ResumenSe realizó gammagrafía de receptores de la somatostatina usando 111In-pentetreotide en un paciente con sospecha de un tumor neuroendocrino de páncreas. La gammagrafía con 111In-pentetreotide demostró una captación discreta del radiotrazador en la cabeza del páncreas y captación fo...
Despite the existence of biological markers of aggressiveness, the clinical course of gastro-entero-pancreatic (GEP) neuroendocrine neoplasms (NEN) remains difficult to predict. Discrepancies between imaging data generated with 111In-pentetreotide scintigraphy and 18F-FDG-PET could reflect the d...
A 34-year old woman with past history of anxiety, depression, and hypothyroidism resulting from prior total thyroidectomy for multinodular goiter presented with complaints of palpitations, sweating, and tachycardia. Clinical examination revealed a painless right lateral neck mass. USG/CT of the ...
The Claisen–Schmidt reaction between 1,1′-diacetylferrocene and ferrocenecarboxaldehyde under microwave irradiation has been investigated in different conditions. The selective synthesis of 1,5-dioxo-3-ferrocenyl[5]ferrocenophane has been achieved and a simple protocol for its purification was...
New [5]ferrocenophane based diphosphine ligands, having planar and central chirality, were prepared. The stereogenic center was generated by the enantioselective CBS-reduction of [5]ferrocenophan-1-one. The straightforward transformation of hydroxyl group to dimethylamino group afforded amine 7,...
This work reports the synthesis and the binding tests on the 5-HT3 and 5-HT4 receptors of new thienopyrimidopiperazine and piperazinylacylaminodimethylthiophene derivatives, in order to identify potent and selective ligands for each receptor. The compound with higher affinity and selectivity for...
This work reports the synthesis and the binding tests on the 5-HT3 and 5-HT4 receptors of new thienopyrimidopiperazine and piperazinylacylaminodimethylthiophene derivatives, in order to identify potent and selective ligands for each receptor. The 3-amino-2-(4-benzyl-1-piperazinyl)-5,6-dimethyl-t...
A high-throughput method to obtain several pyrimido[4,5-e][1,4]diazepines is described by a two-step acylation/cyclization sequence from key intermediates 6-amino-5-(amino)methylpyrimidines, which were prepared from the precursor 6-aminopyrimidin-5-carbaldehydes. The acylation is accomplished wi...
An improved microwave-induced synthesis of five ethidium derivatives (Ethidium derivatives, 2a–d) is presented. As the derivatives 2a–d have been proposed previously to be telomerase inhibitors, the binding interactions of these ethidium derivatives with G-quadruplex DNA were evaluated by mean...
Lipids regularly exhibit complicated thermotropic and lyotropic phase behavior. In this study, the utility of 13C solid‐state nuclear magnetic resonance spectroscopy (SSNMR) in characterizing the phase properties of pharmaceutical lipids was investigated. Variable temperature 13C SSNMR spectra ...
The effects of a series of fatty acids on the percutaneous absorption of propranolol (PL) through rabbit skin and the mechanism by which fatty acids facilitate the skin penetration of PL were examined in vitro and in vivo using a gel base. Lauric and myristic acids, at the fatty acid:PL molar ra...
Thermal analysis of propranolol/oleic acid mixtures prepared by solvent evaporation enabled construction of the binary system phase diagram. This allowed both physical and chemical interactions to be identified, including complex formation at the equimolar composition. An incongruent melting com...
Two studies involving six healthy volunteers were carried out to assess the importance of biphasic rapid and sustained release of oleic acid in enhancing the bioavailability of propranolol using the HALOTM drug delivery system. The results of the first study showed that mean Cmax and AUC values ...
Transdermal permeation of propranolol through human skin in the presence of fatty acid (lauric, capric) penetration enhancers has been investigated. Thermal analysis showed that binary mixtures of propranolol with either fatty acid were not simple mechanical mixtures of the two components. Propr...
The bioavailability of propranolol from a matrix-in-cylinder system for sustained drug delivery, consisting of a hot-melt extruded ethylcellulose pipe surrounding a drug-containing HPMC-Gelucire® 44/14 core, was determined. An oral dose of 80 mg propranolol hydrochloride was administered to heal...
Controllable selective synthesis strategy of polymerizable N-acyl and O-acylpropranolol vinyl derivatives was developed by enzyme-catalyzed acylation of propranolol using divinyl dicarboxylates with different carbon chain length as acyl donor. The influence of parameters including enzyme, solven...
Free fatty acids have been reported to induce cell death (lipotoxicity), but the effects depend on the carbon chain length and number of double bonds. Medium-chain saturated fatty acids (MC-SFAs), such as laurate, have less lipotoxicity than long-chain saturated fatty acids (LC-SFAs), such as pa...
The rate of treatment failure to antileishmanial chemotherapy in Latin America is up to 64%. Parasite drug resistance contributes to an unknown proportion of treatment failures. Identification of clinically relevant molecular mechanisms responsible for parasite drug resistance is critical to the...
SummaryLeishmania is a single-cell eukaryotic parasite of the Trypanosomatidae family, whose members cause an array of tropical diseases. The often fatal outcome of infections, lack of effective vaccines, limited selection of therapeutic drugs, and emerging resistant strains, underline the need ...
Mia40/CHCHD4 and Erv1/ALR are essential for oxidative protein folding in the mitochondrial intermembrane space of yeast and mammals. In contrast, many protists, including important apicomplexan and kinetoplastid parasites, lack Mia40. Furthermore, the Erv homolog of the model parasite Leishmania...
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