Effects of Buspirone, Diazepam, and Zolpidem on Open Field Behavior, and Brain [3H]Muscimol Binding After Buspirone Pretreatment

Siemiątkowski, Marek; Sienkiewicz-Jarosz, Halina; Czlonkowska, A; Bidziński, Andrzej; Płaźnik, Adam

doi:10.1016/s0091-3057(00)00200-8

Cited by 36 publications

(12 citation statements)

References 39 publications

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“…The present study also shows that CPV extract diminishes motor activity in mice in the same way as diazepam and other benzodiazepines (Siemiatkowski et al, 2000); the data obtained in the open field also support the suggested anxiolytic effect of the CPV extract (Prut and Belzung, 2003).…”

Section: Discussionsupporting

confidence: 86%

Preclinical toxicological assessment of a phytotherapeutic product – CPV (based on dry extracts of Crataegus oxyacantha L., Passiflora incarnata L., and Valeriana officinalis L.)

Tabach

Rodrigues

Carlini

2008

Phytotherapy Research

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Associations of plants have been widely used, for centuries, in Ayurveda and in Chinese medicine and have been increasingly acknowledged in Western medicine. The objective of this study is to assess the level of toxicity of an association of three plants: Crataegus oxyacantha, Passiflora incarnata, and Valeriana officinalis (CPV extract). This association was administered to rats, mice, and dogs, both acute and chronically for 180 days. The tests used in the acute experiments were: observational pharmacological screening, LD 50 , motor coordination and motor activity. Chronic tests carried out were: weight gain/loss and behavioral parameters in rats and in mice; estrus cycle, effects on fertility, and teratogenic studies in rats and of mutagenic features in mice, in addition to the Ames test. The following parameters were assessed in dogs: weight gain/loss, general physical conditions, water/food consumption and anatomopathological examination of the organs subsequent to the 180 days of treatment. All of the results were negative, showing that CPV administered in high doses and over a long period of time presents no toxicity, suggestive of the fact that this is an association devoid of risk for human beings.

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Section: Discussionsupporting

confidence: 86%

Preclinical toxicological assessment of a phytotherapeutic product – CPV (based on dry extracts of Crataegus oxyacantha L., Passiflora incarnata L., and Valeriana officinalis L.)

Tabach

Rodrigues

Carlini

2008

Phytotherapy Research

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“…SH-I-048A dose-dependently affected parameters of general motor activity and dexterity, in a manner similar to diazepam (Milić et al, 2012; Savić et al, 2009; Siemiatkowski et al, 2000). Among parameters of locomotor activity, the statistical significance of the sedative effect was reached for distance traveled during the recording period 5–10 min in SLA, at doses of 5 and 10 mg/kg, and the total distance traveled in OF, at the dose of 10 mg/kg.…”

Section: Discussionmentioning

confidence: 87%

Sh-I-048A, an in vitro non-selective super-agonist at the benzodiazepine site of GABAA receptors: The approximated activation of receptor subtypes may explain behavioral effects

et al. 2014

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Enormous progress in understanding the role of four populations of benzodiazepine-sensitive GABAA receptors was paralleled by the puzzling findings suggesting that substantial separation of behavioral effects may be accomplished by apparently non-selective modulators. We report on SH-I-048A, a newly-synthesized chiral positive modulator of GABAA receptors characterized by exceptional subnanomolar affinity, high efficacy and non-selectivity. Its influence on behavior was assessed in Wistar rats and contrasted to that obtained with 2 mg/kg diazepam. SH-I-048A reached micromolar concentrations in brain tissue, while the unbound fraction in brain homogenate was around 1.5%. The approximated electrophysiological responses, which estimated free concentrations of SH-I-048A or diazepam are able to elicit, suggested a similarity between the 10 mg/kg dose of the novel ligand and 2 mg/kg diazepam; however, SH-I-048A was relatively more active at α1- and α5-containing GABAA receptors. Behaviorally, SH-I-048A induced sedative, muscle relaxant and ataxic effects, reversed mechanical hyperalgesia 24 hours after injury, while it was devoid of clear anxiolytic actions and did not affect water-maze performance. While lack of clear anxiolytic actions may be connected with an enhanced potentiation at α1-containing GABAA receptors, the observed behavior in the rotarod, water maze and peripheral nerve injury tests was possibly affected by its prominent action at receptors containing the α5 subunit. The current results encourage further innovative approaches aimed at linking in vitro and in vivo data in order to help define fine-tuning mechanisms at four sensitive receptor populations that underlie subtle differences in behavioral profiles of benzodiazepine site ligands.

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“…Surgery for chemitrode implantation was performed on the 16th day after the beginning of drug treatment. It has been shown that this dose of buspirone has anxiolytic effect in rats tested in different animal models such as the elevated T-maze (Graeff et al 1998;Zanoveli et al 2005), open-field (Siemiatkowski et al 2000), and shock-probe/burying test (Treit and Fundytus 1988).…”

Section: Experiments 2: Buspirone Treatmentmentioning

confidence: 99%

Effects of fluoxetine and buspirone on the panicolytic-like response induced by the activation of 5-HT1A and 5-HT2A receptors in the rat dorsal periaqueductal gray

2005

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Effects of Buspirone, Diazepam, and Zolpidem on Open Field Behavior, and Brain [3H]Muscimol Binding After Buspirone Pretreatment

Cited by 36 publications

References 39 publications

Preclinical toxicological assessment of a phytotherapeutic product – CPV (based on dry extracts of Crataegus oxyacantha L., Passiflora incarnata L., and Valeriana officinalis L.)

Preclinical toxicological assessment of a phytotherapeutic product – CPV (based on dry extracts of Crataegus oxyacantha L., Passiflora incarnata L., and Valeriana officinalis L.)

Sh-I-048A, an in vitro non-selective super-agonist at the benzodiazepine site of GABAA receptors: The approximated activation of receptor subtypes may explain behavioral effects

Effects of fluoxetine and buspirone on the panicolytic-like response induced by the activation of 5-HT1A and 5-HT2A receptors in the rat dorsal periaqueductal gray

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