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Biomedical subjects

T Hara

Publications and source records attributed to T Hara.

At least 1,153 records · Page 64Linked to original sources
PubMed1978

Diazepines. 5. Synthesis and biological action of 6-phenyl-4H-pyrrolo[1,2-a][1,4]benzodiazepines.

A series of 6-phenyl-4H-pyrrolo[1,2-a][1,4]benzodiazepines (2) has been prepared with 2-phthalimidomethylfurans (12) and 1-phthalimidoalkane-2,5-diones (15) or 2,5-dimethoxy-2-phthalimidomethyltetrahydrofurans (16) as the key intermediates and subsequently evaluated for CNS activity. The structure-activity data generated indicate that, in general, introduction of the methyl and/or ethyl group(s) in the pyrrole ring and a chlorine atom at the ortho position of the 6-phenyl group increases the activity and that substitution of the above chlorine atom for a fluorine atom decreases the activity. 8-Chloro-6-(2-chlorophenyl)-1,3-dimethyl-4H-pyrrolo[,2-a][1,4]benzodiazepine (2p), the most potent among the compounds synthesized, was equipotent in taming and sedative activities to diazepam. The acute LD50 of 2p in mice was larger than 3000 mg/kg po.

Animals↗
PubMed1978

Results of esophagocardioplasty with gastric patch in the treatment of esophageal achalasia.

Since 1968 esophagocardioplasty with gastric patch was employed in 57 patients as a primary operation for achalasia of the esophagus and eight patients with previous operations for achalasia. Satisfactory results were obtained in follow-up studies up to eight years. The results indicate that this procedure is successful in dilating the lower part of the esophagus and esophagocardiac junction without interfering with their proper functions. This provides better passage through the junction with preservation of the mechanism which prevents reflux.

Adult↗
PubMed1978

[Effects of a new psychotropic agent, CS-430, on the central nervous system of experimental animals (author's transl)].

In rats and rabbits with chronically implanted electrodes CS-430(10-bromo-2, 3, 7, 11b-tetrahydro--11b-(2-fluorophenyl)-oxazolo(3, 2d) [1, 4]benzodiazepine-6(5H)-one) (3 mg/kg, .o.) decreased the slightly awake period and increased the slow-wave sleep period. The onset time of sleep was significantly shortened. In the rat pre-treated with p-chlorophenylalaine (500 mg/kg, p.o.), the awake period was remarkable increased and the slow wave sleep period was considerably decreased at 48 hours after the pre-treatment. In these rats CS-430 given in the same dose decreased significantly the awake peiod and the onset time of sleep and increased the slow wave sleep period. CS-430 raised the threshold of the arousal response with stimulation of the posterior hypothalamus, but not of the mesencephalic reticular formation. These effects of CS-430 were almost as potent as those of nitrazepam (NZP). CS-430 reduced duration of after-discharges following stimulation of the hippocampus, depressed the decerebrate rigidity and inhibited activity of lumbar gamma-motoneurons in anesthetized cats. CS-430 (10 mg/kg, p.o.) inhibited the evoked responses recorded from the proreus gyrus following stimulation of either the baso-magnocellularis of the amygdaloid nuclear or the ventral hippocampus, although such did not inhibit the responses between the olfactory bulb and the pyriform cortex, the thalamus and the sensory-motor cortex. Thus CS-430 has a sleep-inducing effect in animals of almost the same potency as is seen with NZP, and site(s) of the action in the limbic system appear to be specific.

Amygdala↗
PubMed1978

Pharmacological studies on CS-430, a new psychotropic agent.

10-Bromo-11b-(2-fluorophenyl)-2,3,7,11b-tetrahydrooxazolo[3,2-d][1,4]benzodiazepin-6(5H)-one (CS-430) is a new psychotropic drug and has the following properties. The compound showed sleep-inducing effect at both 0.2 and 5 mg/kg (p.o.) in cynomolgus monkeys or at 3 mg/kg (p.o.) in rats. CS-430 showed selective conflict attenuating in rats or anticonvulsant effects in mice. Furthermore, CS-430 blocked non-discriminated (Sidman) avoidance response without severe impairment of the motor function but not discriminated (shuttle-box) avoidance response in rats. CS-430 also blocked selectively electroshock-induced fighting behavior of mice but not isolation-induced fighting behavior of mice and muricidal behavior induced by ablation of the olfactory bulbs. In addition, CS-430 produced specific potentiation of chlorprothixene-induced sleep and particular potentiation of thiopental sleep in mice. These effects of CS-430 were similar to those of nitrazepam, but differed from those of phenobarbital. The effect of CS-430 on the motor function was roughly 1/2 as potent as that of nitrazepam in the various tests.

Animals↗
PubMed1978

Inhibition of lymphocyte cytotoxicity in chronic active hepatitis.

Inhibitory factors were investigated, using 51Cr-labelled Chang cells as targets, based on the inhibition of lymphocyte-mediated cytotoxicity (LMC) in patients with chronic active hepatitis (CAH). A significant reduction of LMC was noted (P less than 0.001) when autologous sera of patients with CAH was added. The addition of HBsAg-positive and -negative homologous sera from CAH, which were as capable of inhibiting LMC as autologous sera, decreased LMC significantly (P less than 0.001). The LMC fell significantly (P less than 0.001) in the presence of sera of patients with rheumatoid arthritis. A significantly higher inhibition (P less than 0.001) by rheumatoid factor (RF) positive autologous sera of patients with CAH was observed when compared to that of RF-negative sera. Such autologous sera inhibiting LMC contained increased IgG levels (P less than 0.01) when compared to those that failed to inhibit LMC. A significant reduction of LMC was also induced with the addition of anti-HBs (P less than 0.05), HBsAg--anti-HBs (P less than 0.001) and IgG--anti-IgG (P less than 0.01) complexes, or aggregated IgG (P less than 0.001). The LMC was reduced significantly (P less than 0.001) after adding a purified liver-specific membrane lipoprotein (LSP) from human livers. There was some evidence for the inhibition of LMC being effected by these additives as a result of their acting on an effector cell level. These findings suggest that humoral factors including immune complexes, aggregated IgG and LSP play an important role for lymphocyte cytotoxicity in the pathogenesis of CAH.

Antigen-Antibody Complex↗
PubMed1977

Isolation and some properties of nontoxigenic derivatives of a strain of Clostridium tetani.

Nontoxigenic derivatives of a toxigenic strain of Clostridium tetani were isolated gy treatment with acridine orange, N-methyl-N'-nitro-soguanidine, rifampicin or ultraviolet light. The frequency of appearance fo non-toxigenic derivatives on these treatments was 0.8 to 3.2 per cent. The nontoxigenic derivatives peoduced all the same extracellular antigenic and protein components as the toxigenic parent strain, except the toxin and materials cross-reacting with the toxin. The nontoxigenic strains, like the toxigenic parent strain, were lyzed by trratment with mitomycin C. Bacteriophage was detected in the lysates of all the nontoxigenic derivatives produced with mitomycin C, and this bacteriophage was morphologically indistinguishable from that obtained from the toxigenic parent strain. The genetic factor controlling tetanus toxin production is discussed.

Antigens, Bacterial↗