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Merck
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文件

JN0002

Sigma-Aldrich

Loreclezole

≥98% (HPLC)

同義詞:

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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About This Item

經驗公式（希爾表示法）:
C10H6Cl3N3
CAS號碼:
117857-45-1
分子量：:
274.53
MDL號碼:
MFCD00865331
分類程式碼代碼:
12352202
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

room temp

SMILES 字串

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 密鑰

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).

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

分析證明 (COA)

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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
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
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
C L Zhang et al.
Naunyn-Schmiedeberg's archives of pharmacology, 346(5), 581-587 (1992-11-01)
Effects of loreclezole (R72063), a triazole derivative with anticonvulsant properties, were studied on field potentials in rat hippocampal slices and on different patterns of low Mg(2+)-induced epileptiform activity in combined entorhinal cortex-hippocampal slices. Lowering extracellular Mg2+ induced recurrent (10-60/min), short
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