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Merck

T101

Sigma-Aldrich

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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About This Item

经验公式(希尔记法):
C6H8N2O2 · HCl
CAS号:
分子量:
176.60
EC號碼:
MDL號碼:
分類程式碼代碼:
12352100
PubChem物質ID:
NACRES:
NA.22

化驗

≥98% (HPLC)

形狀

solid

儲存條件

desiccated

顏色

white

溶解度

ethanol: 0.91 mg/mL
H2O: 20 mg/mL

SMILES 字串

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 密鑰

ZDZDSZQYRBZPNN-UHFFFAOYSA-N

一般說明

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。

應用

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)


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Chemistry and pharmacology of the GABA agonists THIP (Gaboxadol) and isoguvacine.
Krogsgaard-Larsen, et al.
Drugs of the Future, 9, 597-618 (1984)
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
Zhi-Ao Chen et al.
Cancer biology & medicine, 9(2), 90-98 (2013-05-22)
To investigate the roles of the γ-aminobutyric acid (GABA) in the metastasis of hepatocellular carcinoma (HCC) and to explore the potential of a novel therapeutic approach for the treatment of HCC. The expression levels of GABA receptor subunit genes in
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)

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