所有图片(1)
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
经验公式（希尔记法）:
C10H6Cl3N3
推荐产品
检测方案
≥98% (HPLC)
形式
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).
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
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
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
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
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
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