Biomedical subjects
Publications and source records attributed to A Temperilli.
New ergoline derivatives exhibiting antiulcer and antisecretory activities were synthesized and tested. Stereochemical modification of the ergoline skeleton was found to influence the selective activity of the compounds.
Novel ergolines were synthesized and screened in spontaneous hypertensive rats (SHR) with the aim of finding a new class of ergot related antihypertensives. Their prolactin inhibitory effect (measured as nidation inhibition in rats), acute toxicity (LD50) and interference with CNS function (Irwin test) were also evaluated as a measure of selectivity and safety. Modification of the C8 side-chain enhanced antihypertensive activity selectively, while the introduction of substituents in other positions of the ergoline skeleton generally yielded unfavourable results, either by decreasing selectivity or by increasing toxicity.
The synthesis and the antihypertensive activity in rats of a series of 6-methylergolin-8 beta-yl-propionic acid derivatives are reported. The prolactin lowering activity (nidation inhibition test) in rats and the acute toxicity in mice were also studied as a measure of the specificity and safety of the potential antihypertensive compounds. From the structure-activity considerations reported here it is clear how modifications at the C8 side chain can improve the selectivity of the antihypertensive effects, whilst introducing substituents in other positions of the ergoline skeleton afforded unfavourable results in this respect. Compound 5, namely 2(R,S)-cyano-3-(6-methylergolin-8 beta-yl)-propionamide, emerged as the most interesting antihypertensive derivative.
The alpha-adrenolytic activity of 1-methyl-10-methoxydihydrolysergol 2-(3,5-dimethyl)pyrrolcarboxylate (XV, formula II) is, both in vitro and parenterally, quite similar to that of dihydroergotamine. By oral route the new compound is more active, and longer lasting than dihydroergotamine.
The synthesis and the pharmacological activities of 24 analogues of the alpha-adrenergic blocking drug, nicergoline (I b), are reported. The majority of the new compounds were found to be less active than (I b): the structure-activity relationships are presented and discussed.
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Extracts of the skin of some amphibians from Australia and Papua New Guinea contained, in addition to the usual 5-hydroxyindolealkylamines and histamine: a. two new, hitherto unknown indolealkylamines, i.e. O-sulphate of bufotenidine and 2-(3-indolyl) ethyltrimethylammonium, a quaternary ammonium base of tryptamine. The rare O-sulphate of bufotenine was also present, the occurrence of which had previously been demonstrated only in the skin of some South American toads; b. a series of uncommon imidazolealkylamines, such as N'-acetylhistamine, N'-methylhistamine, N',N'-dimethylhistamine, spinaceamine and 6-methylspinaceamine. It appears evident that amphibian skin continues to be an exceptionally rich source of aromatic amines.