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Merck
CN

SML2447

Sigma-Aldrich

TPA023

≥98% (HPLC)

别名:

7-(1,1-Dimethylethyl)-6-[(1-ethyl-1H-1,2,4-triazol-5-yl)methoxy]-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine, TPA 023

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About This Item

经验公式(希尔记法):
C20H22FN7O
分子量:
395.43
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

−20°C

SMILES字符串

CC(C)(C)C1=CC2=NN=C(C3=CC=CC=C3F)N2N=C1OCC4=NC=NN4CC

InChI

1S/C20H22FN7O/c1-5-27-17(22-12-23-27)11-29-19-14(20(2,3)4)10-16-24-25-18(28(16)26-19)13-8-6-7-9-15(13)21/h6-10,12H,5,11H2,1-4H3

InChI key

QKIWQBLNTSQOLY-UHFFFAOYSA-N

生化/生理作用

Highly potent alpha2/alph3 GABA-A receptor partial agonist for benzodiazepine binding site with anxiolytic activity but lacking sedative activity
TPA023 is a highly potent, functionally selective agonist for α2-, α3-, and α5GABAA receptors that shows zero efficacy at a1GABAA subtypes. TPA023 exhibits anxiolytic and anticonvulsant effects in both animals and humans but lacks sedative effects and abuse potential.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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John R Atack et al.
The Journal of pharmacology and experimental therapeutics, 332(1), 17-25 (2009-09-26)
The GABA(A) receptor alpha2/alpha3 subtype-selective compound 7-(1,1-dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine (TPA023; also known as MK-0777) is a triazolopyridazine that has similar, subnanomolar affinity for the benzodiazepine binding site of alpha1-, alpha2-, alpha3-, and alpha5-containing GABA(A) receptors and has partial agonist efficacy at the
Nina M Shinday et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 38(6), 1006-1014 (2013-01-11)
Benzodiazepines are prescribed widely but their utility is limited by unwanted side effects, including abuse potential. The mechanisms underlying the abuse-related effects of benzodiazepines are not well understood, although α1 subunit-containing GABAA receptors have been proposed to have a critical
Angela N Duke et al.
The Journal of pharmacology and experimental therapeutics, 366(1), 145-157 (2018-05-04)
In nonhuman primates we tested a new set of behavioral categories for observable sedative effects using pediatric anesthesiology classifications as a basis. Using quantitative behavioral observation techniques in rhesus monkeys, we examined the effects of alprazolam and diazepam (nonselective benzodiazepines)

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