Background: Benzodiazepines are the most frequently used drug for the treatment of insomnia. Prolonged use of benzodiazepine therapy is not recommended. However, many patients, particularly older patients, have difficulties discontinuing therapy. Melatonin, a hormone that is produced at night by the pineal gland, promotes normal sleep in humans and augments sleep induction by benzodiazepine the...

Intention in this review is to present a picture of 1,4-benzodiazepine with particular attention to their reactions and uses in synthetic organic chemistry. Some of these reactions have been applied successfully to the synthesis of biologically important compounds. The main purpose of this review is to present a survey of the literature on 1,4-benzodiazepine chemistry.

Quantitative radiohistochemistry was utilized to study alterations of gamma-aminobutyric acid (GABA) and benzodiazepine receptors in the kindling model of epilepsy. The radioligands used for GABA and benzodiazepine receptors were [3H] muscimol and [3H]flunitrazepam, respectively. GABA receptor binding was increased by 22% in fascia dentata of the hippocampal formation but not in neocortex or su...

We have investigated the subcellular localization of the peripheral-type benzodiazepine receptor in rat adrenal gland using the high affinity ligand 3H-labeled 1-(2-chlorophenyl)-N-methyl-(1-methylpropyl)-3-isoquinoline carboxamide ([3H]PK11195). The autoradiographic pattern of [3H]PK11195 binding sites in tissue sections of adrenal gland is similar to the histochemical distribution of the mito...

OBJECTIVE Most depression treatment guidelines emphasize treatment with antidepressant medication and recommend that benzodiazepine use be minimized, particularly among elderly patients. However, little is known about patterns of benzodiazepine use in specialty mental health settings. The authors examined benzodiazepine use among a large sample of depressed patients treated in U.S. Department o...

BACKGROUND In an attempt to control chronic benzodiazepine use and its costs in the Netherlands, health care insurance reimbursement of this medication was stopped on January 1st 2009. This study investigates whether benzodiazepine prescriptions issued by general practitioners changed during the first two years following implementation of this regulation. METHODS Registry study based on data ...

AIMS This study evaluates the suitability of gas chromatographic-mass spectrometric (GC-MS) analysis to follow-up the extent of benzodiazepine (mis)use in a Belgian prison population and compares it to other analytical strategies (e.g. screening followed by confirmation of the positive samples). DESIGN AND PARTICIPANTS From February to August 1998, 598 persons were jailed of which 188 (31.4% ...

PURPOSE OF REVIEW Despite repeated recommendations to limit benzodiazepines to short-term use (2-4 weeks), doctors worldwide are still prescribing them for months or years. This over-prescribing has resulted in large populations of long-term users who have become dependent on benzodiazepines and has also led to leakage of benzodiazepines into the illicit drug market. This review outlines the ri...

Mitochondrial dysfunction has been identified as a possible early event in ischemia-reperfusion damage. The peripheral benzodiazepine receptor, a mitochondrial inner membrane protein, has already been proposed to play a role in mitochondrial regulation, although its exact function remains unclear. The aim of this work was to determine the role of peripheral benzodiazepine receptor in ischemia-r...

The benzodiazepine binding site of GABA(A) receptors is located at the interface of the alpha and gamma subunits. Certain point mutations in these subunits have been demonstrated to dramatically reduce the affinity of benzodiazepine binding site ligands for these receptors. Recently, mice were generated with a phenylalanine (F) to isoleucine (I) substitution at position 77 in the gamma2 subunit...