Search results for: Anna Rapacz

Items from 1 to 20 out of 30 results

article

Promising anticonvulsant and/or analgesic compounds among 5‐chloro‐2‐ or 5‐chloro‐4‐methyl derivatives of xanthone coupled to aminoalkanol moieties—Design, synthesis and pharmacological evaluation

Gabriela Mazur, Katarzyna Pańczyk‐Straszak, Anna Rapacz, Jan Kiszela, more

Chemical Biology & Drug Design > 101 > 2 > 278 - 325

A series of 10 aminoalkanol derivatives of 5‐chloro‐2‐ or 5‐chloro‐4‐methylxanthone was synthetized and evaluated for anticonvulsant properties (MES test, mice, intraperitoneal) and compared with neurotoxicity rotarod test (NT, mice, i.p.). The best results both in terms of anticonvulsant activity and protective index value were obtained for 3: 5‐chloro‐2‐([4‐hydroxypiperidin‐1‐yl]methyl)‐9H‐xanthen‐9‐one...

article

Synthesis, anticonvulsant, and antinociceptive activity of new 3‐(3‐methyl‐2,5‐dioxo‐3‐phenylpyrrolidin‐1‐yl)propanamides and 3‐phenyl‐butanamides

Jolanta Obniska, Małgorzata Góra, Anna Rapacz, Kinga Sałat, more

Archiv der Pharmazie > 354 > 1 > n/a - n/a

A focused library of new 3‐(3‐methyl‐2,5‐dioxo‐3‐phenylpyrrolidin‐1‐yl)propanamides and their nonimide analogs were synthesized and tested for anticonvulsant activity. These compounds were obtained through the coupling reaction of the starting carboxylic acids with appropriate amines. The initial anticonvulsant screening was performed in mice (intraperitoneal administration) using the maximal electroshock...

article

KA‐104, a new multitargeted anticonvulsant with potent antinociceptive activity in preclinical models

Krzysztof Kamiński, Szczepan Mogilski, Michał Abram, Anna Rapacz, more

Epilepsia > 61 > 10 > 2119 - 2128

Objective The main objective of the present work was to assess the utility of KA‐104 as potential therapy for drug‐resistant seizures and neuropathic pain, and to characterize its druglike properties in a series of absorption, distribution, metabolism, excretion and toxicity (ADME‐Tox) studies. We also aimed to establish its mechanism of action in electrophysiological studies. Methods The activity...

article

The preliminary studies on protein profile in retained and not retained foetal membranes in heavy draft mares

Jacek Wawrzykowski, Anna Rapacz‐Leonard, Dariusz Wiącek, Marta Kankofer, more

Reproduction in Domestic Animals > 54 > 12 > 1543 - 1551

Protein profile of the placenta expresses its function and maintenance. Any alterations can be reflected in qualitative and quantitative changes in this profile. The aim of the present study was the evaluation of protein profile in the placenta of mares suffering from the retention of foetal membranes (FMR) by two separation methods and the comparison with physiologically released tissues. Placentas...

article

ADVANCES AND LIMITATIONS IN PHARMACOTHERAPY OF EPILEPSY

Anna Rapacz

Acta Poloniae Pharmaceutica - Drug Research > 2018 > 75 > 5 > 1069-1082

Epilepsy is a chronic neurologic disorder that affects about 0.7% of the population. Patients with epilepsy suffer from recurrent seizures, which can be focal or generalized in nature. The third-generation of anticonvulsant drugs includes lacosamide, rufinamide, vigabatrin, retigabine, perampanel, eslicarbazepine acetate, brivaracetam and stiripentol. Other compounds, such as ganaxolone, cannabidiol,...

article

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),...

article

Synthesis and Anticonvulsant Properties of New 3,3‐Diphenyl‐2,5‐dioxo‐pyrrolidin‐1‐yl‐acetamides and 3,3‐Diphenyl‐propionamides

