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Dibenzo[1,2,5]thiadiazepines are non-competitive GABAA receptor antagonists
type: Continuant
crisid: 3307
e iscopus: 2-s2.0-84872872369
abstract: 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. © 2013 by the authors.
related by: authorship_19182
issue: 1
type: Entity
page end: 913
has publication venue: Molecules
type: Information Content Entity
related by: authorship_19180
page start: 894
related by: authorship_19187
related by: authorship_19185
chemicalscas: 4 aminobutyric acid, 28805-76-7, 56-12-2; GABA-A Receptor Antagonists; Receptors, GABA-A; Thiadiazines; gamma-Aminobutyric Acid, 56-12-2
volume: 18
type: Document
related by: authorship_19183
type: Thing
estado: published
type: Generically Dependent Continuant
most specific type: Article
related by: authorship_19188
date time value: article date 3307
related by: authorship_19186
most specific type: Document
doi: 10.3390/molecules18010894
freetext keyword: Biological activity; Dibenzothiadiazepines; Electrophysiology; Enteric neurons; GABAA receptor antagonists; Neurochemistry; Patch clamp 4 aminobutyric acid; 4 aminobutyric acid A receptor; 4 aminobutyric acid A receptor blocking agent; 4 aminobutyric acid receptor; thiadiazine derivative; animal; article; cell culture; cytology; drug effect; female; guinea pig; IC 50; male; membrane potential; metabolism; myenteric plexus; patch clamp; primary cell culture; synthesis; Animals; Cells, Cultured; Female; GABA-A Receptor Antagonists; GABAergic Neurons; gamma-Aminobutyric Acid; Guinea Pigs; Inhibitory Concentration 50; Male; Membrane Potentials; Myenteric Plexus; Patch-Clamp Techniques; Primary Cell Culture; Receptors, GABA-A; Thiadiazines
related by: authorship_19181
pmid: 23344200
accesstype: All Open Access, Gold, Green
origen: scopus
related by: authorship_19184
type: Article

Generically Dependent Continuant
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RDF description of Dibenzo[1,2,5]thiadiazepines are non-competitive GABAA receptor antagonists - http://orbis.uaslp.mx/vivo/individual/scopus3306
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date: 2026-08-26T20:53:29
publisher: vivo
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Article
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Molecules
type: Periodical
publication venue for: Dibenzo[1,2,5]thiadiazepines are non-competitive GABAA receptor antagonists
type: Generically Dependent Continuant
type: Document
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Information Content Entity
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