Benzodiazepines receptor

AMNES - AMINES,AROMATIC - PHENYLENEDIAMINES] (Vol 2) benzodiazepine receptor complex... 

Nonbenzodiazepine Benzodiazepine Receptor Ligands. The simultaneous discovery of the molecular target for the BZs, the GABA /BZ receptor complex, by two teams of workers (34,35) resulted ia the identification of a number of atypical or anxioselective anxiolytics that, whereas not having the BZ pharmacophore, interacted direcdy with the central BZ receptor. The anxioselective nature of such agents was considered to be... 

Synthesis of imidazo[l,2-d]pyridazines and their interaction with central and peripheral-type (mitochondrial) benzodiazepine receptors 98JHC1205. 

A medication that causes induction of sleep. The majority of currently available hypnotics (for example benzodiazepine receptor agonists) act via potentiating the brain s inhibitory GABAergic systems, in turn reducing the activity of arousal (i.e. wake promoting) neurotransmitter systems. 

The benzodiazepines currently available for clinical use vary substantially in pharmacokinetics, acute euphoriant effects, and frequency of reported dependence. It is likely, therefore, than not all benzodiazepines have the same potential for abuse. Diazepam, lorazepam, and alprazolam may have greater abuse potential than chlordiazepoxide and clorazepate (Wolf et al. 1990). Similarly, oxazepam has been reported to produce low levels of abuse (Eliding 1978). Jaffe et al. (1983) found that in recently detoxified alcoholic patients, halazepam produces minimal euphoria even at a supratherapeutic dosage. The development of partial agonist and mixed agonist/antagonist compounds at the benzodiazepine receptor complex may offer an advantage over approved benzodiazepines for use in alcoholic patients. 

Farde L, Pauli S, Litton JE, et al PET-determination of benzodiazepine receptor binding in studies on alcoholism. EXS 71 143—153, 1994... 

Clinical experience suggests that alprazolam can be particularly difficult to taper when lower doses are reached (e.g., tapering from 1 to 0 mg) (Ciraulo et al. 1990). One possible explanation for this is suggested by data from an animal model showing that alprazolam at doses of 0.02—0.05 mg/kg increases benzodiazepine receptor number above baseline (Miller et al. 1987). When difficulty is encountered in tapering the last 1—2 mg of alprazolam, the rate of dose reduction can be decreased to 0.25 mg/week, and/or adjunctive medication may... 

Braestrup C, Nielsen M, HonoreT, etal Benzodiazepine receptor ligands with positive and negative efficacy. Neuropharmacology 22 1451—1457, 1983... 

Buldakova S, Weiss M Electrophysiological evidence for agonist properties of flumazenil, a benzodiazepine receptor antagonist, in rat hippocampus slices. J Neurol Sci 149 121-126, 1997... 

Miller LG, Greenblatt DJ, Barnhill JG, et ah Benzodiazepine receptor binding of tri-azolobenzodiazepines in vivo increased receptor number with low-dose alprazolam. J Neurochem 49 1595-1601, 1987... 

Nutt DJ, Glue P, Lawson C, et al Flumazenil provocation of panic attacks evidence for altered benzodiazepine receptor sensitivity in panic disorder. Arch Gen Psychiatry 47 917-923, 1990... 

Pritchett DB, Seeburg PH Gamma-aminobutyric acidA receptor alpha3-subunit creates novel type II benzodiazepine receptor pharmacology. J Neurochem 34 1802-1804, 1990... 

Reynaud M, Petit G, Potard D, et al Six deaths linked to concomitant use of buprenor-phine and benzodiazepines. Addiction 93 1383-1392, 1998 Richards JG, Martin JR Binding profiles and physical dependence liabilities of selected benzodiazepine receptor ligands. Brain Res Bull 43 381-387, 1998... 

The term benzodiazepine refers to a specific chemical structure. Numerous benzodiazepine-receptor ligands exist which have different structures. These include the jS-carbolines (e.g. methyl-6,7-dimethoxy-4-ethyl-jS-carboline 3-carboxylate DMCM), triazolopyridazines (e.g. CL 218872), imidazopyridines (e.g. zolpidem), and pyrazolo-quinolinones (e.g. CGS 8216). In experimental animals these compounds produce... 

The discovery of the benzodiazepine receptor was quickly followed by their subdivision as evidenced by (see also Chapter 11) ... 

Competition binding studies showing that when using compounds like jS-CCE (ethyl- S-carboline-3-carboxylate), which bind to the benzodiazepine receptor, the displacement curve for [ H]flunitrazepam was shallow in the hippocampus and... 

THE BENZODIAZEPINE RECEPTOR AGONIST/INVERSE AGONIST SPECTRUM... 

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