Effects of oxazolam, cloxazolam, and CS-386, new anti-anxiety drugs, on socially induced suppression and aggression in Pairs of monkeys

Kamioka, Toshiharu; Nakayama, Isao; Akiyama, Seigo; Takagi, H.

doi:10.1007/bf00426594

Cited by 14 publications

(2 citation statements)

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“…Preclinical studies showed that mexazolam was 2–3 times more effective than diazepam and cloxazolam at improving performance in conflict behavior or lever-pressing tests (regarded as a measure of an antianxiety effect) [ 21 , 22 ]. Mexazolam was also shown to inhibit megimide-induced convulsions in mice [ 23 ].…”

Section: Mexazolammentioning

confidence: 99%

Mexazolam: Clinical Efficacy and Tolerability in the Treatment of Anxiety

Fernandes

Moreira

2014

Neurol Ther

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IntroductionMexazolam is indicated for the management of anxiety with or without psychoneurotic conditions. In adult patients, the recommended daily dosage of mexazolam is 1–3 mg, administered three times daily. The objective of this article is to review the available information on the benzodiazepine (BZD) mexazolam and its clinical utility in treating patients with anxiety.MethodsThe PubMed database was searched using the keyword “mexazolam” with no date or language restrictions applied to the search. As only 11 papers were retrieved, some previously published manuscripts of interest known by the authors (not indexed on PubMed) have been added for completeness. Relevant information was selected for inclusion by the authors.ResultsA number of early studies demonstrated the ability of mexazolam to reduce anxiety symptoms with few side effects in patients with disorders associated with anxiety. Following on from this preliminary evidence, controlled studies directly comparing mexazolam with other BZDs showed that the drug is more effective than bromazepam and oxazolam, and is at least as effective as alprazolam. A larger, multicenter, phase IV study also showed that mexazolam 2 or 3 mg/day rapidly improved Hamilton Anxiety Rating Scale scores and substantially reduced the frequency and severity of numerous somatic anxiety symptoms in patients with anxiety disorders. With regard to safety, the clinical evidence indicates that mexazolam is generally well tolerated, with a low incidence of drowsiness and sedation. Furthermore, the lack of psychomotor or cognitive performance impairment following mexazolam administration may lead to better treatment compliance.ConclusionThe available clinical evidence suggests that mexazolam is an effective therapeutic option for the management of anxiety. However, larger, well-controlled clinical trials are needed to directly compare and contrast mexazolam’s efficacy and safety with other BZDs.Electronic supplementary materialThe online version of this article (doi:10.1007/s40120-014-0016-7) contains supplementary material, which is available to authorized users.

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Section: Mexazolammentioning

confidence: 99%

Mexazolam: Clinical Efficacy and Tolerability in the Treatment of Anxiety

Fernandes

Moreira

2014

Neurol Ther

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“…as an originally inactive compound that is internally metabolized into a pharmacologically active drug and which after administration generates a number of active metabolites, in this case, with a number of differentiated properties, viz. anticonvulsant (Ito et al, 2004), hypnotic (Inoue et al, 2000), sedative (Brisse et al, 1980) and skeletal muscle relaxant (Ansseau & von Frenckell, 1990), but which is extensively used because of its marked anxiolytic properties (Kamioka et al, 1977;Fischer-Cornelssen, 1981). The drug is administrated orally, either in a single large in-take as a premedication before anesthesia, or in separate smaller doses in the short-term management of anxiety.…”

Section: Introductionmentioning

confidence: 99%

Crystal structure and pseudosymmetry analysis of the triclinic prodrug cloxazolam (Z′ = 4)

Garraza

Gimenez²,

Vega

et al. 2019

Acta Crystallogr C

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The prodrug cloxazolam [systematic name: 13‐chloro‐2‐(2‐chlorophenyl)‐3‐oxa‐6,9‐diazatricyclo[8.4.0.02,6]tetradeca‐1(10),11,13‐trien‐8‐one], C17H14Cl2N2O2, crystallizes in the triclinic space group P, with four chemically identical independent molecules in the asymmetric unit. However, in order to facilitate the analysis of the striking pseudosymmetry relating the four independent molecules, the structure has been analysed and reported in the nonconventional centred B space‐group setting. Pseudosymmetry is an eminently local property, valid only in the realm of the unit‐cell boundary and not propagating to the whole crystal structure. It has been analyzed using the MP procedure described in the preceding article [Baggio (2019). Acta Cryst. C75, 837–850]. The molecules consist of a rigid core made up of three rings (five‐, six‐ and seven‐membered) and an extra six‐membered ring joined to the latter group by a single C—C bond, together with a clamping intramolecular C—H…O interaction preventing free rotation and providing additional rigidity. The four molecules in the asymmetric unit pair into dimers with almost exact twofold pseudosymmetry, further linked into (001) slabs as the building bricks of the structure. Interpenetration of slabs finally leads to a three‐dimensional structure of unusual compactness for an organic structure, with a Kitaigorodskii packing index of ca 0.71.

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Psychopharmacological Agents

Martin

Godel

Hunkeler

et al. 2000

Kirk-Othmer Encyclopedia of Chemical Technology

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Martin, James R.; Godel, T.; Hunkeler, W.; Jenck, F.; Moreau, J‐L.; Sleight, A. J.; and Widmer, U. (F. Hoffmann‐La Roche Ltd.). A number of important advances have occurred in the understanding and the treatment of disorders of the central nervous system including mood disorders, schizophrenia, anxiety disorders, insomnia, substance use disorders, and dementias. The plethora of novel drugs act by means of diverse neurobiological mechanisms and represent a great diversity of chemical structures. Along with improvements in the therapeutic index of anxiolytics, sedative–hypnotics, antidepressants, and antipsychotics, some progress has also been made in the search for drugs effective in the treatment of substance use disorders, as well as Alzheimer's disease and other dementias. Nonetheless, such improvements in symptomatic therapy have not been accompanied by the discovery of effective etiological and pathophysiological interventions. It is from here that the successful psychopharmacological agents of the future must come.

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Effects of oxazolam, cloxazolam, and CS-386, new anti-anxiety drugs, on socially induced suppression and aggression in Pairs of monkeys

Cited by 14 publications

References 10 publications

Mexazolam: Clinical Efficacy and Tolerability in the Treatment of Anxiety

Mexazolam: Clinical Efficacy and Tolerability in the Treatment of Anxiety

Crystal structure and pseudosymmetry analysis of the triclinic prodrug cloxazolam (Z′ = 4)

Psychopharmacological Agents

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