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
M Lancel
Sleep, 22(1), 33-42 (1999-02-16)
This paper reviews the sleep effects of systemically administered agonistic modulators of GABAA receptors, including barbiturates, benzodiazepines, zolpidem, zopiclone and neuroactive steroids, and the selective GABAA agonists muscimol and THIP. To assess the involvement of GABAA receptors in the physiologic
GABA and Sleep: Molecular, Functional and Clinical Aspects (2010)
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