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Comparing adenosine A receptor modulation of cannabinoid CB receptor-mediated inhibition of GABA and glutamate release in rodent striatal nerve terminals.
Eur J Neurosci
January 2025
CNC-Center for Neuroscience and Cell Biology, University of Coimbra, Coimbra, Portugal.
In corticostriatal nerve terminals, glutamate release is stimulated by adenosine via A receptors (ARs) and simultaneously inhibited by endocannabinoids via CB receptors (CBRs). We previously identified presynaptic AR-CBR heterotetrameric complexes in corticostriatal nerve terminals. We now explored the possible functional interaction between ARs and CBRs in purified striatal GABAergic nerve terminals (synaptosomes) and compared these findings with those on the release of glutamate.
View Article and Find Full Text PDFTheoretical-Cheminformatic Study of Four Indolylphytoquinones, Prospective Anticancer Candidates.
Pharmaceuticals (Basel)
November 2024
Departamento de Mantenimiento Industrial y Nanotecnología, Universidad Tecnológica de Ciudad Juárez, Maestría en Ingeniería Industrial Sustentable, Av. Universidad Tecnológica No. 3051, Col. Lote Bravo II, Ciudad Juárez 32695, Chihuahua, Mexico.
Breast cancer is a disease with a high mortality rate worldwide; consequently, urgent achievements are required to design new greener drugs, leaving natural products and their derivatives as good options. A constant antineoplastic effect has been observed when the phytoproduct contains an indole fragment. Therefore, the objective of this work was to carry out a thoughtful computational study to perform an appropriate evaluation of four novel molecules of the class of the 3-indolylquinones as phytodrug candidates for antineoplastic activity: thymoquinone (TQ), 2,6-dimethoxy-1,4-benzoquinone (DMQ), 2,3-dimethoxy-5-methyl-1,4-benzoquinone (DMMQ), and 2,5-dihydroxy-1,4-benzoquinone (DHQ).
View Article and Find Full Text PDFHit Selection of Dipeptidyl Peptidase-4 Inhibitors Bearing Thieno[2,3-d]Pyrimidine Scaffold.
Chem Biodivers
December 2024
Faculty of Medicine, Department of Chemistry, University of Niš, Niš, Serbia.
The thieno[2,3-d]pyrimidine fragment is in the structure of many drug-like candidate derivatives with a wide range of biological activities. However, very few dipeptidyl peptidase-4 (DPP-4) inhibitors with this building block are currently known. Here, the selection of a novel DPP-4 inhibitor based on the thienopyrimidine scaffold is reported.
View Article and Find Full Text PDFCannabinoids as cytotoxic agents and potential modulators of the human parasite Trichomonas vaginalis.
Biomed Pharmacother
January 2025
Structural Biology Laboratory, Oswaldo Cruz Institution, Fiocruz, Rio de Janeiro, Brazil; Programa de Pós-graduação em Biologia Celular e Molecular, Oswaldo Cruz Institution, Fiocruz, Rio de Janeiro, Brazil. Electronic address:
Trichomoniasis, a globally prevalent sexually transmitted infection caused by Trichomonas vaginalis, affects approximately 278 million people each year. It presents a challenge due to resistance to the current treatment, Metronidazole (MTZ), which is also associated with side effects. Cannabis sativa, with more than 100 phytocannabinoids and numerous studies for therapeutic applications, including parasitic infections, has undergone a significant shift in acceptance worldwide, highlighted by legalizations and substantial revenue projections.
View Article and Find Full Text PDFIdentification and field testing of sex-attractant semiochemicals produced by male deer mice, .
R Soc Open Sci
December 2024
Department of Biological Sciences, Simon Fraser University, Burnaby, British Columbia V5A 1S6, Canada.
Following previous reports that male deer mice, , produce chemical signals that attract conspecific females, we analysed and field-tested sex-attractant semiochemicals (message-bearing chemicals) of male deer mice. Field traps baited with urine- and faeces-soiled bedding of male mice captured adult female, but not male, mice, indicating dissemination of sex-attractant semiochemicals from the males' excreta. Analysing excreta headspace volatiles of both males and females by gas chromatography-mass spectrometry revealed that 5-methyl-2-hexanone was male-specific, and that eight other ketones (3-methyl-2-pentanone, 2-hexanone, 4-heptanone, 2-heptanone, 6-methyl-2-heptanone, 3-octanone, 2-octanone, 2-nonanone) were 2.
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