Anticonvulsant activity of 7-phenyl-5H-thiazolo[5,4-e][1,2,3,4]tetrazolo[5,1-c]pyrrolo[1,2-a][1,4]diazepine (5) and 7-phenyl-5H-thiazolo[5,4-e][1,3,4]triazolo[5,1-c]pyrrolo[1,2-a][1,4]diazepines (6a-d) was measured against pentylenetetrazole (PTZ)-induced seizures in mice. Intraperitoneal injections of different doses (12.5, 25 and 50 mg/kg, i.p.) of test compounds decreased PTZ-induced seizure...

Benzodiazepines (BZDs) are an important class of psychoactive drugs with hypnotic-sedative, myorelaxant, anxiolytic and anticonvulsant properties due to interaction the GABAa receptor in central nervous system mammals. BZDs interesting both clinical forensic toxicology for their pharmacological characteristics potential abuse. The presence a non-planar diazepine ring generates chiral conformati...

A automedicação é o ato que consiste no paciente fazer uso dos fármacos por conta própria sem uma devida prescrição médica, e nos últimos anos vem se tornando um sério problema de saúde pública. Os psicotrópicos são substancias usadas há milênios possuem ação hipnóticas, sedativas, ansiolíticas antidepressivas. Como psicotrópicas constam os ansiolíticos, dentre quais, benzodiazepínicos (BZD). P...

BACKGROUND Saccadic eye velocity (SEV) has been shown to be a reliable neurophysiological tool for the assessment of gamma-aminobutyric acid GABA(A) receptor sensitivity. Administration of benzodiazepines targeting the GABA(A) receptor decreases SEV in healthy volunteers. Tiagabine is a new antiepileptic drug which acts via selective blockade of GABA reuptake. Therefore, we examined the effects...

A total of 588 blood specimens collected in an emergency unit were screened for benzodiazepines (BZDs) using enzyme-multiplied immunoassay and gas chromatography. Two-hundred eighty-five samples were positive for BZDs, and 303 samples that were negative by EMIT included 20 samples with BZDs detectable by gas-liquid chromatography. A total of 15 BZDs were identified, and the most frequently occu...

Here we characterized the first known transcriptional regulator that accounts for carbon catabolite repression (CCR) control of the anaerobic catabolism of aromatic compounds in bacteria. The AccR response regulator of Azoarcus sp. CIB controls succinate-responsive CCR of the central pathways for the anaerobic catabolism of aromatics by this strain. Phosphorylation of AccR to AccR-P triggers a ...

GABA is the major inhibitory neurotransmitter in the central nervous system (CNS). The type A GABA receptor (GABA(A)R) system is the primary pharmacological target for many drugs used in clinical anesthesia. The α1, β2, and γ2 subunit-containing GABA(A)Rs located in the various parts of CNS are thought to be involved in versatile effects caused by inhaled anesthetics and classic benzodiazepines...

BACKGROUND Benzodiazepines (BZDs), the most commonly prescribed psychotropic drugs with anxiolytic action, may cause hyposalivation. It has been previously shown that BZDs can cause hypertrophy and decrease the acini cell number. In this study, we investigated the effects of BZDs and pilocarpine on rat parotid glands, specifically on acinar, ductal, and myoepithelial cells. METHODS Ninety mal...