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Joanne Mather, Paul D Rainville, Warren B Potts, Norman W Smith, Robert S Plumb
A rapid, specific, assay was developed for the benzodiapine alprazolam in rat plasma using sub-2 ┬Ám particle liquid chromatography (LC) and tandem quadrupole mass spectrometry (MS/MS). The limit of quantification using protein precipitation was determined to 10 pg/mL, whereas the limit of quantification using solid-phase extraction (SPE) was determined to be 1.0 pg/mL. The assay was optimized for throughput and resolution of the analyte of interest from the hydroxy metabolite. During the method development process the plasma matrix signal was monitored, for lipids and other endogenous metabolites, to maximize signal response and minimize ion suppression...
January 2010: Drug Testing and Analysis
Eric Lattmann, Pornthip Lattmann, Yodchai Boonprakob, Wanchai Airarat, Harjit Singh, Michael Offel, Jintana Sattayasai
Oxazepam (CAS 604-75-1) 4a served as building block in the synthesis of substituted 3-amino-1,4-benzodiazepines, which were subsequently tested in various CNS animal models. The hydroxy group of oxazepam was either activated as a chloride (Method A) or as a phosphor-oxy derivative (Method B) giving the desired 3-amino-1,4-benzodiapines 6a-6r in high yields with primary and secondary amines in a typical nucleophilic substitution reaction. Eighteen 3-substituted 1,4-benzodiazepines were prepared and served as new chemical entities and for lead structure discovery...
2009: Arzneimittel-Forschung
Scott D Lane, Oleg V Tcheremissine, Lori M Lieving, Sylvain Nouvion, Don R Cherek
RATIONALE: GABA-A receptor ligands, including benzodiapines, may induce disinhibitory effects that increase the probability of risky decision making. To date, few laboratory studies have examined the acute, dose-related effects of benzodiazepines on human risk-taking behavior. Recent data indicate that in the United States alprazolam is the benzodiazepine most frequently misused for recreational purposes. OBJECTIVES: The present study was designed to demonstrate a dose-response relationship between acute alprazolam administration and human risk taking...
September 2005: Psychopharmacology
W W Yew
Clinically significant interactions occurring during antituberculous chemotherapy principally involve rifampicin (rifampin), isoniazid and the fluoroquinolones. Such interactions between the antituberculous drugs and coadministered agents are definitely much more important than among antituberculous drugs themselves. These can be associated with consequences even amounting to therapeutic failure or toxicity. Most of the interactions are pharmacokinetic rather than pharmacodynamic in nature. The cytochrome P450 isoform enzymes are responsible for many interactions (especially those involving rifampicin and isoniazid) during drug biotransformation (metabolism) in the liver and/or intestine...
2002: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
S Chaki, T Funakoshi, R Yoshikawa, S Okuyama, T Okubo, A Nakazato, M Nagamine, K Tomisawa
Here, we investigated the binding characteristics of [3H]N-(2,5-dimethoxybenzyl)-N-(5-fluoro-2-phenoxyphenyl)acetamide ([3H]DAA1106), a potent and selective ligand for peripheral benzodiazepine receptors, in mitochondrial fractions of the rat brain. [3H]DAA1106 bound to the mitochondrial fraction of the rat brain in a saturable manner. The dissociation constant (Kd) and maximal number of binding sites (Bmax) obtained from Scatchard plot analysis of the saturation curve of [3H]DAA1106 binding were 0.12 +/- 0...
April 29, 1999: European Journal of Pharmacology
L Dennerstein, A Callan, G Warne, J Montalto, J Brown, G Burrows, A Fulton, M Notelovitz
A single blind study was planned to investigate whether benzodiapines would reduce androgens in women with idiopathic hirsutism. Placebo was given for the first month followed by four months of a benzodiazepine (chlorazepate 15 mg nocte or diazepam 10 mg nocte ). Plasma samples were collected during the follicular and luteal phases of each therapy month. Hair growth was assessed monthly. Eighteen women concluded the five months of the trial of whom ten received chlorazepate and eight diazepam. Comparison of follicular plasma samples during the placebo phase and fourth month of benzodiazepine found a significant increase in sex hormone binding globulin and a significant decrease in dehydroepiandrosterone sulphate with benzodiazepine therapy...
1984: Progress in Neuro-psychopharmacology & Biological Psychiatry
P C Moser, P H Redfern
The effects of four benzodiazepines (diazepam, clonazepam, oxazepam and clobazam) were studied on the head-twitch response induced in mice by several 5-HT receptor agonists. All the benzodiazepines tested potentiated the effects of the directly acting agonists 5-methoxy-N,N-dimethyltryptamine (5-MeODMT), quipazine and mescaline, without themselves inducing head-twitches. In contrast, none of them potentiated head-twitches induced by the indirectly acting agonist 5-hydroxytryptophan (5-HTP; with carbidopa 25 mg/kg), and in some experiments a clear inhibition was seen...
July 7, 1988: European Journal of Pharmacology
G De Sarro, A De Sarro, F Federico, B S Meldrum
1. The anticonvulsant activity of calcium channel antagonists, was studied after intraperitoneal or oral administration in genetically epilepsy prone rats (GEPR). 2. Flunarizine, dihydropyridines and HA 1004, administered intraperitoneally, were the most potent compounds. Diltiazem, prenylamine, perhexiline, verapamil and methoxyverapamil, given intraperitoneally, were able to reduce the incidence of the tonic phase but were completely ineffective in preventing clonic and running phases of sound-induced seizures in GEPR...
1990: General Pharmacology
G T Bolger, S Abraham, N Oz, B A Weissman
The effects of the peripheral-type benzodiapine receptor (PBR) ligands Ro 5-4864 and PK 11195 were studied in the spontaneously beating guinea pig atrium and in a model for myocardial ischemia in the rat. In the former, Bay K 8644 produced positive chronotropic and inotropic responses; intracarotid administration of this agonist (5 or 10 micrograms kg-1) to anesthetized rats elicited a transient increase in mean arterial blood pressure accompanied by alterations in the ECG pattern. Ro 5-4864 and PK 11195 (10 microM) completely blocked the positive chronotropic effect of Bay K 8644 in the atrium, PK 11209, a structural analog of PK 11195 with a low affinity for PBR, was inactive, and the central benzodiazepine receptor ligand clonazepam had a marginal effect...
January 1990: Canadian Journal of Physiology and Pharmacology
T Tsuchiya, H Fukushima
Effects of benzodiapines administered by the intraperitoneal route on PGO firings and multiple unit activity in the midbrain reticular formation in chronic cat preparations were investigated at various levels of consciousness. Changes in the sleep-wakefulness cycle induced by direct injection of benzodiazepines into the reticular formation were also investigated. Benzodiazepines markedly decreased multiple unit activity in the midbrain reticular formation during each stage of sleep, but had little effect during behavioral and EEG arousal...
November 1977: Electroencephalography and Clinical Neurophysiology
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