Chemical structure and biological activity of the diazepines.

Danneberg, P; Kh, Weber

doi:10.1111/j.1365-2125.1983.tb02295.x

Cited by 36 publications

(10 citation statements)

References 48 publications

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“…They have anxiolytic, sedative-hypnotic, anticonvulsant, and muscle-relaxant properties [14] and act mainly by reinforcing inhibitory effects on the GABA-A receptor [15]. Diazepam has an elimination half-life of >24 h [14] and is metabolized in the liver [16].…”

Section: Introductionmentioning

confidence: 99%

Comparison of Clomethiazole and Diazepam in the Treatment of Alcohol Withdrawal Syndrome in Clinical Practice

2017

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Background: The objective of this retrospective study was to compare the effectivity and tolerability of diazepam and clomethiazole in the treatment of alcohol withdrawal syndrome (AWS) in a large clinical sample. Methods: The data of 566 patients admitted to an intensive care psychiatric unit in Germany (2010-2014) were evaluated. The course of withdrawal was analyzed on a matched sample (n = 152) consisting of a diazepam group (n = 76) and a clomethiazole group (n = 76). Medical assessment was based on a standardized point-based symptom rating scale called AESB (Alkoholentzugssymptom-Bogen), a German modified version of the Revised Clinical Institute Withdrawal Assessment of Alcohol Scale (CIWA-Ar). Results: Although the mean daily symptom reduction did not differ significantly, patients treated with clomethiazole were treated significantly shorter and needed less concomitant antipsychotic medication. Numbers of complications and adverse events did not show significant differences. Conclusion: Both clomethiazole and diazepam were effective and equally safe in the treatment of AWS. Clomethiazole provided a faster withdrawal and required less concomitant antipsychotic medication and therefore might be the more favorable option for patients and physicians. Taken into account the methodological limitations of the study (retrospective design, secondary matching, missing randomization, use of clomethiazole as drug of first choice), further studies are needed to confirm this result.

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Section: Introductionmentioning

confidence: 99%

Comparison of Clomethiazole and Diazepam in the Treatment of Alcohol Withdrawal Syndrome in Clinical Practice

2017

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“…Ro 5-6900 (le) (2',4'-dichlorodiazepam) has a high affinity for "peripheral-type'' binding sites ( K , -1.6 nM) but was inactive ( K , > 10 pM) at central BZ receptors. KW 1937 (2a) is a positional isomer of the 1,4-diazepine, brotizolam (Dannenberg and Weber, 1983). A p-chloro substitution in the phenyl group of this compound gives KW 1937 the same relative orientation as Ro 5-4864.…”

Section: Inhibition Of Radioligand Binding By Pharmacologic Agentsmentioning

confidence: 99%

“Peripheral‐Type”Binding Sites for Benzodiazepines in Brain: Relationship to the Convulsant Actions of Ro 5–4864

Weissman

Cott

Jackson

et al. 1985

Journal of Neurochemistry

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Previous studies have shown that Ro 5-4864 is a potent convulsant and increases the firing rate of substantia nigra zona reticulata neurons. The pharmacologic profile of compounds that antagonize these actions suggested that the effects of Ro 5-4864 were not mediated by "brain-type" benzodiazepine receptors. We examined a number of compounds that are structurally related to Ro 5-4864 for their capacities to displace [3H]Ro 5-4864 from "peripheral-type" binding sites and their potencies as convulsants (or as antagonists of Ro 5-4864-induced convulsions). It was observed that compounds such as KW 3600 (the N-desmethyl analog of Ro 5-4864), which have very low affinities for "peripheral-type" sites, are convulsants with a potency nearly equal to that of Ro 5-4864. In contrast, compounds such as Ro 5-6900 and PK 11195, which bind with very high affinities to "peripheral-type" binding sites, are neither convulsants nor do they antagonize the convulsant actions of Ro 5-4864. Within a series of compounds that are structurally related to Ro 5-4864 there is a good correlation (r = 0.93; p less than 0.01) between their potencies as convulsants and their capacities to displace [35S]t-butylbicyclophosphorothionate from sites that may be associated with the chloride ionophore. Thus, it appears that occupation of "peripheral-type" binding sites by high-affinity ligands may not be directly involved in the convulsant actions of Ro 5-4864 and related compounds.

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“…Compounds containing diazepine moieties are of significant interest in medicinal & pharmaceutical research due to their important biological activities 1 . Besides being core unit of commercial drugs such as Diazepam, Oxazepam, Laurazepam, Anthramycin & Mazhethramycin; there are numerous Diazepines that are described with antiinflammatory, anticancer, anti-HIV, antibacterial, herbicidal and PAF receptor antagonist activities 1,2,3 .…”

Section: Introductionmentioning

confidence: 99%

“…Besides being core unit of commercial drugs such as Diazepam, Oxazepam, Laurazepam, Anthramycin & Mazhethramycin; there are numerous Diazepines that are described with antiinflammatory, anticancer, anti-HIV, antibacterial, herbicidal and PAF receptor antagonist activities 1,2,3 . Investigators are motivated to continuously develop strategies for producing new diazepine-based compounds due to the surprisingly vast biological activities exhibited by diazepines 1 .…”

Section: Introductionmentioning

confidence: 99%

Untitled

2011

IJPSR

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Chemical structure and biological activity of the diazepines.

Abstract: Since the introduction of chlordiazepoxide and diazepam many diazepines have been developed. Use of these drugs is increasing and considerable knowledge has accumulated about their mechanisms of action. The structural and pharmacological properties of these drugs are surveyed briefly.

Cited by 36 publications

References 48 publications

Comparison of Clomethiazole and Diazepam in the Treatment of Alcohol Withdrawal Syndrome in Clinical Practice

Comparison of Clomethiazole and Diazepam in the Treatment of Alcohol Withdrawal Syndrome in Clinical Practice

“Peripheral‐Type”Binding Sites for Benzodiazepines in Brain: Relationship to the Convulsant Actions of Ro 5–4864

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