Jolanta Obniska, Anna Rapacz, Sabina Rybka, Małgorzata Góra, more

Archiv der Pharmazie > 350 > 3-4 > n/a - n/a

The focused library of new amides derived from 3,3‐diphenyl‐2,5‐dioxo‐pyrrolidin‐1‐yl‐acetic acid (2a–t) and 3,3‐diphenyl‐propionic acid (3a–t) as potential anticonvulsant agents was synthesized. The final products were obtained in the amidation reaction of the given carboxylic acid (2, 3) with appropriate secondary amines in the presence of carbonyldiimidazole (CDI) as a coupling reagent. The initial...

article

Synthesis and evaluation of anticonvulsant properties of new N-Mannich bases derived from pyrrolidine-2,5-dione and its 3-methyl-, 3-isopropyl, and 3-benzhydryl analogs

Sabina Rybka, Jolanta Obniska, Anna Rapacz, Barbara Filipek, more

Bioorganic & Medicinal Chemistry Letters > 2017 > 27 > 6 > 1412-1415

The aim of this paper was to describe the synthesis of a library of 28 new 1,3-substituted pyrrolidine-2,5-dione as potential anticonvulsant agents. The anticonvulsant activity was evaluated using three acute models of seizures in mice (MES-maximal electroshock, scPTZ-subcutaneous pentylenetetrazole, and 6Hz-psychomotor seizure tests). The neurotoxicity was determined by rotarod test. The most promising...

article

Analgesic, antiallodynic, and anticonvulsant activity of novel hybrid molecules derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide in animal models of pain and epilepsy

Anna Rapacz, Krzysztof Kamiński, Jolanta Obniska, Paulina Koczurkiewicz, more

Naunyn-Schmiedeberg's Archives of Pharmacology > 2017 > 390 > 6 > 567-579

The purpose of the present study was to examine the analgesic activity of six novel hybrid molecules, which demonstrated in the previous research anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure (scPTZ) tests in mice. The antinociceptive properties were estimated in three models of pain in mice—the hot plate test, the formalin test, and...

article

Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH3 or 2-CH3

Agnieszka Gunia-Krzyżak, Dorota Żelaszczyk, Anna Rapacz, Ewa Żesławska, more

Bioorganic & Medicinal Chemistry > 2017 > 25 > 2 > 471-482

A series of twenty two (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH₃ or 2-CH₃ was designed, synthesized and evaluated for anticonvulsant activity in rodent models of seizures: maximal electroshock (MES) test, subcutaneous pentylenetetrazole (scPTZ) test, and 6-Hz test. There were identified three most active compounds: S-(2E)-N-(1-hydroxypropan-2-yl)-3-(2-methylphenyl)prop-2-enamide...

article

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...

article

Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides

Krzysztof Kamiński, Anna Rapacz, Barbara Filipek, Jolanta Obniska

Bioorganic & Medicinal Chemistry > 2016 > 24 > 13 > 2938-2946

The focused library of 21 new N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide, 2-(3-methyl-2,5-dioxopyrrolidin-1-yl)propanamide, and 2-(2,5-dioxopyrrolidin-1-yl)butanamide derivatives as potential new hybrid anticonvulsant agents was synthesized. These hybrid molecules were obtained as close analogs of previously described N-benzyl derivatives and fuse the chemical fragments of clinically relevant...

article

Anticonvulsant and antinociceptive activity of new amides derived from 3-phenyl-2,5-dioxo-pyrrolidine-1-yl-acetic acid in mice

Anna Rapacz, Jolanta Obniska, Beata Wiklik-Poudel, Sabina Rybka, more

European Journal of Pharmacology > 2016 > 781 > C > 239-249

The aim of the present experiments was to examine the anticonvulsant and antinociceptive activity of five new amides derived from 3-phenyl-2,5-dioxo-pyrrolidine-1-yl-acetic acid in animal models of seizures and pain. The antiseizure activity was investigated in three acute models of seizures, namely, the maximal electroshock (MES), the subcutaneous pentylenetetrazole (scPTZ), and 6Hz psychomotor seizure...

