t-Butylbicyclophosphorothionate (TBPS), a derivative of potent GABA antagonistic cage convulsants, has recently been introduced (Squires, R. F., J. E. Casida, M. Richardson, and E. Saederup (1983) Mol. Pharmacol. 13: 326-336) as ligand for a GABA-A receptor-linked drug receptor. Using conventionally prepared washed membrane fractions from rat cerebral cortex, we have confirmed that in the prese...

1,5-Benzodiazepine derivatives were synthesized by the condensation reactions of o-phenylenediamine and ketones catalyzed by bismuth (III) salts under mild conditions. This method is easy, efficient, environment and eco-friendly, free of toxic catalysts, and gives good to excellent yields of 1, 5-benzodiazepines.

The pharmacological effects of 4-phenyl-2-trichloromethyl-3H-1, 5-benzodiazepine hydrogen sulfate (PTMB), a novel synthetic benzodiazepine, were examined in mice. In the elevated plus-maze test of anxiety, 0.3-1 mg/kg diazepam ip (F(3,53) = 3.78; P<0.05) and 1-10 mg/kg PTMB ip increased (F(5,98) = 3.26; P<0.01), whereas 2 mg/kg picrotoxin ip decreased (F(3,59) = 8.32; P<0.001) the proportion of...

conclusions zolpidem dependency and withdrawal seizure can occur with a dosage under last reported doses. therefore, possibility of mentioned problems cannot be excluded at any dosage and physicians should pay more attention to potential of zolpidem to create these adverse effects. introduction zolpidem is a short acting inducer of sleep and thought to lack benzodiazepine properties such as anx...

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...

OBJECTIVES To determine the risk of injury associated with the new use of individual benzodiazepines and dosage regimens in the elderly. DESIGN Prospective database cohort study with 5 years of follow-up. SETTING Quebec, Canada. PARTICIPANTS Two hundred fifty-three thousand two hundred forty-four persons aged 65 and older who were nonusers of benzodiazepines in the year before follow-up. ...

OBJECTIVE This study examined the risk of accidental events in older adults prescribed a sedating antidepressant, long-acting benzodiazepine, short-acting benzodiazepine, and nonbenzodiazepine, relative to a reference group (selective melatonin receptor agonist). METHODS This was a retrospective cohort analysis of older adults (≥65 years) with newly initiated pharmacological treatment of inso...

In the title compound, C(21)H(21)N(5)O(2)·H(2)O, the seven-membered ring adopts a boat-shaped conformation with the methine C atom as the prow. In the crystal, the water mol-ecule links adjacent mol-ecules by O-H⋯O and O-H⋯N hydrogen bonds into a zigzag chain running along the c axis of the monoclinic cell.

Modification of glutamatergic synaptic function, a mechanism central to neuronal plasticity, may also mediate long-term drug effects, including dependence and addiction. Benzodiazepine withdrawal results in increased glutamatergic strength, but whether -amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptors (AMPARs) are functionally and structurally remodeled during benzodiazepine ...