Some Ph-ring-substituted phenacylthioimidazolines are very potent antagonists of reserpine-induced hypothermia in mice. The proportion of open chain to cyclic carbinolamine tautomer depends on the type of substituent and possibly affects the activity. [1][2][3][4][5][6] thiazoles obtained by cyclodehydration are also active.
Schizochytrium sp. is an algae-like microorganism utilized for commercial production of docosahexaenoic acid (DHA)-rich oil and dried microalgae for use as a source of DHA in foods, feeds, and nutritional supplements. Electron microscopic analysis of whole cells of Schizochytrium sp. employing sample preparation by high-pressure freeze substitution suggests the presence of secondary and tertiary semicrystalline structures of triacylglycerols within the oil bodies in Schizochytrium sp. A fine secondary structure consisting of alternating light- and dark-staining bands was observed inside the oil bodies. Dark bands were 29 +/- 1 A in width, and light bands were 22 +/- 1 A in width. The tertiary (three-dimensional) structure may be a multilayered ribbon-like structure which appears coiled and interlaced within the oil body. In freeze-fracture photomicrographs, Schizochytrium oil bodies exhibited fracture planes with terraces averaging 52 +/- 7 A in height which could correspond to the combined width of two halves of two light bands and one dark band observed in the high-pressure freeze substitution photomicrographs. The results suggest that triacylglycerols within Schizochytrium sp. oil bodies may be organized in a triple chain-length structure. High-pressure freeze substitution electron micrographs of two other highly unsaturated oil-producing species of microalgae, Thraustochytrium sp. and Isochrysis galbana, also revealed this fine structure, whereas microalgae containing a higher proportion of saturated oil did not. The results suggest that the staining pattern is not an artifact of preparation and that the triple chain-length conformation of triacylglycerols in Schizochytrium sp. oil bodies may be caused by the unique fatty acid composition of the triacylglycerols.
The subcutaneous implantation of a cotton pellet in the rat evokes a short-lasting phase of increased capillary permeability lasting some 20 rnin. after implantation followed by a more sustained phase which occurs after 25-3 hr. The early increase is antagonised by lysergic acid diethylamide, reserpine and 5-HT. The peak granuloma weight is reached at 2 days, and then falls rapidly. Antagonism of oedema and granulation tissue by hydrocortisone and reserpine can be demonstrated at 2 days after implantation.
Although the selective monoamine oxidase (MAO) B inhibitor, (-)deprenyl, has been shown to be free from the "cheese effect" in man after tyramine challenge, the reason for this is far from clear: it may well be independent of the selective inhibitory action of the drug, for during chronic administration there is some evidence to suggest that both A and B forms of the enzyme are equally inhibited. By-passing the putative MAO A gut barrier in the pig (chosen because it possesses MAO B alone in all other tissues) by intravenous tyramine administration into the deprenyl-pretreated animal failed to provoke a pressor response, despite substantial MAO inhibition. Conversely, clorgyline (MAO A inhibitor) pretreatment, which resulted in minimal MAO inhibition, produced a profound hypertensive response, resembling that observed with the non-MAO-inhibiting drug, isoniazid. The most parsimonious explanation for these findings may be that two separate but closely associated pharmacological effects are normally found with "orthodox" MAO inhibitors, enzyme inhibition proper and facilitation of noradrenaline release from its binding sites during tyramine challenge.
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