BIOMAT Database Logo BIOMAT Database Logo

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). 1975

Y Asami, and M Otsuka, and M Akatsu, and S Kitagawa, and S Inaba, and H Yamamoto

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.

UI MeSH Term Description Entries
D008297 Male Males
D009043 Motor Activity Body movements of a human or an animal as a behavioral phenomenon. Activities, Motor,Activity, Motor,Motor Activities
D009125 Muscle Relaxants, Central A heterogeneous group of drugs used to produce muscle relaxation, excepting the neuromuscular blocking agents. They have their primary clinical and therapeutic uses in the treatment of muscle spasm and immobility associated with strains, sprains, and injuries of the back and, to a lesser degree, injuries to the neck. They have been used also for the treatment of a variety of clinical conditions that have in common only the presence of skeletal muscle hyperactivity, for example, the muscle spasms that can occur in MULTIPLE SCLEROSIS. (From Smith and Reynard, Textbook of Pharmacology, 1991, p358) Centrally Acting Muscle Relaxants,Central Muscle Relaxants,Relaxants, Central Muscle
D012018 Reflex An involuntary movement or exercise of function in a part, excited in response to a stimulus applied to the periphery and transmitted to the brain or spinal cord.
D002415 Cats The domestic cat, Felis catus, of the carnivore family FELIDAE, comprising over 30 different breeds. The domestic cat is descended primarily from the wild cat of Africa and extreme southwestern Asia. Though probably present in towns in Palestine as long ago as 7000 years, actual domestication occurred in Egypt about 4000 years ago. (From Walker's Mammals of the World, 6th ed, p801) Felis catus,Felis domesticus,Domestic Cats,Felis domestica,Felis sylvestris catus,Cat,Cat, Domestic,Cats, Domestic,Domestic Cat
D002749 Chlorprothixene A thioxanthine with effects similar to the phenothiazine antipsychotics. Chlorprotixen,Taractan
D003975 Diazepam A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity. 7-Chloro-1,3-dihydro-1-methyl-5-phenyl-2H-1,4-benzodiazepin-2-one,Apaurin,Diazemuls,Faustan,Relanium,Seduxen,Sibazon,Stesolid,Valium
D004357 Drug Synergism The action of a drug in promoting or enhancing the effectiveness of another drug. Drug Potentiation,Drug Augmentation,Augmentation, Drug,Augmentations, Drug,Drug Augmentations,Drug Potentiations,Drug Synergisms,Potentiation, Drug,Potentiations, Drug,Synergism, Drug,Synergisms, Drug
D004569 Electroencephalography Recording of electric currents developed in the brain by means of electrodes applied to the scalp, to the surface of the brain, or placed within the substance of the brain. EEG,Electroencephalogram,Electroencephalograms
D004597 Electroshock Induction of a stress reaction in experimental subjects by means of an electrical shock; applies to either convulsive or non-convulsive states. Electroconvulsive Shock,Electroconvulsive Shocks,Electroshocks,Shock, Electroconvulsive,Shocks, Electroconvulsive

Related Publications

Y Asami, and M Otsuka, and M Akatsu, and S Kitagawa, and S Inaba, and H Yamamoto
[Antiulcerogenic action of 7-chloro-1-cyclopropylmethyl-1,3-dihydro-5-(2-fluorophenyl)-2H-1,4-benzodiazepin-2-one (KB-509), a new benzodiazepine derivative].
March 1981, Nihon yakurigaku zasshi. Folia pharmacologica Japonica,
Y Asami, and M Otsuka, and M Akatsu, and S Kitagawa, and S Inaba, and H Yamamoto
Urinary metabolites of 7-chloro-1-(2-diethylaminoethyl)-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one dihydrochloride.
July 1968, Journal of medicinal chemistry,
Y Asami, and M Otsuka, and M Akatsu, and S Kitagawa, and S Inaba, and H Yamamoto
Electrophysiological and behavioral effects of 1-methyl-5-(o-fluorophenyl)-7-chloro-1,3-dihydro-2H-1,4-benzodiazepin-2-one (ID-540) in cats and rabbits.
May 1975, Arzneimittel-Forschung,
Y Asami, and M Otsuka, and M Akatsu, and S Kitagawa, and S Inaba, and H Yamamoto
[Effects of l-methyl-5-(O-fluorophenyl)-7-chloro-1,3-dihydro-2H-1,4-benzodiazepin-2-One (ID-540) on operant behavior in rats].
November 1976, Nihon yakurigaku zasshi. Folia pharmacologica Japonica,
Y Asami, and M Otsuka, and M Akatsu, and S Kitagawa, and S Inaba, and H Yamamoto
Quinazolines and 1,4-benzodiazepines. XL. The synthesis of metabolites of 7-chloro-1-(2-diethylaminoethyl)-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one.
July 1968, Journal of medicinal chemistry,
Y Asami, and M Otsuka, and M Akatsu, and S Kitagawa, and S Inaba, and H Yamamoto
Pharmacology of 7-chloro-5-(o-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one (lorazepam; Wy 4036).
July 1971, Arzneimittel-Forschung,
Y Asami, and M Otsuka, and M Akatsu, and S Kitagawa, and S Inaba, and H Yamamoto
[Behavioral effects of 5-(o-chlorophenyl)-1-methyl-7-nitro-1,3-dihydro-2H-1,4-benzodiazepin-2-one (ID-690)].
March 1977, Nihon yakurigaku zasshi. Folia pharmacologica Japonica,
Y Asami, and M Otsuka, and M Akatsu, and S Kitagawa, and S Inaba, and H Yamamoto
Double-blind cross-over clinical comparison of two 2'-chloro benzodiazepines: 7-chloro-5-(2-chlorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one (chlordesmethyldiazepam) versus 7-chloro-5-(o-chlorophenyl)-1,3-dihydro-3-hydroxy-2H-1,4-benzodiazepin-2-one (lorazepam) in neurotic anxiety.
February 1977, Arzneimittel-Forschung,
Y Asami, and M Otsuka, and M Akatsu, and S Kitagawa, and S Inaba, and H Yamamoto
[Pharmacologic effects of 7-chloro-1,3-dihydro-3-hydroxy-5-phenyl-2H-1,4-benzodiazepin-2-one].
April 1965, Arzneimittel-Forschung,
Y Asami, and M Otsuka, and M Akatsu, and S Kitagawa, and S Inaba, and H Yamamoto
Dose-dependent pharmacokinetics of 7-chloro-1,3-dihydro-5-(2'-chlorophenyl)-2H-1,4-benzodiazepin-2-one in dogs.
December 1978, Journal of pharmaceutical sciences,
Copied contents to your clipboard!