Search results for "Azepine"

Sociodemographic characteristics of female habitual benzodiazepine consumers in the catchment area of a health care centre.

1997

Electrophysiological evidence for an inverse benzodiazepine receptor agonist in panic disorder.

1999

Abstract Inverse agonists of the GABA A receptor clearly decrease the amplitudes of the spontaneous EEG in the P-frequency range. Therefore, we tested the hypothesis that panic patients exhibit a reduction of the EEGs spectral power in the P-frequency band. Ten unmedicated patients with panic disorder and agoraphobia according to DSM-III-R criteria and 10 matched controls were investigated under baseline conditions, after hyperventilation and 30 min after hyperventilation. EEG recordings from the position P z and C z were performed under eyes closed conditions. At baseline conditions the patients suffering from panic disorder depicted a reduced P-power reaching statistically significance fo…

Actions of two GABAA receptor benzodiazepine-site ligands that are mediated via non-γ2-dependent modulation.

2011

The potent sedative-hypnotic zolpidem and the convulsant methyl-6,7-dimethoxy-4-ethyl-β-carboline-3-carboxylate (DMCM) act primarily by binding to the benzodiazepine site of the main inhibitory neurotransmitter receptor, the pentameric γ-aminobutyric acid type A receptor (GABA(A)). This binding depends critically on the wild-type F77 residue of the GABA(A) receptor γ2 subunit. Mice with γ2 subunit F77I point mutation (γ2I77 mouse line) lose the high-affinity nanomolar binding of these ligands as well as their most robust behavioral actions at low doses. Interestingly, the γ2I77 mice offer a tool to study the actions of these substances mediated via other possible binding sites of the GABA(A…

Locomotor and antidepressant-like effects of 5-HT(1A) agonist LY 228729 in prenatally benzodiazepine-exposed rats.

1998

Locomotor activity and antidepressant-like effect in the forced swim test (FST) of 5-HT(1A) agonist LY 228729 were investigated in adult rats prenatally exposed at doses of diazepam (DZ) and alprazolam (ALP) which induce persistent downregulation of GABA/ benzodiazepine (BZ) receptors. Prenatal exposure to ALP and DZ did not modify the efficacy of subchronic LY 228729 to decrease immobility time in the FST. Prenatal DZ and ALP potentiated the facilitatory effect of subchronic LY 228729 on locomotor activity; prenatal DZ was more effective than prenatal ALP. Moreover, prenatal DZ increased stereotypic movements induced by LY 228729. These data suggest that the persistent downregulation of GA…

Modulation by fenoldopam (SKF 82526) and bromocriptine of the electrically evoked release of vasopressin from the rat neurohypophysis. Effects of dop…

1986

1. Single neurointermediate lobes were fixed by their stalks to a platinum wire electrode and incubated in Krebs-bicarbonate solution. Vasopressin release into the medium was determined by a radioimmunoassay. Vasopressin secretion was increased by electrical stimulation (15 Hz, 10 s trains with 10 s intervals for 10 min). 2. Fenoldopam (SKF 82526) had a dual effect on vasopressin release, 30 nM decreasing (by 30%) and 3 μM increasing (by 32%) the evoked vasopressin secretion. The facilitatory effect of fenoldopam was antagonized in a concentration-dependent manner by flupenthixol but not by sulpiride. Sulpiride (1 μM) prevented the inhibitory effect of fenoldopam (30 μM). 3. After pretreatm…

A preliminary study on the stability of benzodiazepines in blood and plasma stored at 4 degrees C.

1997

An approach to determine the stability of benzodiazepines and some of their metabolites (n = 13) by means of a routinely applied gas chromatographic method using electron capture detection was made in this preliminary study. Validation data of the method are given. Spiked blood and plasma samples were stored at 4 degrees C and analysed at selected times up to 240 days. The concentrations of all analytes had decreased to at least 60% of the original levels at the end of the observation period. A clear pattern of breakdown could not be established. The data obtained suggest that results from long-term stored samples should be interpreted cautiously. Further investigations concerning the stabi…

2-Sulfoximidoyl Acetic Acids from Multicomponent Petasis Reactions and Their Use as Building Blocks in Syntheses of Sulfoximine Benzodiazepine Analog…

2021

Upon application of a multicomponent Petasis reaction, a broad range of NH-sulfoximines and boronic acids react with glyoxalic acid to afford the corresponding 2-substituted acetic acids with N-bound sulfoximidoyl groups. The protocol features excellent yields under ambient, metal-free conditions and short reaction times. Furthermore, the applicability of 2-sulfoximidoyl acetic acids as building blocks for synthesizing sulfoximine-based benzodiazepine analogues was demonstrated.

�ber die Bedeutung der Plasmaproteinbindung f�r Verteilung und Wirkung von Tranquillantien vom Benzodiazepintyp

1977

This paper discusses the problem if the plasma protein binding of benzodiazepine derivatives can influence distribution and pharmacological activity of the drugs. The distribution of the benzodiazepines in the organism is influenced not only by the plasma protein binding of the drugs, but also by several other factors, especially since the drugs are mostly lipophilic. Thus, an effect of the plasma protein binding on the distribution can only be expected if the benzodiazepine derivative is highly bound to the plasma proteins. Thus results have been shown only for diazepam and chlordiazepoxid, which indicate an effect of the plasma protein binding on distribution and pharmacological activity,…

Synthese und Kristallstrukturanalyse eines 2,4-Diaryl-2,3-dihydro-1H-1,5-benzodiazepins / Synthesis and Crystal Structure Analysis of a 2,4-Diaryl-2,…

2004

Abstract The enone unit of chalcones is a synthetically valuable substructure for the formation of heterocycles. Whereas propoxy groups as solubilizing side chains on the phenyl groups do not much affect the generation of pyrazole and pyridine rings, they reduce significantly the yield of the diazepine ring system 4. We attribute this effect to the large twist angles between the ring planes, which are demonstrated by a crystal structure analysis.

Vitamin C blocks inflammatory platelet-activating factor mimetics created by cigarette smoking.

1997

Cigarette smoking within minutes induces leukocyte adhesion to the vascular wall and formation of intravascular leukocyte-platelet aggregates. We find this is inhibited by platelet-activating factor (PAF) receptor antagonists, and correlates with the accumulation of PAF-like mediators in the blood of cigarette smoke-exposed hamsters. These mediators were PAF-like lipids, formed by nonenzymatic oxidative modification of existing phospholipids, that were distinct from biosynthetic PAF. These PAF-like lipids induced isolated human monocytes and platelets to aggregate, which greatly increased their secretion of IL-8 and macrophage inflammatory protein-1alpha. Both events were blocked by a PAF r…