article

Synthesis and evaluation of anticonvulsant properties of new N-Mannich bases derived from 3-(1-phenylethyl)- and 3-benzyl-pyrrolidine-2,5-dione

Sabina Rybka, Jolanta Obniska, Anna Rapacz, Anna Furgała, more

Bioorganic & Medicinal Chemistry Letters > 2016 > 26 > 9 > 2147-2151

Two series of new derivatives of pyrrolidine-2,5-dione were synthesized and evaluated for their anticonvulsant properties. Initial screening for their anticonvulsant properties was performed in mice after intraperitoneal administration, using the maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ) and 6-Hz seizure tests. Quantitative pharmacological research revealed that the highest...

article

Synthesis, and anticonvulsant activity of new amides derived from 3-methyl- or 3-ethyl-3-methyl-2,5-dioxo-pyrrolidin-1-yl-acetic acids

Jolanta Obniska, Anna Rapacz, Sabina Rybka, Małgorzata Góra, more

Bioorganic & Medicinal Chemistry > 2016 > 24 > 8 > 1598-1607

This paper describes the synthesis of the library of 22 new 3-methyl- and 3-ethyl-3-methyl-2,5-dioxo-pyrrolidin-1-yl-acetamides as potential anticonvulsant agents. The maximal electroshock (MES) and the subcutaneous pentylenetetrazole (scPTZ) seizure models were used for screening all the compounds. The 6Hz model of pharmacoresistant limbic seizures was applied for studying selected derivatives. Six...

article

New hybrid molecules with anticonvulsant and antinociceptive activity derived from 3-methyl- or 3,3-dimethyl-1-[1-oxo-1-(4-phenylpiperazin-1-yl)propan-2-yl]pyrrolidine-2,5-diones

Krzysztof Kamiński, Mirosław Zagaja, Anna Rapacz, Jarogniew J. Łuszczki, more

Bioorganic & Medicinal Chemistry > 2016 > 24 > 4 > 606-618

The purpose of this study was to synthetize the focused library of 34 new piperazinamides of 3-methyl- and 3,3-dimethyl-(2,5-dioxopyrrolidin-1-yl)propanoic or butanoic acids as potential new hybrid anticonvulsants. These hybrid molecules join the chemical fragments of well-known antiepileptic drugs (AEDs) such as ethosuximide, levetiracetam, and lacosamide. Compounds 5–38 were prepared in a coupling...

article

Evaluation of anticonvulsant and antinociceptive properties of new N-Mannich bases derived from pyrrolidine-2,5-dione and 3-methylpyrrolidine-2,5-dione

Anna Rapacz, Sabina Rybka, Jolanta Obniska, Kinga Sałat, more

Naunyn-Schmiedeberg's Archives of Pharmacology > 2016 > 389 > 3 > 339-348

The aim of the present experiments was to examine anticonvulsant activity of new pyrrolidine-2,5-dione and 3-methylpyrrolidine-2,5-dione derivatives in animal models of epilepsy. In addition, the possible collateral antinociceptive activity was assessed. Anticonvulsant activity was investigated in the electroconvulsive threshold (MEST) test and the pilocarpine-induced seizure models in mice. Antinociceptive...

article

Cardiovascular activity of the chiral xanthone derivatives

Natalia Szkaradek, Anna Rapacz, Karolina Pytka, Barbara Filipek, more

Bioorganic & Medicinal Chemistry > 2015 > 23 > 20 > 6714-6724

A series of 6 derivatives of xanthone were synthesized and evaluated for cardiovascular activity. The following pharmacological experiments were conducted: the binding affinity for adrenoceptors, the influence on the normal electrocardiogram, the effect on the arterial blood pressure, the effect on blood pressor response and prophylactic antiarrhythmic activity in adrenaline induced model of arrhythmia...

