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PubMed · 3509340

Antihypertensive ergoline derivatives.

S Mantegani·A Temperilli·G Traquandi·P Salvati·E Di Salle·E Lamberti·A Bonsignori
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Abstract

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.

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AnimalsAntihypertensive AgentsBlood PressureErgolinesIsoxazolesMaleMiceProlactinPyrazolesPyrimidinesRatsRats, Inbred SHRRats, Inbred StrainsStructure-Activity RelationshipJournal Article

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S Mantegani, A Temperilli, G Traquandi, P Salvati, E Di Salle, E Lamberti, A Bonsignori. 1987. Antihypertensive ergoline derivatives.. https://pubmed.ncbi.nlm.nih.gov/3509340/

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