Prostaglandins X. An improved route for synthesis of PGF2beta analogues.
Esterification with inversion is a highly stereospecific reaction by which one-step conversion of PGF2alpha to PGF2beta is obtained with very satisfactory yield.
Biomedical subjects
Publications and source records attributed to C Gandolfi.
Esterification with inversion is a highly stereospecific reaction by which one-step conversion of PGF2alpha to PGF2beta is obtained with very satisfactory yield.
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The biological activities of 8,12-diiso-PGE2 (ent-11,15-epi-PGE2), PGE2 and PGF2alpha have been compared in a series of pharmacological preparations intended to differentiate between F and E type of activity. Similar to PGF2alpha but unlike PGE2, 8,12-diiso-PGE2 increased the tone of isolated smooth muscle preparations of guinea pig trachea, guinea pig colonic circular layer, rabbit Fallopian tubes. The stimulation effect of 8,12-diiso-PGE2 and PGF2alpha on visceral smooth muscle was also shown in vivo: the two drugs were in all instances able to increase the miogenic activity and tone of rabbit uterus in situ, while these were depressed by PGE2. 8,12-diiso-PGE2 decreased pulmonary compliance and increased pulmonary vascular resistance in the anaesthetized cat; PGE2 always decreased pulmonary vascular resistance, while leaving pulmonary compliance unaltered. The possibility is suggested that 8,12-diiso-PGE2 acts on PGF receptor in different tissues.
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Monoiodinated angiotensin II at a specific activity in the order of 1 C/mg can be prepared with high yields by controlling the pH of iodination and can be purified on G-25 Sephadex. The fractions from the head to the centre of the single peak of radioactivity obtained by gel filtration of the iodination mixture contain pure monoiodinated angiotensin. The monoiodinated derivative shows an immunoreactivity very close to that of the native hormone; in contrast, the diiodinated derivative has a low immunoreactivity and its use as a tracer results in a loss of sensitivity in the radioimmunoassay of angiotensin II. It is suggested that the use of the monoiodinated derivative in pure form should be recommended whenever a small hormonal polypeptide labelled at high specific activity is to be prepared for radioimmunoassay purposes.
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