Michela Buccioni

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The aim of the present paper was to investigate the role of the octamethylene spacer of methoctramine (1) on the biological profile. Thus, this spacer was incorporated into a dianiline or dipiperidine moiety to determine whether flexibility and the basicity of the inner nitrogen atoms are important determinants of potency with respect to muscarinic(More)
Starting from compound 1, a previously reported alpha(1D)-adrenoceptors antagonist, a new series of ligands acting at 5-HT(1A) serotonin receptor were identified through simple structure modifications. Among them (2,2-diphenyl-[1,3]oxathiolan-5-yl-methyl)-(3-phenyl-propyl)amine (19) exhibits outstanding activity (pK(i)=8.72, pD(2)=7.67, E(max)=85) and(More)
Ligands that selectively block P2X3 receptors localized on nociceptive sensory fibres may be useful for the treatment of chronic pain conditions including neuropathic pain, migraine, and inflammatory pain. With the aim at exploring the suitability of adenine moiety as a scaffold for the development of antagonists of this receptor, a series of(More)
A series of new 1,2,4-benzothiadiazine derivatives with an arylpiperazine mojety linked at position 3 of the heterocyclic ring were synthesized and assessed for their pharmacological profiles at alpha(1)-adrenoceptor subtypes (alpha(1A), alpha(1B) and alpha(1D)) by functional experiments and by in vitro binding studies at human cloned 5-HT(1A) receptor.(More)
Starting from compounds previously identified as alpha(1)-adrenoceptor antagonists that were also found to bind to the 5-HT(1A) receptor, in an attempt to separate the two activities, a new series of 5-HT(1A) receptor agonists was identified and shown to have high potency and/or high selectivity. Of these, compound 13, which combines high selectivity(More)
The anticancer activity of isofuranodiene, extracted from Smyrnium olusatrum, was evaluated in human breast adenocarcinomas MDA-MB 231 and BT 474, and Caucasian prostate adenocarcinoma PC 3 cell lines by MTS assay. MTS assay showed a dose-dependent growth inhibition in the tumor cell lines after isofuranodiene treatment. The best antiproliferative activity(More)
A2B receptor agonists are studied as possible therapeutic tools for a variety of pathological conditions. Unfortunately, medicinal chemistry efforts have led to the development of a limited number of potent agonists of this receptor, in most cases with a low or no selectivity versus the other adenosine receptor subtypes. Among the developed molecules, two(More)
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