Biography:

In the past Enzo Brambilla has collaborated on articles with Sergio Mantegani. One of their most recent publications is Original paperSynthesis and nidation inhibitory activity of a new class of ergoline derivativesSynthèse et activité inhibitrice sur la nidation d'une nouvelle classe de dérivés de l'ergoline. Which was published in journal European Journal of Medicinal Chemistry.

More information about Enzo Brambilla research including statistics on their citations can be found on their Copernicus Academic profile page.

Enzo Brambilla's Articles: (4)

Original paperSynthesis and nidation inhibitory activity of a new class of ergoline derivativesSynthèse et activité inhibitrice sur la nidation d'une nouvelle classe de dérivés de l'ergoline

AbstractThe synthesis and the nidation inhibitory activity (indirect evidence of prolactin activity) of a new class of ergolinyl-acylureas is described. Some structure—activity relationship considerations are also reported. N-[3-(Dimethyl-amino)propyl]-N-[(ethylamino)carbonyl]-6-(2-propenyl)ergoline-8β-carboxamide (laboratory code FCE 21336; international non-proprietary name cabergoline) was the most interesting compound of the series and is now under extensive clinical evaluation in treatment of hyperprolactinemic disorders.

5(10→9)Abeo-ergoline derivatives: Synthesis, 5-HT1A-receptor affinity and selectivity

AbstractThe synthesis and the structure-affinity relationship (S.A.F.I.R.) study for the 5-HT1A receptor sites of a novel series of 5(10→9)abeo-ergoline derivatives are presented. Most derivatives showed moderate to high affinity and selectivity for 5-HT1A receptor sites. The structure-affinity relationship pointed out the role of the substituent at position 8, and the outstanding importance of the reduction of the indole 2,3-double bond for achieving the highest 5-HT1A affinity and selectivity within the compounds presented.

D1 Agonist and/or D2 antagonist dopamine receptor properties of a series of ergoline derivatives: a structure–activity study

AbstractA series of (3,5-dioxopiperazin-1-yl)ergoline derivatives has been synthesised and evaluated in vitro and in vivo for their dopaminergic D1 and D2 components. The structural contributions to the pharmacological profile of the ergoline skeleton, its substituents on positions 1, 2, 6, 9, and the 3,5-dioxopiperazin-1-yl portion of the molecule were examined. Structure–activity relationships within this series suggested that substitution on the ergoline skeleton in position 1 or 2 and on the 3,5-dioxopiperazin-4-nitrogen generated compounds with a spectrum of dopamine agonistic/antagonistic activity sensitive to both the nature and position of substituents.

Serotonergic ergoline derivatives

AbstractNovel classes of 13- and 14-tertbutyl-ergoline derivatives were prepared, and characterised in vitro for their affinity for adrenergic, dopaminergic and serotonergic binding sites. This study particularly examines the importance of the presence and the position of the tert-butyl group in conferring either significant 5-HT1A or 5-HT2 affinity and selectivity respectively.

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