Potentiative effects of sulfhydryl compounds on carrageenin-induced oedema in rats and relationship to their potencies as inhibitors of angiostin-coverting enzyme in vivo.

Carrageenin-induced oedema in rats was potentiated by oral administration of (4R)-3-[(2S)-3-mercapto-2-methylpropanoyl]-4-thiazolidinecarboxylic acid (SA291) and related sulfhydryl compounds, and the effect was closely correlated with their potencies as inhibitors of angiotensin-converting enzyme in vivo.     

Comparative effects of sulfhydryl inhibitors on melanosome movements within vertebrate melanophores

Résumé Dans les mélanophores des grenouilles et des lézards examinés in vitro, les inhibiteurs du groupe sulfhydryl (thiol) tels que le mérsalyle et les maléimides N-substitutés bloquent irrévocablement la dispersion des mélanosomes soumis à l'action de la MSH et provoquent même leur retrait. On étudie les conditions structurales de l'action inhibitrice d'un certain nombre de maléimides N-substitués, étroitement apparentés.     

In vivo effects of Sumithion on tissue respiration and enzyme activity in the fish,Etroplus maculatus

Summary LD₅₀ exposure of a teleost fish.Etroplus maculatus, to Sumithion depressed the rate of oxygen consumption, concomitantly with an inhibition in succinate dehydrogenase activity in the tissues, in the order gill>brain>liver>muscle. The effect of the same pesticide on the activity of acetylcholinesterase was quite interesting, with a maximal inhibitory effect on the brain followed by liver, muscle and gill, suggesting a tissue specificity, and a differential sensitivity of the enzyme towards the pesticide.I wish to express may gratitude to Dr K. Sasira Babu and Dr J. Hemalatha for their valuable discussions and encouragement.     

Triphasic vascular effects of thiol compounds and their oxidized forms on dog coronary arteries

The vascular effects of 2-mercaptoethanol, cysteamine, L-cysteine, glutathione (GSH), cystamine and oxidized GSH (GSSG) on the isometric tension of isolated dog coronary arterial strips were examined, and these effects were compared with the triphasic response induced by dithiothreitol (DTT); a rapid and weak contraction (phase A), an intervening slow relaxation (phase B) and a slowly-developing strong contraction (phase C) which we previously reported. The responses of the arteries induced by 2-mercaptoethanol, cysteamine and L-cysteine consisted of phases A, B and C. The order of contractile potency (ED₅₀ of phase C) was DTTL-cysteine>2-mercaptoethanolcysteamine, while the order of relaxant potency (ED₅₀ of phase B) was DTT>cysteamine2-mercaptoethanol. GSSG and cystamine mainly produced relaxation, which corresponded to phase B. The phase C contraction was specific to the reduced forms of thiols, except for GSH, which produced only relaxation. The participation of endothelial cells was not essential for the contracting or relaxing effects of the thiol compounds. The phase C contraction was depressed by W-7, a calmodulin antagonist, while phase A was not. Therefore calmodulin-dependent protein kinases may participate in phase C, not in phase A.     

Cardiotonic activities of four new compounds derived from digitoxigenin and uzarigenin,and their structure-activity relationship

Zusammenfassung Die kardiotonischen Wirkungen der vier neuen Cardenolid-Derivate auf das isolierte Froschherz wurden untersucht und die Beziehungen zwischen ihren chemischen Strukturen und Wirkungen diskutiert.     

42K spaces in submandibular gland of early postnatal rats: effects of carbachol and transport inhibitors

Summary Equivalent spaces of⁴²K were measured in fragments of the submandibular gland of 1-, 7-, 14- and 21-day-old and adult rats in the absence and presence of carbachol and the transport inhibitors ouabain and furosemide. The results indicate that the⁴²K space was increased by carbachol in an ouabain-sensitive manner at all ages studied and that part of the secretagogue-stimulated K uptake occurred by way of a furosemide-sensitive transport system in the latter part of the postnatal period and in the adult.     

42K spaces in submandibular gland of early postnatal rats: effects of carbachol and transport inhibitors

Equivalent spaces of 42K were measured in fragments of the submandibular gland of 1-, 7-, 14- and 21-day-old and adult rats in the absence and presence of carbachol and the transport inhibitors ouabain and furosemide. The results indicate that the 42K space was increased by carbachol in an ouabain-sensitive manner at all ages studied and that part of the secretagogue-stimulated K uptake occurred by way of a furosemide-sensitive transport system in the latter part of the postnatal period and in the adult.     

