A radioreceptor assay to study the affinity of benzodiazepines and their receptor binding activity in human plasma including their active metabolites.

Dorow, RG; Seidler, Jessica M.; Hh, Schneider

doi:10.1111/j.1365-2125.1982.tb01422.x

Cited by 32 publications

(9 citation statements)

References 19 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…in comparison with placebo. These results agree with the high receptor affinity (Dorow et al, 1982) of lormetazepam in vitro. The increase in heart rate reached a significant level in the first and second hours p.a.…”

Section: Discussionsupporting

confidence: 90%

Alcohol Interaction of Lormetazepam, Mepindolol Sulphate and Diazepam Measured by Performance on the Driving Simulator

Willumeit¹,

Ott²,

Neubert³

et al. 1984

Pharmacopsychiatry

View full text Add to dashboard Cite

Sixteen healthy volunteers of a mean age of means = 26.4 years took part in a driving simulator test in an eightfold crossover study under double-blind conditions. The additional influence of alcohol was tested acutely after a single administration of 2 mg lormetazepam, a new, highly effective derivative from the benzodiazepine class, 10 mg mepindolol sulphate, a new betablocker without sedating properties, and 10 mg diazepam. All drugs were compared with placebo and the test was performed 1, 2 and 3 hours after oral intake. The aim was to investigate particularly the risks relevant in road traffic caused by simultaneous intake of these substances with alcohol. For this purpose, besides the driving simulator, an accurate reaction test ( WDG ) and self-rating scales were used, the latter in order to assess subjective stress and anxiety levels. Lormetazepam, due to its strong sedating property, showed a reduction in driving performance and an increase in reaction time and pulse rate as compared with placebo, and these effects were highly potentiated by alcohol. Mepindolol sulphate expectedly reduced pulse rate when compared with placebo, otherwise there were no significant differences. Diazepam, when compared with placebo, like lormetazepam caused a reduction in driving performance and reaction capacity and an increase in pulse rate, but intensity and duration of this effect were less than with lormetazepam and did not reach statistical significance. No significant potentiating effects were observed after the additional application of alcohol.

show abstract

Section: Discussionsupporting

confidence: 90%

Alcohol Interaction of Lormetazepam, Mepindolol Sulphate and Diazepam Measured by Performance on the Driving Simulator

Willumeit¹,

Ott²,

Neubert³

et al. 1984

Pharmacopsychiatry

View full text Add to dashboard Cite

show abstract

“…Plasma levels of ligands binding to the BZ receptor, i.e. BZ (FNZ and LMZ) (data not shown) and Ro 15-1788 (Klotz et al 1984), were monitored on both experimental days with a BZ radioreceptor assay (Dorow et al 1982) and/or a HPLC assay (Timm and Zell 1983). Measurement of BZ binding equivalents in plasma 24 h after treatment showed still significant values for both BZ-treated groups: FNZ binding equivalents (ng/ml) -FNZ group 4.87 4-1.8; LMZ group 3.02+_ 1.38.…”

Section: Resultsmentioning

confidence: 99%

“…Coefficients of inter-or intra-assay variations were 7% and 6%, respectively. Concentrations of benzodiazepine binding equivalents in plasma were measured with a radioreceptor assay (Dorow et al 1982). For statistical evaluation the Wilcoxon matched paired test and Mann-Whitney U-test were employed.…”

Section: Methodsmentioning

confidence: 99%

Changes in noradrenaline plasma levels and behavioural responses induced by benzodiazepine agonists with the benzodiazepine antagonist Ro 15-1788

Duka¹,

Ackenheil²,

Noderer

et al. 1986

Psychopharmacology

View full text Add to dashboard Cite

Noradrenaline (NA) plasma levels were examined in 18 healthy volunteers on 2 consecutive days after a single treatment with either lormetazepam (0.06 mg/kg) (LMZ group), flunitrazepam (0.03 mg/kg) (FNZ group) or placebo (PLA group) in combination with the benzodiazepine (BZ) antagonist Ro 15-1788 (0.1 mg/kg). Behavioural responses (mood changes, anxiety) were also investigated in parallel. Both BZ decreased NA plasma levels to 50% of the basal values 10 min after the injection; administration of Ro 15-1788 15 min later reinstated NA plasma levels to basal values. A second administration of Ro 15-1788 (0.1 mg/kg) 24 h after BZ or PLA treatment increased NA plasma levels, estimated 10 min after the injection in both the LMZ- and the FNZ groups, but not in the PLA group. Behavioural responses measured under the same treatment also indicated minor anxiety responses followed by mood impairment. These data suggest that a stressful situation may be precipitated by the antagonist Ro 15-1788 24 h after a single BZ treatment, which resembles a withdrawal response, and increases NA plasma levels.

show abstract

“…These specific affinities are justified by the choice of the competitor ligand and the kind of receptor tissue material. Indeed, flunitrazepam which is a fluorine nitrazepam derivative was selected because of its high affinity for benzodiazepine receptors [39]. In the same way, spiperone and DAMGO have respectively high affinity for dopaminergic and µ receptors.…”

Section: Discussionmentioning

confidence: 99%

Neurosedative and Antioxidant Activities of Phenylpropanoids from Ballota nigra

Daels-Rakotoarison

Seidel²,

Gressier

et al. 2011

Arzneimittelforschung

View full text Add to dashboard Cite

Ballota nigra is a European plant known for its neurosedative properties. In this study, the ability of five phenylpropanoids (verbascoside, forsythoside B, arenarioside, ballotetroside, and caffeoyl malic acid) isolated from a hydroalcoholic extract, to bind to benzodiazepine, dopaminergic, and morphinic receptors was investigated. To carry out these studies, affinity tests with rat striata, entire brains and receptor rich preparations were employed. In addition, the phenolic aspect of these five phenylpropanoid esters led to investigate antioxidant activities using cell-free experiments and cellular experiments including isolated polymorphonuclear neutrophils (PMN). Effects of phenylpropanoid esters against reactive oxygen species as superoxide anion, peroxide hydrogen, hypochlorous acid and hydroxyl radical were tested. These molecules are liberated by PMN during inflammatory disorders, so that reproduction of this process in vitro stimulating PMN by chemical stimulants was undertaken. Results show that four of the five compounds are able to bind to the studied receptors. Inhibitory concentrations at 50% were determined and vary from 0.4 to 4.7 mg/ml. This may be in relation with the Ballota nigra known neurosedative activities. Results concerning antioxidant investigations evidence an ability to scavenge reactive oxygen species. Inhibitory concentrations at 50% obtained are comparable to those of known antioxidant drugs (mesna or N-acetyl cysteine). Moreover, the use of different stimuli having various pathways of action on PMN oxidative metabolism permits to establish that each phenylpropanoid ester has its own particular way of action by using proteine kinase C or phospholipase C pathways.

show abstract

A radioreceptor assay to study the affinity of benzodiazepines and their receptor binding activity in human plasma including their active metabolites.

Cited by 32 publications

References 19 publications

Alcohol Interaction of Lormetazepam, Mepindolol Sulphate and Diazepam Measured by Performance on the Driving Simulator

Alcohol Interaction of Lormetazepam, Mepindolol Sulphate and Diazepam Measured by Performance on the Driving Simulator

Changes in noradrenaline plasma levels and behavioural responses induced by benzodiazepine agonists with the benzodiazepine antagonist Ro 15-1788

Neurosedative and Antioxidant Activities of Phenylpropanoids from Ballota nigra

Contact Info

Product

Resources

About