Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H6Cl3N3 |
Molecular Weight | 274.534 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 1 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl\C(=C/N1C=NC=N1)C2=C(Cl)C=C(Cl)C=C2
InChI
InChIKey=XGLHZTBDUXXHOM-WMZJFQQLSA-N
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-
Loreclezole was found to be active in all animal models of seizures, whether a genetic model of reflex epilepsy was used or models where seizures were elicited by chemical or electrical stimulation. In addition, loreclezole was active against both TON and CLON seizures and increased the threshold for behavioral as well as EEG seizures. Loreclezole has a very rapid onset of action and a duration of the activity, which in certain tests last for more than 24 hr. Chronic administration for 5-7 days did not lead to tolerance to the anticonvulsant action of loreclezole. Loreclezole potentiates gamma-aminobutyric acid (GABA) type A receptor function, by interacting with a specific allosteric modulatory site on receptor beta-subunits. It also acts as a negative modulator at a novel regulatory site, enhancing GABAA receptor sensitization. Inhibits homomeric ρ1 GABAC receptors.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: P47870 Gene ID: 2561.0 Gene Symbol: GABRB2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/9076754 |
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C264
Created by
admin on Fri Dec 15 16:35:24 GMT 2023 , Edited by admin on Fri Dec 15 16:35:24 GMT 2023
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DTXSID6048252
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CHEMBL1397886
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100000082033
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3034012
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DD-38
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C066440
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SUB08586MIG
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C66036
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LORECLEZOLE
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6DJ32STZ5W
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117857-45-1
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6389
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ACTIVE MOIETY