摘要:

The clinically effective antidepressant imipramine, an iminodibenzyl structure, was examined in two experimental methods which had previously demonstrated high prediction ability in descerning and categorizing potential psychotherapeutic drugs. The chronic administration of imipramine produced a significant reduction in the scores of aberrant behavioral response evoked by the fixed-dose with Ditran seen as early as 1 week after treatment was initiated and continuing through the 8-week treatment duration. This chronic per oral treatment with impramine was also associated with a significant potentiation of mean arterial pressure responses to fixed-dose treatment with serotonin, noradrenaline, yohimbine and adrenaline, while significantly inhibiting the histamine-induced depressor response. The results of this study support the speculation that, in dogs, the clinically effective antidepressants antagonize or reverse the Ditran-induced response and produce an associated response of sympathetic nervous system arousal or sensitization.

ISSN:0031-7012    

DOI:10.1159/000136748

出版商:S. Karger AG    

年代:1978

数据来源: Karger

摘要:

Nine radiolabeled compounds were identified in human urine after administering a single oral dose of 3H-l-bunolol (3 mg) to 5 male volunteers. These compounds represented 54.7% of the dose and 71.4% of the isotope excreted in 3 days. Intact bunolol accounted for 14.7% of the dose and its conjugates totaled an additional 5.0%. The major drug metabolite (28.2% of dose) was dihydrobunolol, a reduction product known to have the same pharmacological activity and potency as bunolol. Dihydrobunolol conjugates amounted to 3.9% of the dose. Two minor acidic metabolites were produced by oxidative cleavage of the bunolol side chain, and another minor metabolite (hydroxydihydrobunolol) resulted from both reductive and oxidative biotransformation. Bunolol metabolism in man showed qualitative and quantitative differences from patterns observed in the rat and dog.

ISSN:0031-7012    

DOI:10.1159/000136749

出版商:S. Karger AG    

年代:1978

数据来源: Karger

摘要:

Principal glycoproteins, uronic acid and amino acids were determined in canine gastric secretion, obtained from isolated canine stomachs perfused extracorporeally with homologous blood. Gastric secretion was collected during intraarterial infusion of pentagastrin alone for 3 h, and of secretin + pentagastrin for the next 3 h. Secretin produced a significant increase in the output of D-galactose, D-glucosamine, L-fucose, D-glucose, total sugars, total sulfate and uronic acid. Secretin had no significant effect on the output of most of amino acids of gastric secretion.

ISSN:0031-7012    

DOI:10.1159/000136750

出版商:S. Karger AG    

年代:1978

数据来源: Karger

摘要:

A growth reduction of 30–40% was noted in barley plants grown in two phenothiazine tranquilizers. Similar reductions were noted in the number of mid-anaphase cells, indicating the reduced growth could have been the result of a reduced mitotic rate. Also observed were several types of chromosomal aberrations. Electron microscopy revealed less endoplasmic reticulum and cytoplasmic organelles in the treated cells than in untreated cells. Various sized discontinuities in the nuclear membrane was the most frequent abnormality observed in the electron micrographs. The abnormal nuclear membrane was possibly a result of enzyme degradatio

ISSN:0031-7012    

DOI:10.1159/000136751

出版商:S. Karger AG    

年代:1978

数据来源: Karger

摘要:

The effects of kinins on the central action of amphetamine were investigated. It was found that bradykinin or activation of the kinin-forming system under the influence of kallikrein decreases the psychostimulatory effects of amphetamine given in a small dose (0.5 mg/kg) and increases the action of larger doses of amphetamine (2 and 10 mg/kg). It was shown that these effects may depend upon the influence of kinins on the level of neuromediators in the CNS after injection of 0.5 and 2 mg/kg of amphetamine. In comparison with a group of animals receiving only amphetamine, bradykinin given together with amphetamine at a dose of 0.5 mg/kg decreased the level of norepinephrine and increased the serotonin level in the corpus striatum; it decreased the level of dopamine in the brain cortex. On the other hand, this peptide given together with amphetamine at a dose of 2 mg/kg increased the level of norepinephrine in the hippocampus, of dopamine in the corpus striatum and hippocampus, and also caused a fall in the level of serotonin in the midbrain, as compared with a group of animals given amphetamine only. Investigations with platelets as a model showed that bradykinin may have a bi-directional effect on the uptake of norepinephrine by the nerve endings, depending on the concentration of amphetamine.

ISSN:0031-7012    

DOI:10.1159/000136752

出版商:S. Karger AG    

年代:1978

数据来源: Karger

ISSN:0031-7012    

DOI:10.1159/000136972

出版商:S. Karger AG    

年代:1967

数据来源: Karger

摘要:

The possibility that REM sleep deprivation induces increased sensitivity of rats to the effects of apomorphine was investigated. Rats were deprived of REM sleep by placing them on 6.0 cm platforms for 3 days. Stress control groups consisting of rats placed on 14 cm platforms (control rats) and groups of nonmanipulated animals (normal rats) were used for comparison purposes. Several doses of apomorphine were administered to these 3 groups of animals, and aggressive behavior, stereotyped behavior, verticalization and body temperature were recorded. All measures indicated that REM-deprived rats were more responsive to apomorphine than the normal and control animals, with the exception of verticalization effect, in which both REM-deprived and control animals reacted similarly. These results suggest that REM deprivation induced supersensitivity in brain dopamine receptors. Other possible interpretations are also discussed.

ISSN:0031-7012    

DOI:10.1159/000136753

出版商:S. Karger AG    

年代:1978

数据来源: Karger

ISSN:0031-7012    

DOI:10.1159/000136973

出版商:S. Karger AG    

年代:1967

数据来源: Karger

摘要:

2-(2,6-Dichlorophenylimino)piperimidine·HNO3 (St-404), 2-(2,6-dichlorophenyl)-5,6-dihydroimidazo[2,1-b]thiazole fumarate (compound 44–549) and 1,2,3,5-tetrahydroimidazo-[2,1-b]quinazoline·HCl (TIQ) were studied with respect to their effects on blood pressure and heart rate in the anaesthetized, normotensive rat following intravenous administration and in the chloralose-anaesthetized cat by means of infusions via the left vertebral artery. St-404 and compound 44-549 possess central hypotensive and bradycardic activities and display modes of action similar to that of clonidine. Central α-adrenergic receptors are presumably involved. In the anaesthetized, normotensive rat St-404 is about 3,400 times less active than clonidine, whereas compound 44-549 is 5 times more effective in lowering arterial pressure. The hypotensive effect of TIQ is brought about by a mechanism of action which is different from that of clonidine. The α-sympatholytic properties of TIQ suggested previously by others are not confirmed by the experiments presented in this

ISSN:0031-7012    

DOI:10.1159/000136754

出版商:S. Karger AG    

年代:1978

数据来源: Karger

ISSN:0031-7012    

DOI:10.1159/000136974

出版商:S. Karger AG    

年代:1967

数据来源: Karger