Circling behavior in mice and rats: possible relationship to isolation-induced aggression

Summary The relationship between circling behavior (rotation), isolation, and aggression was investigated in normal male mice and rats. Initially the animals were tested for spontaneous nocturnal rotation, then conspecific aggression and muricidal behavior was observed for mice and rats respectively. Subsequently, animals were paired on the basis of net nocturnal rotations and either group-housed or individually housed. Four weeks later all animals were retested for the same behaviors. Spontaneous nocturnal rotation increased significantly for the isolated mice but not for the group-housed animals. Moreover, 9 of the 10 isolates became aggressive and their net rotations were significantly and positively correlated with the number of biting attacks. None of the group-housed mice became aggressive. Rats, on other hand, showed a decrease in rotation and a relationship between rotation and muricidal behavior was not evident. The possible relationship between circling behavior, aggression, and territoriality is discussed.     

Circling behavior in mice and rats: possible relationship to isolation-induced aggression

The relationship between circling behavior (rotation), isolation, and aggression was investigated in normal male mice and rats. Initially the animals were tested for spontaneous nocturnal rotation, then conspecific aggression and muricidal behavior was observed for mice and rats respectively. Subsequently, animals were paired on the basis of net nocturnal rotations and either group-housed or individually housed. Four weeks later all animals were retested for the same behaviors. Spontaneous nocturnal rotation increased significantly for the isolated mice but not for the group-housed animals. Moreover, 9 of the 10 isolates became aggressive and their net rotations were significantly and positively correlated with the number of biting attacks. None of the group-housed mice became aggressive. Rats, on other hand, showed a decrease in rotation and a relationship between rotation and muricidal behavior was not evident. The possible relationship between circling behavior, aggression, and territoriality is discussed.     

Rate of uptake of75Se,as selenourea-75Se,in rats in vivo

Zusammenfassung Die Geschwindigkeit der Verteilung und Fixierung des Selenharnstoff-⁷⁵Se wurde in diversen Rattenorganen in vivo und bei Stoffwechselzeiten von 6 h bis zu 14 Tagen untersucht. Die Selenharnstoffmengen varierten zwischen 0,4 und 3,0 mg pro Tier.

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The authors wish to thank Dr. H.Hope(Kjemisk Institute, Universitet i Oslo, Norway), for supplying the first selenourea used in these experiments.     

The effect of hypoxia on hepatic cytochromes and heme turnover in rats in vivo

We evaluated the effect of hypoxia (7% v/v) on hepatic heme turnover in vivo and microsomal heme protein content in male Sprague-Dawley rats. Hepatic heme protein turnover, measured as 14CO-production during continuous infusion of 5-14C-aminolevulinic acid, a precursor of nonerythrogenic heme, was decreased 60% during hypoxia and returned to control levels promptly after reoxygenation. Hepatic cytochrome P-450 content was decreased in hypoxic and 24-h reoxygenated animals. We conclude that normobaric hypoxia decreases hepatic cytochrome P-450 which could contribute to decreased drug metabolism in hypoxia. This decrease is probably due to heme oxygenase-independent breakdown of hepatic heme.     

Translocation of hepatic cytosol androgen receptor to the nucleus in vivo in male rats

Summary Testosterone, which was injected s.c. into adult male rats castrated 15 h prior to the injection, decreased the number of androgen-specific binding sites in the cytosol at 30 min. Coincidentally, a substantial increase was observed in the nucleus. The decreased number of the sites in the cytosol was restored to the initial level at 60 min; on the contrary, a decrease was observed in the nucleus.     

The effect of hypoxia on hepatic cytochromes and heme turnover in rats in vivo

Summary We evaluated the effect of hypoxia (7% v/v) on hepatic heme turnover in vivo and microsomal heme protein content in male Sprague-Dawley rats. Hepatic heme protein turnover, measured as¹⁴CO-production during continuous infusion of 5-¹⁴C-aminolevulinic acid, a precursor of nonerythrogenic heme, was decreased 60% during hypoxia and returned to control levels promptly after reoxygenation. Hepatic cytochrome P-450 content was decreased in hypoxic and 24-h reoxygenated animals. We conclude that normobaric hypoxia decreases hepatic cytochrome P-450 which could contribute to decreased drug metabolism in hypoxia. This decrease is probably due to heme oxygenase-independent breakdown of hepatic heme.