Search results for "Azepine"

Sensitive Screening of New Psychoactive Substances in Serum Using Liquid Chromatography-Quadrupole Time-of-Flight Mass Spectrometry.

2021

Abstract Analysis of new psychoactive substances (NPS) still poses a challenge for many institutions due to the number of available substances and the constantly changing drug market. Both new and well-known substances keep appearing and disappearing on the market, making it hard to adapt analytical methods in a timely manner. In this study we developed a qualitative screening approach for serum samples by means of liquid chromatography--quadrupole time-of-flight mass spectrometry. Samples were measured in data-dependent auto tandem mass spectrometry mode and identified by fragment spectra comparison, retention time and accurate mass. Approximately 500 NPS, including 195 synthetic cannabino…

Comparative studies on the detection of benzodiazepines in serum by means of immunoassays (FPIA).

1993

Serum was tested for benzodlazeplnes by fluorescence polarlzatlon Immunoassay (FPIA) on Abbott's ADx system uslng the benzodlazeplne serum reagents (Benzo S) and the benzodlazeplne urine reagents (Benzo U) after pretreatment of speclmens by means of acetone preclpltatlon. The followlng sera were included for comparing the two methods: negatlve sera spiked with varlous benzodlazeplnes; 80 sera randomly selected out of a total of 8654 serum specimens from Impalred drlvers; and blood speclmens from Indlvlduals who stated that they had taken benzodlazeplnes. The different benzodlazeplnes were added to serum st concentratlons of 25, 75, and 300 ng/mL. The low-dose benzodlazeplnes flunltrazepam a…

Production of specific antibodies and development of a non-isotopic immunoassay for carbamazepine by the carbonyl metallo-immunoassay (CMIA) method.

1995

Abstract As part of our ongoing work to extend the range of applications of the non-isotopic carbonyl metalloimmunoassay (CMIA), previously developed in our laboratory, we describe here the first CMIA study of carbamazepine. The CMIA method uses a metal carbonyl complex as a non-isotopic tracer, and in this case we chose to employ the dicobalt hexacarbonyl moiety (Co2(CO)6) attached to an alkyne. Two organometallic tracers, 3 and 7 , were synthesized, differentiated by the nature and length of the spacer arm of the Co2(CO)6 moiety. Two different coupling methods were subsequently used to synthesize the immunogens 1 and 2, the first one used a carbodiimide, while the second, employed dimethy…

Screening of oxazepine indole enantiomers by means of high performance liquid chromatography with imprinted polymer stationary phase.

2004

Chromatographic enantiomer separations of different oxazepine indole derivatives were performed using a molecularly imprinted polymer. A 5aR,12R,13S-trans-6,6-dimethyl-12,13-dihydro-6H-5a, 1 3-methanoindolo[2,1-b][1,3]naphthoxazepine-12-carboxamide enantiomerderivative was used as a template and the resultant polymer has shown enantiomer recognition for series of template related compounds. The mechanistic description of the chiral discrimination process is scrutinised, comparing the discrimination between the different conformations and substituents of the oxazepine indoles.

Inactivation and tachyphylaxis of heat-evoked inward currents in nociceptive primary sensory neurones of rats.

2000

In contrast to other sensory modalities, pain does not decrease when a noxious stimulus is applied at constant intensity (Greene & Hardy, 1962). From this lack of adaptation on the perceptive level it has traditionally been implied that primary nociceptive afferents also do not adapt upon constant stimulation. This is in contrast to the results of recordings from these afferents, which exhibit pronounced adaptation for physical as well as chemical stimuli (Meyer et al. 1994). Peripheral adaptation of nociceptive nerve endings is compensated by central summation (Mendell & Wall, 1965; Price et al. 1977); this slow summation process of small fibre input to the dorsal horn of the spinal cord i…

Diagnosis and therapeutic management of primary headache in an emergency setting

2013

Synthesis of isoindolo[1,4]benzoxazinone and isoindolo[1,5]benzoxazepine: two new ring systems of pharmaceutical interest

2015

Abstract Two new ring systems, isoindolo[1,4]benzoxazinone and isoindolo[1,5]benzoxazepine, were conveniently synthesized through cyclization of suitably substituted isoindole derivatives. Some of the new compounds exhibited antiproliferative activity against a wide range of human tumor cell lines with GI 50 mean values at low micromolar level (3.72–5.13 μM).

Isoindolo[1,5]benzoxazepines as potential antitumor and/or antiviral agents

2013

Synthesis and characterization of biotinylated and photoactivatable neuroleptics. Novel bifunctional probes for dopamine receptors

1992

Abstract We have synthesized and characterized a series of novel derivatives of established antagonists of the neurotransmitter dopamine, i.e. butyrophenones, hexahydrocarbolines and phenothiazenes. All derivatives were biotinylated, some of them carried an additional (photoactivatable) azido group. In the case of butyrophenones, the structural modifications were introduced at the aliphatic keto group and/or the heterocyclic ring system, both modifications resulting in significant decreases in binding affinity to dopamine D 2 and dopamine D 1 receptor subtypes. Biotinylation of hexahydrocarbolines significantly increased their binding affinity to D 1 receptors, with the affinity for D 2 rec…

Involvement of TRPV1 channels in the activity of the cannabinoid WIN 55,212-2 in an acute rat model of temporal lobe epilepsy

2016

The exogenous cannabinoid agonist WIN 55,212-2, (R)-(+)-[2,3-dihydro-5-methyl-3-(4-morpholinylmethyl) pyrrolo[1,2,3-de]-1,4-benzoxazin-6-Yl]-1-naphthalenylmethanone (WIN), has revealed to play a role on modulating the hyperexcitability phenomena in the hippocampus. Cannabinoid-mediated mechanisms of neuroprotection have recently been found to imply the modulation of transient receptor potential vanilloid 1 (TRPV1), a cationic channel subfamily that regulate synaptic excitation. In our study, we assessed the influence of pharmacological manipulation of TRPV1 function, alone and on WIN antiepileptic activity, in the Maximal Dentate Activation (MDA) acute model of temporal lobe epilepsy. Our r…