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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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About This Item

经验公式（希尔记法）:
C10H6Cl3N3
CAS号:
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).
Sedative & anticonvulsant with beta2-/beta3- (β2-/β3-) selective GABAA receptor PAM and GABAC (GABAA-rho receptor) NAM activity.

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

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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U Thomet et al.
European journal of pharmacology, 408(2), R1-R2 (2000-11-18)
GABA(C) receptors are expressed in the whole brain, but predominantly in the retina. They can be identified by their unique pharmacology. The establishment of the entire pharmacology is, however, quite tedious. We show here that loreclezole dose dependently inhibits ionic
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
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
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
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
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