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http://ipicyt.repositorioinstitucional.mx/jspui/handle/1010/1225| Dibenzo[1,2,5]thiadiazepines are non-competitive GABAA receptor antagonists | |
| JUAN FRANCISCO RAMIREZ MARTINEZ RODOLFO GONZALEZ CHAVEZ RAQUEL GUERRERO ALBA PAUL EDUARDO REYES GUTIERREZ ROBERTO MARTINEZ MARCELA MIRANDA MORALES ROSA ESPINOSA LUNA MARCO MARTIN GONZALEZ CHAVEZ CARLOS BARAJAS LOPEZ | |
| Acceso Abierto | |
| Atribución-NoComercial-SinDerivadas | |
| http://dx.doi.org/10.3390/molecules18010894 | |
| Dibenzothiadiazepines GABAA receptor antagonists Patch clamp Neurochemistry Biological activity Enteric neurons Electrophysiology | |
| "A new process for obtaining dibenzo[c,f][1,2,5]thiadiazepines (DBTDs) and their effects on GABAA receptors of guinea pig myenteric neurons are described. Synthesis of DBTD derivatives began with two commercial aromatic compounds. An azide group was obtained after two sequential reactions, and the central ring was closed via a nitrene to obtain the tricyclic sulfonamides (DBTDs). Whole-cell recordings showed that DBTDs application did not affect the holding current but inhibited the currents induced by GABA (IGABA), which are mediated by GABAA receptors. These DBTDs effects reached their maximum 3 min after application and were: (i) reversible, (ii) concentration-dependent (with a rank order of potency of 2c = 2d > 2b), (iii) mediated by a non-competitive antagonism, and (iv) only observed when applied extracellularly. Picrotoxin (which binds in the channel mouth) and DBTDs effects were not modified when both substances were simultaneous applied. Our results indicate that DBTD acted on the extracellular domain of GABAA channels but independent of the picrotoxin, benzodiazepine, and GABA binding sites. DBTDs used here could be the initial model for synthesizing new GABAA receptor inhibitors with a potential to be used as antidotes for positive modulators of these receptors or to induce experimental epilepsy." | |
| MDPI AG | |
| 2013 | |
| Artículo | |
| Inglés | |
| Público en general | |
| Ramírez-Martínez, J., González-Chávez, R., Guerrero-Alba, R., Reyes-Gutiérrez, P., Martínez, R., Miranda-Morales, M., Espinosa-Luna, R., et al. (2013). Dibenzo[1,2,5]thiadiazepines Are Non-Competitive GABAA Receptor Antagonists. Molecules, 18(1), 894–913. MDPI AG. Retrieved from http://dx.doi.org/10.3390/molecules18010894 | |
| BIOLOGÍA Y QUÍMICA | |
| Versión publicada | |
| publishedVersion - Versión publicada | |
| Aparece en las colecciones: | Publicaciones Científicas Biología Molecular |
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