Aromatase and 5-alpha reductase gene expression: modulation by pain and morphine treatment in male rats

<p>Abstract</p> <p>Background</p> <p>The steroid hormone testosterone has been found to be greatly reduced by opioids in different experimental and clinical conditions. The purpose of this study on male rats was to determine the effects of a single injection of morphine (5 mg/Kg) on persistent pain (formalin test) and the single or combined effects on p450-aromatase and 5-alpha reductase type 1 mRNA expression in the brain, liver and testis. Testosterone was determined in the plasma and in the brain, morphine was assayed in the plasma.</p> <p>Results</p> <p>In the morphine-treated rats, there were increases of 5-alpha reductase mRNA expression in the liver and aromatase mRNA expression in the brain and gonads. Morphine was detected in the blood of all morphine-treated rats even though there were no clear analgesic affects in the formalin-treated animals three hours after treatment. Testosterone was greatly reduced in the plasma and brain in morphine-treated subjects.</p> <p>Conclusions</p> <p>It appears that morphine administration can induce long-lasting genomic effects in different body areas which contribute to the strong central and peripheral testosterone levels. These changes were not always accompanied by behavioral modifications.</p

Synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl and sulfamoyl acetamides and ethyl acetates as potent COX-2 inhibitors

We report herein the synthesis, biological evaluation and docking analysis of a new series of methylsulfonyl, sulfamoyl acetamides and ethyl acetates that selectively inhibit cyclooxygenase-2 (COX-2) isoform. Among the newly synthesized compounds, some of them were endowed with a good activity against COX-2 and a good selectivity COX-2/COX-1 in vitro as well as a desirable analgesic activity in vivo, proving that replacement of the ester moiety with an amide group gave access to more stable derivatives, characterized by a good COX-inhibition

L’area di Porta Maggiore a Roma: caratteri attuali di un nodo pluristratificato, problemi e strategie per la valorizzazione

L’attuale contesto di Porta Maggiore a Roma trae origine dalla confluenza delle viae Praenestina e Labicana e dal passaggio dei diversi acquedotti che hanno progressivamente garantito in epoca antica l’approvvigionamento idrico della città. Tra di essi spicca l’Aqua Claudia, per la quale fu realizzata una mostra monumentale a cavallo delle due strade. Sotto Aureliano le arcate dell’acquedotto vengono tamponate e convertite in mura e la mostra è trasformata in una porta urbana. Dal Medioevo al Rinascimento le fortificazioni vengono potenziate, mentre nuove strutture sorgono a ridosso della mostra celandola in gran parte. L’intervento di liberazione nell’800 da parte di Valadier e Folchi riporta alla luce le antichità romane e configura l’area come piazza. Nel corso del ‘900 il luogo è sottoposto a lavori che lo trasformano in un nodo viabilistico strategico, implicando scavi che portano alla luce testimonianze archeologiche rilevanti come una Basilica Ipogea. Oggi la piazza è percepita come mero luogo di passaggio e le vestigia archeologiche, ad esclusione della porta, sono difficilmente leggibili. Lo stesso PRG indica l’area come ambito di valorizzazione, esplicitando la necessità di un disegno efficace per aggiungere altre funzioni a quelle già presenti e per innescare nuovi rapporti tra archeologia e città contemporanea.The present landscape of Porta Maggiore in Rome has its origins in the crossroads between via Praenestina and via Labicana, and in the existence of the many aqueducts that provided water supply to the city starting from the II century BC. Among them there is the Aqua Claudia, whose monumental Mostra was built over the confluence of the two roads. Since 271 AD the acqueducts were incorporated in the Aurelian Walls, the arches were curtained and the Mostra itself turned into a Porta. From the Middle Ages to the Renaissance the defensive walls were reinforced while new structures were built around the Mostra, hiding it until the XIX century intervention of Valadier and Folchi. Their plan got rid of all the medieval add-ons and provided the very first design of the area as a piazza. In the XX century the area became a strategic location for local and national infrastructures, whose construction sites brought to light relevant remains such as the Basilica Ipogea. The piazza is now a heavily-trafficked junction in which the archeological rests, with the exception of the Porta, can not be fully appreciated. The general development plan itself specifies the need of a valorization programme for the area, in order to enhance the potentiality of the complex and to activate new connections between archeological and contemporary features

ChemInform Abstract: Synthesis of 6,7-Dihydro-8-(4-methyl-1-piperazinyl)(1)benzoxepino(4,5- c)quinoline as Potential 5-HT3 Receptor Ligand.

Two synthetic routes to the achievement of the title compound are described. The [1]benzoxepino[4,5-c]quinoline nucleus was prepared by nucleophilic aromatic fluoride displacement-cyclization and functionalized with N-methylpiperazine moiety. Alternatively the oxepino ring closure is shifted as the final step. An oxepine ring cleavage occurred in compounds (9) and (3); a mechanistical interpretation is proposed