Clinically used benzodiazepine and nonbenzodiazepine sedative-hypnotic agents for the treatment of insomnia produce their therapeutic effects through allosteric enhancement of the effects of the inhibitory neurotransmitter GABA at the GABA(A) receptor. Indiplon is a novel pyrazolopyrimidine sedative-hypnotic agent, currently in development for insomnia. Using radioligand binding studies, indipl...

In previous studies using Fos expression as a marker of neuronal activation, we showed that nitrous oxide (N(2)O) activates bulbospinal noradrenergic neurons in rats and that destruction of these neuronal pathways leads to loss of N(2)O antinociceptive action. Based on previous rat studies it has been proposed that these noradrenergic neurons are activated through opioid receptors through the r...

We describe a quantitative screen for hypnotic-sedative drugs in which we use capillary gas chromatography with a nitrogen-phosphorus detector (GC/NPD) as the primary method and capillary gas chromatography-mass spectrometry (GC-MS) for confirmation. GC retention times of the acid-extracted underivatized drugs were stable (CVs less than 1%), and the detector response varied linearly over a 20-f...

Scoparia dulcis Linn. (SD) is a perennial herb that has been well studied for its antioxidant, anti-inflammatory, antidiabetic, and hepatoprotective effects. However, scientific information on SD regarding the neuropharmacological effect is limited. This study evaluated the sedative and hypnotic effect of the ethanolic extract of whole plants of Scoparia dulcis (EESD). For this purpose, the who...

T HE CONCEPT of tranquilizing drugs in medicine is a new one, going back little more than 5 years. The term itself is essentially a popular one and defies precise definition. In general, however, substances which are included tinder the general heading of tranquilizers are those which exert a favorable effect Ofl disturbed emotions of human beings, particularly in terms of relieving tension and...

Alcohol tolerance resulting from chronic administration is well known to be accompanied by cross-tolerance to sedative/anesthetic drugs, especially those acting on the gamma-aminobutyric acid type A receptors (GABAARs). Rats treated with chronic intermittent ethanol (CIE) show decreased function and altered pharmacology of GABAARs in hippocampal neurons, consistent with cell- and location-speci...

THIS review will treat the more commonly prescribed hypnotic agents and their sleep-inducing properties. Hypnotic agents that are seldom used (paraldehyde), drugs that are not singularly soporific but may be used either alone or as adjuncts in inducing sleep [e.g. meprobamate (Equanil, Miltown), chlordiazepoxide (Librium) and diazepam (Valium)] and drugs that have little soporific effect [antih...