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Showing 1 to 20 of 20 for “"Sigma 2"”.
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PICTURE PRE-PROCESSING INTERFACE FOR THE SIGMA-2 COMPUTER
… of the conversion modifications and the Sigma -2 interface. Finally, the Sigma-2 programs are described and some results obtained with a modified FIDAC are shown.
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Development of pharmacophore and comfa study of rigid and flexible sigma 2 receptor ligands
… a pharmacophore and CoMFA model was derived for sigma 2 (62) receptors by using Sybyl 7.2 Software Package. The CoMFA studies used 22 bioactive molecules as a training set and 4 molecules as a test set for the o2 receptor ligands. The geometries and electrostatic charges of all molecules were …
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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 …
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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 …
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Pharmacophore derivation using discotech and comparison of semi-emperical, AB initio and density functional CoMFA studies for sigma 1 and sigma 2 receptor-ligands
… of pharmacophore and CoMFA models for sigma receptor ligands. CoMFA studies were performed for 48 bioactive sigma 1 receptorligands using [H^3 ](+) pentazocine as the radioligand, for 30 PCP derivatives for sigma 1 receptor-ligands using [^3H](+)SK-F 10047 as the radioligand and for 24 …
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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 …
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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 …
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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 …
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Progettazione e sintesi di ligandi sigma selettivi
ABSTRACT Ligandi selettivi per recettori sigma-1 e sigma-2, possono essere farmaci potenzialmente utili per il trattamento di diverse condizioni patologiche, quali disturbi psichiatrici, abuso di cocaina, memoria e disturbi di apprendimento, discinesia e reazioni distoniche indotte da farmaci …
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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 …
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Statistical analysis for discretely observed Lévy processes
… X_t given by the Lévy triplet (mu(theta),sigma^2(theta),nu_theta(dx)), where mu(theta) denotes the drift, sigma^2(theta) the diffusion part, nu_theta(dx) the Lévy measure, and theta is some unknown parameter. Our aim is to establish efficiency results for the estimation of theta, when the …
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Polytopes, generating functions, and new statistics related to descents and inversions in permutations
… the alternating descent set of a permutation [sigma] = [sigma] 1 [sigma] 2 an defined as the set of indices i such that either i is odd and ai > ui+l, or i is even and au < au+l. We show that this statistic is equidistributed with the 3-descent set statistic on permutations [sigma] = [sigma] 1 …
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Design, Synthesis, & Biological Evaluation of Novel Het-Aromatic/Aromatic Analogs for the Treatment of HIV, Cancer, & Cognitive Dysfunctions
… Emerging data suggest that inhibition of sigma-2 receptors has the potential to deliver disease-modifying AD drugs. Using pharmacophore analysis and analog-based drug design, two novel series of piperazine derivatives were synthesized as sigma-2 receptor antagonists.</p>
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Development of pharmacophore and CoMFA studies for sigma2 receptor ligands
… of a pharmacophore and CoMIFA model for sigma 2 ([sigma]_2) receptor ligands. CoMFA studies were performed for 32 bioactive [sigma]_2 receptor ligands using the radioligand [H 3] (+) DTG in the presence of pentazocine. The pharmacophore was derived using Distance Comparisons (DISCOtech) …
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Genomic and non genomic effects of elevated concentration of anabolic steroids in human neuronal cells
… effects is independent of activation of AR and sigma-2 receptor. An increased of caspase-3 activity was observed in cells treated with Nandrolone 10-6M for 48h. Collectively, these data support the existence of two cellular mechanisms that might explain the neurological syndromes observed in …
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Unkonventionelles Verhalten von Dianionen und vibronische Wechselwirkung in metastabilen Anionen
… In dieser Arbeit wird die neue Methode CAP/Sigma^(2) vorgestellt, die aufgrund ihrer Effizienz und einfachen Implementierbarkeit das Potential bietet, eine Standardmethode für die Lösung dieses Problems zu werden. Nicht nur größere Systeme bis zu Trichlorbenzol konnten damit untersucht …
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From Forest Floors to Pharmacology: Elucidating Millipede Defensive Alkaloids for Drug Discovery
… that a subset of the alkaloids potently binds to sigma-1 receptor (ischnocybine A: Ki 14 nM), while others bind to sigma-2 (homo-hydrogosodesmine hydrate: Ki 260 nM). Furthermore, ecology studies revealed that the alkaloid production is conserved over large geographical regions, accumulated as the …
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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, …
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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 …
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Label-free carbon nanotube sensors for glycan and protein detection
… polyclonal human IgG (KD [mu] = 19 [mu]M, [sigma]2 = 1000 [mu]M2 ). murine IgG (KD = 4.3 [mu]M, 2= 3 [mu]M 2), and human IgG from CHO cells (KD [mu] = 2.5 nM, [sigma]F2 = 0.01 RM2). Second, we show that an array of nanosensors can uniquely monitor weakly-affined analyte interactions via the …