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Merck
CN

JN0002

Sigma-Aldrich

Loreclezole

≥98% (HPLC)

别名:

1-[(1Z)-2-Chloro-2-(2,4-dichlorophenyl)ethenyl]-1H-1,2,4-triazole, 1-[(Z)-2-Chloro-2-(2,4-dichlorophenyl)vinyl]-1,2,4-triazole, R 72063, R-72063, R72063

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关于此项目

经验公式（希尔记法）:
C10H6Cl3N3
化学文摘社编号:
117857-45-1
分子量:
274.53
MDL编号:
MFCD00865331
UNSPSC代码:
12352202
NACRES:
NA.77

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方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

room temp

SMILES字符串

Cl/C(C1=CC=C(Cl)C=C1Cl)=C\N2N=CN=C2

InChI

1S/C10H6Cl3N3/c11-7-1-2-8(9(12)3-7)10(13)4-16-6-14-5-15-16/h1-6H/b10-4-

InChI key

XGLHZTBDUXXHOM-WMZJFQQLSA-N

生化/生理作用

Loreclezole (R72063) is a sedative and anticonvulsant that exerts subtype-selective positive allosteric modulator (PAM) potency toward beta2 (β2)- or β3-containing GABAA gamma-aminobutyric acid (GABA) receptors (% potentiation by 1 μM Loreclezole of GABA EC20-stimulated current/human α1βγ2 = 100/α1β2γ2, 120/α1β3γ2, 13/α1β1γ2; α1β2γ2 EC50 = 1 μM) with >300-fold lower β1 affinity, while acting as a negative allosteric modulator (NAM) against the homomeric rho1 (ρ1) GABAA-rho receptor (rat GABAC IC50 = 0.5 μM against GABA EC10-induced current).
Sedative & anticonvulsant with beta2-/beta3- (β2-/β3-) selective GABAA receptor PAM and GABAC (GABAA-rho receptor) NAM activity.

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number
0000076779
0000076780
0000073464

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K A Wafford et al.
Neuron, 12(4), 775-782 (1994-04-01)
Cloning of cDNAs that code for GABAA receptor subunits has revealed multiple receptor populations constructed from different subunit combinations. On native rat and cloned human GABAA receptors, the anticonvulsant compound loreclezole strongly potentiated GABA-mediated chloride currents. Using different combinations of
James O Groves et al.
The European journal of neuroscience, 24(1), 167-174 (2006-08-03)
The majority of inhibitory neurotransmission in the brain is mediated by the gamma-aminobutyric acid (GABA) type A (GABA(A)) receptor. The anticonvulsant loreclezole largely acts by potentiating GABA(A) receptors containing beta2 and beta3 subunits. We used a genetically modified mouse containing
P B Wingrove et al.
Proceedings of the National Academy of Sciences of the United States of America, 91(10), 4569-4573 (1994-05-10)
Type A gamma-aminobutyric acid (GABAA) receptors of the mammalian nervous system are a family of ligand-gated ion channels probably formed from the coassembly of different subunits (alpha 1-6, beta 1-3, gamma 1-3, delta) in the arrangement alpha beta gamma or
R B Raffa et al.
Naunyn-Schmiedeberg's archives of pharmacology, 342(5), 613-615 (1990-11-01)
Rats were injected intraperitoneally with loreclezole (R 72063), diazepam, or scopolamine 60 min prior to acquisition of a passive avoidance task and tested 18 h later for retention of the learned (passive) behavior. The known impairment of performance produced by
D Ashton et al.
Epilepsy research, 11(1), 27-36 (1992-03-01)
In animal models of epilepsy the anticonvulsant profile of loreclezole resembles that of barbiturates and benzodiazepines. We examined whether the increase in seizure threshold to pentylenetetrazole infusion produced by 10 mg/kg of loreclezole, pentobarbital or diazepam could be reversed by
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