article

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...

article

Design, synthesis and biological activity of new amides derived from 3-methyl-3-phenyl-2,5-dioxo-pyrrolidin-1-yl-acetic acid

Jolanta Obniska, Anna Rapacz, Sabina Rybka, Beata Powroźnik, more

European Journal of Medicinal Chemistry > 2015 > 102 > C > 14-25

A series of new 3-methyl-3-phenyl-2,5-dioxo-pyrrolidin-1-yl-acetamides (6–23) has been synthesized and evaluated for their anticonvulsant activity in the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) seizure tests after intraperitoneal injection in mice. The acute neurological toxicity was determined using the rotarod test. The in vivo preliminary pharmacological results showed...

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Keywords

ANTICONVULSANT ACTIVITY (12)
IN VIVO STUDIES (7)
PYRROLIDINE-2,5-DIONE (6)
ANTIARRHYTHMIC (4)
HYBRID COMPOUNDS (4)
IN VITRO STUDIES (4)
EPILEPSY (3)
HYPOTENSIVE (3)
XANTHONE (3)
5-HT1A RECEPTOR ANTAGONIST (2)
ANTICONVULSANT (2)
ANTIDEPRESSANT-LIKE ACTIVITY (2)
ANTINOCICEPTIVE PROPERTIES (2)
FORMALIN (2)
HORSE (2)
MICE (2)
MUTAGENICITY AND ANTIMUTAGENICITY STUDIES (2)
NEUROPATHIC PAIN (2)
OXALIPLATIN (2)
RETAINED PLACENTA (2)
SUCCINIMIDE (2)
SUCCINIMIDES (2)
SYNTHESIS (2)
XANTHONES (2)
(2‐METHOXYPHENYL)PIPERAZINE (1)
4-AMINOBUTANAMIDES (1)
5-DIONE (1)
5-HT1A RECEPTOR (1)
5-HT2 RECEPTOR (1)
5-HT3 RECEPTOR ANTAGONIST (1)
5-HT7 RECEPTOR ANTAGONIST (1)
5‐HT (1)
6-HZ (1)
ADME‐TOX PROPERTIES (1)
ADRENOCEPTOR (1)
ADRENOCEPTOR BINDING AFFINITY (1)
AMIDES (1)
AMINOALKANOL (1)
ANALGESIC ACTIVITY (1)
ANESTHETIC ACTIVITY (1)
ANTIARRHYTHMIC, HYPOTENSIVE AND ANTICONVULSIVE ACTIVITIES (1)
ANTIDEPRESSANT‐LIKE ACTIVITY (1)
ANTINOCICEPTIVE (1)
ANTINOCICEPTIVE ACTIVITY (1)
APOPTOSIS (1)
BINDING STUDIES (1)
BIOAVAILABILITY (1)
CHIMNEY TEST (1)
CINNAMAMIDE (1)
CRYSTAL STRUCTURE (1)
DEPRESSION (1)
DISTRIBUTION IN BRAIN (1)
DRUG DEVELOPMENT (1)
ELECTROPHYSIOLOGY (1)
FORCED SWIM TEST (1)
GABA UPTAKE INHIBITORS (1)
HISTOPATHOLOGY (1)
HOT PLATE (1)
IMIDES (1)
IN VIVO AND IN VITRO STUDIES (1)
ION CHANNEL BINDING (1)
ION CHANNELS (1)
ION CHANNELS BINDING (1)
ISCHEMIA (1)
LACOSAMIDE (1)
LOCOMOTOR TEST (1)
MANNICH BASES (1)
MARES (1)
MASS SPECTROMETRY (1)
MES (1)
MES TEST (1)
METABOLIC STABILITY (1)
MGAT1–4 (1)
MOTOR COORDINATION (1)
MULTITARGETED ANTICONVULSANT (1)
N-MANNICH BASES (1)
NEUROTOXICITY (1)
PAIN (1)
PHARMACOPHORE (1)
PHARMACORESISTANCE (1)
PIPERAZINE DERIVATIVES (1)
PLACENTAL RETENTION (1)
PROLIFERATION (1)
PROTEOMICS (1)
PSYCHOMOTOR SEIZURES (1)
PYRROLIDINE-2 (1)
PYRROLIDINE‐2,5‐DIONE (1)
RADIOLIGAND-BINDING ASSAY (1)
REPERFUSION (1)
RETAINED FETAL MEMBRANES (1)
ROTAROD (1)
SCPTZ (1)
SCPTZ TEST (1)
SEIZURE THRESHOLD (1)
SEIZURES (1)
SIGMA‐1 RECEPTOR (1)
SIGMA‐2 RECEPTOR (1)
SIX-HERTZ (6HZ) TEST (1)
SMOOTH MUSCLE RELAXATION (1)
SUICIDE (1)
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Springer (2)
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INFONA - science communication portal

