mg/mL
Quality Level
Gene Information
General description
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。
Application
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。
Biochem/physiol Actions
GABAA 受体激动剂。
Disclaimer
光敏
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
P Krogsgaard-Larsen et al.
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
GABA(A) agonists and partial agonists: THIP (Gaboxadol) as a non-opioid analgesic and a novel type of hypnotic.
Krogsgaard-Larsen P, et al.
Biochemical Pharmacology, 68(8), 1573-1580 (2004)
Zhiwen Ye et al.
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 and Sleep: Molecular, Functional and Clinical Aspects (2010)
Vanessa M Hill et al.
PLoS biology, 16(7), e2005206-e2005206 (2018-07-13)
Although sleep appears to be broadly conserved in animals, the physiological functions of sleep remain unclear. In this study, we sought to identify a physiological defect common to a diverse group of short-sleeping Drosophila mutants, which might provide insight into
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