18 documents found, page 1 of 2
Evaluation of P-glycoprotein activity mediated by fiscalin derivatives at the r...
Moreira, Beatriz; Sousa, Pedro; Silva, Nuno; Milhazes, Nuno; Silva, Renata; Remião, Fernando; Sousa, Maria Emília; Rocha-Pereira, CarolinaBackground: P-glycoprotein (P-gp) is an active efflux pump that reduces xenobiotics’ accumulation inside cells, and which activity can be modulated by inhibitors, inducers and activators [1,2]. The first ones have been used to counteract the multidrug resistance (MDR) phenomena and the inducers and activators have been proposed as a therapeutic approach in intoxication scenarios. In fact, P-gp binds several unr...
Enantiomeric profiling of ketamine in street samples for recreational use
Varela, Inês; Milhazes, Nuno; Martins, Daniel; Gonçalves, Virgínia; Tiritan, Maria Elizabeth; Ribeiro, CláudiaBackground: While ketamine (KET) has gained increasing scientific attention for its novel therapeutic applications, there has also been a parallel global rise in its non-medical, recreational use. [1]. Due to its effects on the central nervous system—such as dissociation, perceptual alterations, and its well-known anesthetic properties—KET is frequently used recreationally for its psychoactive effects. [2]. As ...
Enantiomeric biodistribution and toxicity of 3-chloromethcathinone (3-CMC) in W...
Langa, Ivan; Rocha-Pereira, Carolina; Milhazes, Nuno; Dias da Silva, Diana; Domingues, Susana; Silva, Paula; Barbosa, Joana; Faria, JulianaBackground: There has been a surge in global attention to New Psychoactive Substances (NPS) [1]. Synthetic cathinones stand out as a widely consumed NPS class. Notably, 3-chloromethcathinone (3-CMC) accounted for over 34% of NPS seizures in 2021 [2], which underscores concerns regarding its consumption and health effects. Of note, 3-CMC is chiral and mostly sold as a racemate. As human metabolism and pharm...
Enantiomeric biodistribution and toxicity of 3-chloromethcathinone (3-CMC) in W...
Langa, Ivan; Rocha-Pereira, Carolina; Milhazes, Nuno; Silva, Diana Dias da; Domingues, Susana; Silva, Paula; Barbosa, Joana; Faria, JulianaThere has been a surge in global attention to New Psychoactive Substances (NPS) [1]. Synthetic cathinones stand out as a widely consumed NPS class. Notably, 3-chloromethcathinone (3-CMC) accounted for over 34% of NPS seizures in 2021 [2], which underscores concerns regarding its consumption and health effects. Of note, 3-CMC is chiral and mostly sold as a racemate. As human me-tabolism and pharmacological effec...
Long-Term Treatment with Low Doses of Methamphetamine Promotes Neuronal Differe...
Baptista, Sofia; Lourenço, Joana; Milhazes, Nuno; Borges, Fernanda; Silva, Ana Paula; Bacci, AlbertoMethamphetamine (METH) is a psychostimulant, affecting hippocampal function with disparate cognitive effects, which depends on the dose and time of administration, ranging from improvement to impairment of memory. Importantly, in the United States, METH is approved for the treatment of attention deficit hyperactivity disorder. Modifications of long-term plasticity of synapses originating from the entorhinal cor...
Methamphetamine decreases dentate gyrus stem cell self-renewal and shifts the d...
Baptista, Sofia; Lasgi, Charlène; Benstaali, Caroline; Milhazes, Nuno; Borges, Fernanda; Fontes-Ribeiro, Carlos; Agasse, Fabienne; Silva, Ana PaulaMethamphetamine (METH) is a highly addictive psychostimulant drug of abuse that negatively interferes with neurogenesis. In fact, we have previously shown that METH triggers stem/progenitor cell death and decreases neuronal differentiation in the dentate gyrus (DG). Still, little is known regarding its effect on DG stem cell properties. Herein, we investigate the impact of METH on mice DG stem/progenitor cell s...
Variable delay-to-signal: a fast paradigm for assessment of aspects of impulsiv...
Almeida, Hugo Leite; Melo, António; Pêgo, José M.; Bernardo, Sara; Milhazes, Nuno; Borges, Fernanda; Sousa, Nuno; Almeida, Armando; Cerqueira, JoãoTesting impulsive behavior in rodents is challenging and labor-intensive. We developed a new behavioral paradigm-the Variable Delay-to-Signal (VDS) test-that provides rapid and simultaneous assessment of response and decision impulsivity in rodents. Presentation of a light at variable delays signals the permission for action (nose poke) contingent with a reward. 2 blocks of 25 trials at 3 s delay flank a block ...
Lipophilic Caffeic and Ferulic Acid Derivatives Presenting Cytotoxicity against...
Serafim, Teresa L.; Carvalho, Filipa S.; Marques, Maria P. M.; Calheiros, Rita; Silva, Tiago; Garrido, Jorge; Milhazes, Nuno; Borges, FernandaIn the present work, lipophilic caffeic and ferulic acid derivatives were synthesized, and their cytotoxicity on cultured breast cancer cells was compared. A total of six compounds were initially evaluated: caffeic acid (CA), hexyl caffeate (HC), caffeoylhexylamide (HCA), ferulic acid (FA), hexyl ferulate (HF), and feruloylhexylamide (HFA). Cell proliferation, cell cycle progression, and apoptotic signaling wer...
Lipophilic Caffeic and Ferulic Acid Derivatives Presenting Cytotoxicity against...
Serafim, Teresa L.; Carvalho, Filipa S.; Marques, Maria P. M.; Calheiros, Rita; Silva, Tiago; Garrido, J.M.P.J.; Milhazes, Nuno; Borges, FernandaIn the present work, lipophilic caffeic and ferulic acid derivatives were synthesized, and their cytotoxicity on cultured breast cancer cells was compared. A total of six compounds were initially evaluated: caffeic acid (CA), hexyl caffeate (HC), caffeoylhexylamide (HCA), ferulic acid (FA), hexyl ferulate (HF), and feruloylhexylamide (HFA). Cell proliferation, cell cycle progression, and apoptotic signaling wer...
Electrochemical and spectroscopic characterisation of amphetamine-like drugs: A...
Milhazes, Nuno; Martins, Pedro; Uriarte, Eugenio; Garrido, Jorge; Calheiros, Rita; Marques, M. Paula M.; Borges, FernandaA complete physicochemical characterisation of MDMA and its synthetic precursors MDA, 3,4-methylenedioxybenzaldehyde (piperonal) and 3,4-methylenedioxy-[beta]-methyl-[beta]-nitrostyrene was carried out through voltammetric assays and Raman spectroscopy combined with theoretical (DFT) calculations. The former provided important analytical redox data, concluding that the oxidative mechanism of the N-demethylation...