Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
Results
Showing 1 to 14 of 14 for “"Sigma Receptors"”.
-
Design, synthesis, and biological evaluation of sigma receptors (σRS) ligands as potential pharmacotherapy for cancer and drug addiction
Sigma receptors are a well-defined unique class of receptors and are highly expressed in the central nervous system and also widely distributed in peripheral organs and tissues. There are two subtypes of sigma receptors: sigma-1 and sigma-2. These receptors are thought to be associated with …
-
Expression of sigma receptors in human cancer cell lines and effects of novel sigma-2 ligands on their proliferation
Sigma receptors originally thought to be an opioid receptor is now categorized as a distinct class of receptor. There are two main subtypes, the sigma-1 receptor and an uncharacterised binding site, named the sigma-2 binding site. The presence of the sigma-2 binding site shows high correlation with …
-
Semi-synthesis, synthesis and preclinical evaluation of sigma receptors ligands for the treatment of neuropathic pain [Semi-sintesi, sintesi e valutazione preclinica dei ligandi dei recettori sigma per il trattamento del dolore neuropatico]
… ha volta la propria attenzione sui recettori sigma (SR) come nuovi bersagli terapeutici, con l'obiettivo primario di sviluppare piccole molecole selettive per ciascun sottotipo di SR: sigma-1 (S1R) e sigma-2 (S2R). Sono state esplorate varie strutture, tra cui quella morfanica, piperazinica, …
-
Design, Synthesis, Biological Evaluation and Metabolic Stability Studies of Sigma Receptor Ligands
Sigma receptors represent a unique family of proteins that includes two subtypes: sigma-1 and sigma-2. Sigma-1 receptors have been implicated in the behavioral and motivational effects of psychostimulants as well as in the pathophysiology of depression and Alzheimer's disease. Sigma-2 receptors are …
-
Pharmacokinetic Evaluation of a Novel Compound, Sn79, a Putative Sigma-2 Receptor Antagonist, By Intravenous and Oral Administration in Rats
… and addiction. The affinity of cocaine to sigma receptors (sigma-1 and sigma-2) rendered the hypothesis that blocking sigma receptors could be a possible mechanism to attenuate cocaine-induced toxicity and addiction. In this view, SN79, a synthetic compound with selectivity to both sigma-1 …
-
Metabolic Stability And Pharmacokinetics In Lead Optimization Of Potential Anti-Psychostimulant Pharmacotherapies
… to treat cocaine and methamphetamine abuse. Sigma receptors have recently been identified as potential targets for the development of novel therapeutics. The affinity of cocaine and methamphetamine to sigma receptors represents that targeting these receptors using selective antagonists will …
-
Synthesis and structure-activity relationship of a series of sigma receptor ligands
Sigma receptors are involved in several biological processes, and sigma ligands might be promising as cancer treatment agents, cocaine abuse medicines, and valuable psychiatric drugs. In an attempt to elucidate effectual structure-activity relationships, a series of N-phenylpropyl- …
-
Scaffold Perception, ComPharmacophore Model Development, And Quantitative Structure-Affinity Relationships Of Sigma Site Ligands
Sigma receptors are endogenous proteins with potential utility in treating psychological disorders, ischemia, the psychological and convulsive effects of drugs of abuse, and as an imaging agent for cancerous tissues, among others. Drug design efforts targeting these receptors have been hindered by …
-
Molecular modeling of sigma 1 and sigma 2 receptor ligands: pharmacophore development and comparison using discotech and bioactivity prediction comparison of ab initio and density functional comfa studies for spiro and other receptor ligands
… by researchers in medicine. Information about sigma receptors in particular can be gained by studying the ligands associated with each type, sigma 1 or sigma 2. Sigma 1 receptor ligands consist of drug candidates that often have psychiatric and neurological applications; sigma 2 receptor …
-
Modulation of heme oxygenase-1 activity by novel synthetic compounds for pharmacological applications
… molecules endowed with antitumor activity. Since sigma receptors (sigmaRs) ligands showed potential antiproliferative effects in human cancers, the coadministration of sigmaR ligands and HO-1 inhibitors was evaluated in cancer cell lines that overexpress both proteins. Based on the promising …
-
Ligandi ibridi Sigma-HDAC come potenziale trattamento terapeutico per il melanoma uveale: design, sintesi e valutazione biologica
L’obiettivo principale di questa tesi di dottorato è stato quello di identificare nuove molecole di sintesi con efficacia terapeutica nei confronti del melanoma uveale, un tumore intraoculare tanto raro quanto aggressivo. Il lavoro è stato condotto presso il Dipartimento di Scienze del Farmaco e …
-
Progettazione e sintesi di nuovi ligandi sigma-1 bifunzionali con attività antiossidante
… stato suggerito il coinvolgimento del recettore sigma-1 nei meccanismi che mediano la neuroprotezione. Questa proteina è localizzata a livello della Mitochondrial Associated Membranes (MAM), dove modula il flusso di ioni Ca2+ dal reticolo endoplasmatico (ER) ai mitocondri, agendo da chaperone …
-
PROGETTAZIONE E SINTESI DI LIGANDI IBRIDI SIGMA-NO LIGHT-ACTIVATED A POTENZIALE ATTIVITA ANTIPROLIFERATIVA. NIH 10495 E DERIVATI: MODULAZIONE DELL ATTIVITA OPPIOIDE, SIGMA-1 ED HDAC NEL DOLORE NEUROPATICO.
… la progettazione e sintesi di ligandi ibridi NO/sigma attivati dalla luce a potenziale attività antitumorale, sfruttando l'overespressione dei recettori sigma in molte linee cellulari tumorali umane. Dato il crescente interesse per i ligandi sigma come potenziali agenti chemioterapici e sulla …