Search results for: Anna Rapacz

Promising anticonvulsant and/or analgesic compounds among 5‐chloro‐2‐ or 5‐chloro‐4‐methyl derivatives of xanthone coupled to aminoalkanol moieties—Design, synthesis and pharmacological evaluation

Synthesis, anticonvulsant, and antinociceptive activity of new 3‐(3‐methyl‐2,5‐dioxo‐3‐phenylpyrrolidin‐1‐yl)propanamides and 3‐phenyl‐butanamides

KA‐104, a new multitargeted anticonvulsant with potent antinociceptive activity in preclinical models

The preliminary studies on protein profile in retained and not retained foetal membranes in heavy draft mares

ADVANCES AND LIMITATIONS IN PHARMACOTHERAPY OF EPILEPSY

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

Synthesis and Anticonvulsant Properties of New 3,3‐Diphenyl‐2,5‐dioxo‐pyrrolidin‐1‐yl‐acetamides and 3,3‐Diphenyl‐propionamides

Synthesis and evaluation of anticonvulsant properties of new N-Mannich bases derived from pyrrolidine-2,5-dione and its 3-methyl-, 3-isopropyl, and 3-benzhydryl analogs

Analgesic, antiallodynic, and anticonvulsant activity of novel hybrid molecules derived from N-benzyl-2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2,5-dioxopyrrolidin-1-yl)butanamide in animal models of pain and epilepsy

Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH3 or 2-CH3

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

Design, synthesis and anticonvulsant activity of new hybrid compounds derived from N-phenyl-2-(2,5-dioxopyrrolidin-1-yl)-propanamides and -butanamides

Anticonvulsant and antinociceptive activity of new amides derived from 3-phenyl-2,5-dioxo-pyrrolidine-1-yl-acetic acid in mice

Synthesis and evaluation of anticonvulsant properties of new N-Mannich bases derived from 3-(1-phenylethyl)- and 3-benzyl-pyrrolidine-2,5-dione

Synthesis, and anticonvulsant activity of new amides derived from 3-methyl- or 3-ethyl-3-methyl-2,5-dioxo-pyrrolidin-1-yl-acetic acids

New hybrid molecules with anticonvulsant and antinociceptive activity derived from 3-methyl- or 3,3-dimethyl-1-[1-oxo-1-(4-phenylpiperazin-1-yl)propan-2-yl]pyrrolidine-2,5-diones

Evaluation of anticonvulsant and antinociceptive properties of new N-Mannich bases derived from pyrrolidine-2,5-dione and 3-methylpyrrolidine-2,5-dione

Cardiovascular activity of the chiral xanthone derivatives

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

Design, synthesis and biological activity of new amides derived from 3-methyl-3-phenyl-2,5-dioxo-pyrrolidin-1-yl-acetic acid

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