Background: A family of 4-benzo[][1,3]oxazines were obtained from a group of -(2-alkynyl)aryl benzamides precursors via gold(I) catalysed chemoselective 6--dig C-O cyclization.
Method: The precursors and oxazines obtained were studied in breast cancer cell lines MCF-7, CAMA-1, HCC1954 and SKBR-3 with differential biological activity showing various degrees of inhibition with a notable effect for those that had an aryl substituted at C-2 of the molecules. 4-benzo[][1,3]oxazines showed an IC rating from 0.
Anxiety is a mental disorder characterized by excessive concern about possible future threats that, if prolonged, becomes a pathology that must be controlled through psychotherapy and medication. Currently, the pharmacological treatment for anxiety involves the use of antidepressants and benzodiazepines; however, these treatments often come with adverse effects. Thus, there is a need to seek natural compounds that can help alleviate anxiety and reduce these side effects.
View Article and Find Full Text PDFKainate receptors (KARs) are glutamate receptors that participate in the postsynaptic transmission of information and in the control of neuronal excitability, as well as presynaptically modulating the release of the neurotransmitters GABA and glutamate. These modulatory effects, general follow a biphasic pattern, with low KA concentrations provoking an increase in GABA and glutamate release, and higher concentrations mediating a decrease in the release of these neurotransmitters. In addition, KARs are involved in different forms of long- and short-term plasticity.
View Article and Find Full Text PDFMutations in the human HERC1 E3 ubiquitin ligase protein develop intellectual disability. The () mouse carries a mutation characterized by cerebellar ataxia due of adult cerebellar Purkinje cells death by extensive autophagy. Our previous studies demonstrated that both the neuromuscular junction and the peripheral nerve myelin sheaths are also affected in this mutant.
View Article and Find Full Text PDFDopamine D receptor (DR) stimulation, in a putative DR/μ opioid heteroreceptor (MOR) complex, counteracts the molecular, cellular and behavioural actions of morphine which are associated with morphine addiction, without any effect on its analgesic properties. In the present work, we have evaluated the role of DR in modulating the effects of a continuous treatment with morphine on the GABAergic system in the basal ganglia. It has been demonstrated that the co-administration of a DR agonist together with morphine leads to a restoration of GABA signaling by preventing drug-induced changes in GAD expression in the caudate putamen, globus palidus and substantia nigra.
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