JN0002
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:
分子量:
274.53
UNSPSC Code:
12352202
NACRES:
NA.77
MDL number:
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-
SMILES string
Cl/C(C1=CC=C(Cl)C=C1Cl)=C\N2N=CN=C2
InChI key
XGLHZTBDUXXHOM-WMZJFQQLSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
room temp
Biochem/physiol Actions
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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
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
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
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
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