The synthesis and pharmacology of a novel benzodiazepine derivative, 1-(beta-methylsulfonylethyl)-5-(o-fluorophenyl)-7-chloro-1,3-dihydro-2H-1,4-benzodiazepin-2-one (ID-622).
The pharmacological profiles of a new benzodiazepine derivative, 1-(beta-methylsulfonylethyl)-5-(o-fluorophenyl)-7-chloro-1,3-dihydro-2H-1,4-benzodiazepin-2-one (ID-622), were shown. In anti-convulsant test, ID-622 was more potent than diazepam and medazepam when tested with pentylenetetrazol or bemegride, but was less potent than diazepam tested with strychnine or MES in mice. Taming effects of ID-622 were more potent than diazepam in both electroshock- and isolation-induced fighting mice tests, but were less potent in both septal rats and O.B. rats tests. ID-622 had only a weak influence on the spontaneous locomotor activity, and did not cause the righting reflex loss. In EEG, ID-622 increased fast activity and depressed hippocampal I-waves and amygdala after-discharge in cats. Acute toxicity of ID-622 was very low.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D000927:Anticonvulsants / Q000494:pharmacology; D001534:Bemegride / Q000037:antagonists & inhibitors; D002415:Cats; D002749:Chlorprothixene / Q000494:pharmacology; D003975:Diazepam / Q000494:pharmacology; D004357:Drug Synergism; D004569:Electroencephalography; D004597:Electroshock; D005260:Female; D005464:Fluorobenzenes / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D006591:Hexobarbital / Q000494:pharmacology; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D009125:Muscle Relaxants, Central / Q000494:pharmacology; D051381:Rats; D012018:Reflex / Q000187:drug effects
D014151:Anti-Anxiety Agents; D000927:Anticonvulsants; D005464:Fluorobenzenes; D009125:Muscle Relaxants, Central; D001534:Bemegride; D002749:Chlorprothixene; D006591:Hexobarbital; D003975:Diazepam