Search results for: Anna Waszkielewicz

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Preliminary antifungal activity assay of selected chlorine‐containing derivatives of xanthone and phenoxyethyl amines

Karolina Klesiewicz, Dorota Żelaszczyk, Danuta Trojanowska, Bożena Bogusz, more

Chemical Biology & Drug Design > 92 > 5 > 1867 - 1875

The aim of this study was to evaluate antifungal activity in a diverse group of chlorine‐containing xanthone and phenoxyethyl amine derivatives – and to select the most promising compounds for further studies. The antifungal efficacy of 16 compounds was tested with qualitative and quantitative methods against both reference and clinical strains of dermatophytes, moulds and yeasts. The disc‐diffusion...

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HBK-14 and HBK-15, triple 5-HT1A, 5-HT7 and 5-HT3 antagonists with potent antidepressant- and anxiolytic-like properties, increase seizure threshold in various seizure tests in mice

Karolina Pytka, Katarzyna Socała, Anna Rapacz, Dorota Nieoczym, more

Progress in Neuro-Psychopharmacology and Biological Psychiatry > 2017 > 79 > PB > 378-385

Most antidepressants lower seizure threshold, which might be due to the modulation of serotonergic neurotransmission. Here, we investigated the effects of two 5-HT_1A, 5-HT₇ and 5-HT₃ antagonists, i.e., 1-(2-(2-(2,6-dimethylphenoxy)ethoxy)ethyl)-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-14) and 1-{2-[2-(2-chloro-6-methylphenoxy)ethoxy]ethyl}-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-15),...

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HBK-15 protects mice from stress-induced behavioral disturbances and changes in corticosterone, BDNF, and NGF levels

Karolina Pytka, Monika Głuch-Lutwin, Magdalena Kotańska, Elżbieta Żmudzka, more

Behavioural Brain Research > 2017 > 333 > C > 54-66

Unlike majority of current antidepressants, HBK-15–a 5-HT_1A and 5-HT₇ receptor antagonist – showed memory-enhancing properties. In this study, we aimed to further characterize pharmacological profile of HBK-15 and investigate its antidepressant- and anxiolytic-like activity in the mouse model of unpredictable chronic mild stress. We used sucrose consumption test, forced swim test and elevated plus...

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Single Administration of HBK-15—a Triple 5-HT_1A, 5-HT₇, and 5-HT₃ Receptor Antagonist—Reverses Depressive-Like Behaviors in Mouse Model of Depression Induced by Corticosterone

Karolina Pytka, Monika Głuch-Lutwin, Magdalena Kotańska, Anna Waszkielewicz, more

Molecular Neurobiology > 2018 > 55 > 5 > 3931-3945

Studies suggest that the blockade of 5-HT_1A, 5-HT₇, and 5-HT₃ receptor may increase the speed of antidepressant response. 1-[(2,6-Dimethylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-14) and 1-[(2-chloro-6-methylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine hydrochloride (HBK-15), dual 5-HT_1A and 5-HT₇ antagonists, showed significant antidepressant- and anxiolytic-like...

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HBK-14 and HBK-15 with antidepressant-like and/or memory-enhancing properties increase serotonin levels in the hippocampus after chronic treatment in mice

Karolina Pytka, Katarzyna Gawlik, Dorota Pawlica-Gosiewska, Jadwiga Witalis, more

Metabolic Brain Disease > 2017 > 32 > 2 > 547-556

5-HT_1A and 5-HT₇ receptor ligands might have antidepressant-like properties and improve cognitive function. We previously reported significant antidepressant- and anxiolytic-like effects of two dual 5-HT_1A and 5-HT₇ receptor antagonists in various behavioral tests in rodents. As a continuation of our previous experiments, in this study we aimed to investigate whether chronic administration of 1-[(2,6-dimethylphenoxy)ethoxyethyl]-4-(2-methoxyphenyl)piperazine...

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HBK-7 — A new xanthone derivative and a 5-HT1A receptor antagonist with antidepressant-like properties

Karolina Pytka, Grzegorz Kazek, Agata Siwek, Barbara Mordyl, more

Pharmacology Biochemistry and Behavior > 2016 > 146-147 > C > 35-43

Xanthone derivatives possess many biological properties, including neuroprotective, antioxidant or antidepressant-like. In this study we aimed to investigate antidepressant- and anxiolytic-like properties of a new xanthone derivative – 6-methoxy-4-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one (HBK-7), as well as its possible mechanism of action, and the influence on cognitive and motor function...

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The antidepressant-like activity of 6-methoxy-2-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one involves serotonergic 5-HT1A and 5-HT2A/C receptors activation

Karolina Pytka, Maria Walczak, Agnieszka Kij, Anna Rapacz, more

European Journal of Pharmacology > 2015 > 764 > Complete > 537-546

Xanthone derivatives have been shown to posses many biological properties. Some of them act within the central nervous system and show neuroprotective or antidepressant-like properties. Taking this into account we investigated antidepressant-like activity in mice and the possible mechanism of action of 6-methoxy-2-[4-(2-methoxyphenyl)piperazin-1-yl]-9H-xanthen-9-one (HBK-11) – a new xanthone derivative...

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Skin metabolism established with the use of MetaSite for selected retinoids employed in topical and systemic treatment of various skin disorders and found in cosmeceuticals

Karolina Słoczyńska, Agnieszka Gunia-Krzyżak, Dorota Żelaszczyk, Anna Waszkielewicz, more

Acta Biochimica Polonica > 2015 > 62 > 2 > 201-206

Purpose. Besides being widely used in cosmetics, retinoids are potent therapeutic agents used topically and systemically as anti-acne agents. The aim of this study was to predict with the use of MetaSite the skin metabolism of selected retinoids employed in treatment of skin disorders and found in cosmeceuticals. The following compounds were studied: retinol, retinaldehyde, retinoic acid, retinyl...

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The study of the lipophilicity of some aminoalkanol derivatives with anticonvulsant activity

Anna Waszkielewicz, Natalia Szkaradek, Elżbieta Pękala, Fabiola Galzarano, more

Biomedical Chromatography > 24 > 12 > 1365 - 1372

A series of new (phenoxyethyl)aminoalkanol derivatives were synthesized and evaluated for their anticonvulsant activity. The most promising compound seemed to be (R,S)‐1N‐[(2,6‐dimethyl)phenoxyethyl]amino‐2‐butanol, which displayed anti‐MES activity (in mice, i.p.) with protective index (TD₅₀/ED₅₀) of 5.712, corresponding to that of phenytoin (6.6), carbamazepine (4.9) and valproate (1.7). The lipophilicity...

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