Publications by authors named "L Pirona"
Conformational changes as well as molecular determinants related to the activation and inactivation of olfactory receptors are still poorly understood due to the intrinsic difficulties in the structural determination of this GPCR family. Here, we perform, for the first time, the inactivation of human olfactory receptor OR51E2, highlighting the possible role of calcium in this receptor state transition. Using molecular dynamics simulations, we show that a divalent ion in the ion binding site, coordinated by two acidic residues at positions 2.
View Article and Find Full Text PDFProcto-Glyvenol© accelerates the natural healing process of wounds: a pre-clinical study.
Eur Rev Med Pharmacol Sci
September 2023
Objective: Hemorrhoids are a common anorectal disease that causes pain, itching, and burning. The prevalence of hemorrhoids is estimated to be as high as 36% in the general population, with approximately 50% of individuals experiencing symptomatic hemorrhoids at least once in their life. Middle age, obesity, and pregnancy are risk factors.
View Article and Find Full Text PDFArticle Synopsis
- - A series of modified 1,3-dioxolane compounds were created and evaluated for their ability to bind to serotonin (5-HTR) and alpha adrenergic receptors, with the most promising candidates chosen for further testing.
- - One standout compound, named 12, demonstrated strong activity as a full agonist at 5-HTR and showed favorable pharmacokinetics by effectively reaching the brain after oral administration.
- - In vivo studies of compound 12 revealed significant anxiolytic and antidepressant effects, along with a reduction in pain responses in a formalin test, suggesting its potential for treating anxiety, depression, and chronic pain conditions.
Negative allosteric modulators (NAMs) of the metabotropic glutamate receptor 5 (mGlu) hold great promise for the treatment of a variety of central nervous system disorders. We have recently reported that prop-2-ynylidenecycloalkylamine derivatives are potent and selective NAMs of the mGlu receptor. In this work, we explored the amide, carbamate, sulfonamide, and urea derivatives of prop-2-ynylidenecycloalkylamine compounds with the aim of improving solubility and metabolic stability.
View Article and Find Full Text PDFAim: Targeting 5-HT receptor (5-HTR) as a strategy for CNS disorders and pain control.
Methodology: A series of 1,3-dioxolane-based 2-heteroaryl-phenoxyethylamines was synthesized by a convergent approach and evaluated at α-adrenoceptors and 5-HTR by binding and functional experiments. Absorption, distribution, metabolism, excretion and toxicity prediction studies were performed to explore the drug-likeness of the compounds.