Farmacologia, Toxicologia i Química Terapèutica: Recent submissions
Now showing items 221-240 of 675
Exposure of adolescent mice to 3,4-methylenedioxypyrovalerone increases the psychostimulant, rewarding and reinforcing effects of cocaine in adulthood
BACKGROUND AND PURPOSE 3,4-Methylenedioxypyrovalerone (MDPV) is a synthetic cathinone with powerful psychostimulant effects. It selectively inhibits the dopamine transporter (DAT) and is 10-50-fold more potent as a DAT ...
Phosphoenolpyruvate from Glycolysis and PEPCK Regulate Cancer Cell Fate by Altering Cytosolic Ca2+
Changes in phosphoenolpyruvate (PEP) concentrations secondary to variations in glucose availability can regulate calcium signaling in T cells as this metabolite potently inhibits the sarcoplasmic reticulum Ca2+/ATPase pump ...
Chiral Aminoalcohol-Derived delta-Lactams Provide Easy Access to Piperidines and Acyclic Five-Carbon Building Blocks Bearing a Tertiary and a Quaternary Stereocenter.
A procedure for the synthesis of enantiopure piperidines and acyclic building blocks (5-aminopentanols, O-protected 5-hydroxypentanenitriles) containing a tertiary and a quaternary stereocenter has been developed. Starting ...
Iron-Catalyzed Radical Intermolecular Addition of Unbiased Alkenes to Aldehydes
The intermolecular reductive radical coupling of aldehydes with nonactivated alkenes, employing metal hydride atom transfer (MHAT) catalysis with a combination of FeII and FeIII salts, is described. This constitutes the ...
Novel synthesis of arylethynyl heterocyles
A new and easy synthesis of 2-arylethynyl-indole and 2-arylethynyl-pyrrole is described. N-deprotection and subsequent base-catalyzed elimination of N-tosylheteroaryl benzyl ketones are the key steps of the process.
Approach to cis-Phlegmarine Alkaloids via Stereodivergent Reduction: Total Synthesis of (+)-Serratezomine E and Putative Structure of (−)-Huperzine N
A unified strategy for the synthesis of the cisphlegmarine group of alkaloids is presented, leading to the first synthesis of serratezomine E (1) as well as the putative structure of huperzine N (2). A contrasteric ...
Peroxisomal Proliferator-Activated Receptor β/ δ Deficiency Induces Cognitive Alterations
Peroxisome proliferator-activated receptor β/δ (PPARβ/δ), the most PPAR abundant isotype in the central nervous system, is involved in microglial homeostasis and metabolism, whose disturbances have been demonstrated to ...
Multicomponent-based synthesis and biological evaluation of tricyclic heterofused quinolines with multi-trypanosomatid activity
Human African trypanosomiasis (HAT), Chagas disease and leishmaniasis, which are caused by the trypanosomatids Trypanosoma brucei, T. cruzi and Leishmania species, are among the most deadly neglected tropical diseases. The ...
GDF15 mediates the metabolic effects of PPARβ/δ by activating AMPK
Peroxisome proliferator-activated receptor β/ (PPARβ/) activates AMP-activated protein kinase (AMPK) and plays a crucial role in glucose and lipid metabolism. Here, we examined whether the beneficial effects of PPARβ/δ ...
The Ethyl Acetate Extract of Leaves of Ugni molinae Turcz. Improves Neuropathological Hallmarks of Alzheimer's Disease in Female APPswe/PS1dE9 Mice Fed with a High Fat Diet
The most common type of dementia is Alzheimer's disease (AD), a progressive neurodegenerative disease characterized by impairment in cognitive performance in aged individuals. Currently, there is no effective pharmacological ...
PGC-1α induces mitochondrial and myokine transcriptional programs and lipid droplet and glycogen accumulation in cultured human skeletal muscle cells
The transcriptional coactivator peroxisome proliferator-activated receptor-gamma coactivator 1 alpha (PGC-1α) is a chief activator of mitochondrial and metabolic programs and protects against atrophy in skeletal muscle ...
Guia de medicaments d’Atenció Primària que requereixen una vigilància especial per la seva dispensació en pacients amb funció renal disminuïda.
Projecte: AVCRI 279 Requeriments tècnics: L’entorn és l’EXCEL de Microsoft. L'accés al codi no estarà disponible fins la fi de la data d'embargament. Si esteu interessats a accedir-hi, contacteu amb idea(at)fbg.ub.edu
Discovery and In Vivo Proof of Concept of a Highly Potent Dual Inhibitor of Soluble Epoxide Hydrolase and Acetylcholinesterase for the Treatment of Alzheimer's Disease
With innumerable clinical failures of target-specific drug candidates for multifactorial diseases, such as Alzheimer's disease (AD), which remains inefficiently treated, the advent of multitarget drug discovery has brought ...
Protein tyrosine phosphatase 1B (PTP1B) as a potential therapeutic target for neurological disorders
Protein tyrosine phosphatase 1B (PTP1B) is a typical member of the PTP family, considered a direct negative regulator of several receptor and receptor-associated tyrosine kinases. This widely localized enzyme has been ...
Lipid Nanoparticles for the Posterior Eye Segment
This review highlights the application of lipid nanoparticles (Solid Lipid Nanoparticles, Nanostructured Lipid Carriers, or Lipid Drug Conjugates) as effective drug carriers for pathologies affecting the posterior ocular ...
Orthogonal protecting groups in the synthesis of tryptophanyl-hexahydropyrroloindoles
The synthesis of various polycyclic systems containing a C3a-Ni bond between a hexahydropyrrolo[2,3-b]indole and an indole tryptophan is described here. A series of experiments were performed to determine the best combination ...
Microarray Analysis Revealed Inflammatory Transcriptomic Changes after LSL60101 Treatment in 5XFAD Mice Model
I2-IR have been found dysregulated in patients with neurodegenerative diseases, such as Alzheimer's disease (AD), in which the importance of neuroinflammation in the establishment and maintenance of cognitive decline is ...
Textile dyes induce toxicity on zebrafish early life stages
Textile manufacturing is one of the most polluting industrial sectors because of the release of potentially toxic compounds, such as synthetic dyes, into the environment. Depending on the class of the dyes, their loss in ...
Cognitive Decline and BPSD Are Concomitant with Autophagic and Synaptic Deficits Associated with G9a Alterations in Aged SAMP8 Mice
Behavioural and psychological symptoms of dementia (BPSD) are presented in 95% of Alzheimer's Disease (AD) patients and are also associated with neurotrophin deficits. The molecular mechanisms leading to age-related diseases ...
