9 research outputs found
New arylpiperazine derivatives with antidepressant-like activity containing isonicotinic and picolinic nuclei: evidence for serotonergic system involvement
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ANTINOCICEPTIVE AND ANTIANXIETY ACTIVITY OF HYDROETHANOLIC EXTRACTS OF THREE IMPATIENS SPECIES IN MICE
The plants of the Impatiens L. (Balsaminaceae) have been used for a long time in folk medicine in different painful conditions, and to treat rheumatism, isthmus and crural aches, fractures, superficial infections, fingernail inflammation. This study was undertaken to determine the pharmacological profile of hydroethanolic extracts from Impatiens glandulifera, I. noli-tangere and I. parviflora. A range of behavioral assessments was applied to evaluate the effects of obtained extracts i.e. measurement of body temperature, tests of locomotor activity and motor coordination, nociceptive reaction and anxiety-like behavior. Hydroethanolic extracts were analyzed for total polyphenol (TPC), flavonoid (TFC), flavones/flavonols (TFFC), and flavonones/dihydroflavonols (TFDC) content. Our results show that the extracts from Impatiens species contain high levels of TPC, TFC, TFFC, and TFDC. Oral (i.e., by gavage) administration of Impatiens L. extracts (except for I. noli-tangere) presented an antinociceptive or/and anti-inflammatory activity in the writhing test. The antinociceptive effect of I. parviflora leaves (100 mg/kg) and I. glandulifera flowers (100 mg/kg) was reversed by naloxone. I. glandulifera flowers and roots extracts (100 mg/kg) increased the reaction time to the thermal stimulus in the hot-plate test. All extracts from I. glandulifera (100 mg/kg) showed antianxiety effect in the elevated plus-maze test. It is worth noting that none of the extracts, at the highest used dose – 0.1 ED50 (200 mg/kg), caused coordination impairments or myorelaxation as measured in the rota-rod and chimney tests. These results seem to suggest that the tested extracts are not neurotoxic
New Atypical Antipsychotics in the Treatment of Schizophrenia and Depression
Schizophrenia and depression are heterogeneous disorders. The complex pathomechanism of the diseases imply that medication responses vary across patients. Many psychotropic drugs are available but achieving optimal therapeutic effect can be challenging. The evidence correlates well with clinical observations, suggesting that new atypical antipsychotic drugs are effective against negative and cognitive symptoms of schizophrenia, as well as against affective symptoms observed in depression. The purpose of this review presents the background and evidence for the use of the new second/third-generation antipsychotics (aripiprazole, cariprazine, lurasidone, asenapine, brexpiprazole, lumateperone, pimavanserin) in treatment of schizophrenia and depression. We have first provided a brief overview of the major neurobiological underpinnings of schizophrenia and depression. We then shortly discuss efficacy, safety and limitations of ongoing pharmacotherapy used in depression and schizophrenia. Mainly, we have focused this review on the therapeutic potential of new atypical antipsychotic drugs—currently existing—to be effective in psychotic, as well as in affective disorders
Currently used anorexic drugs in the pharmacotherapy of obesity
W przedstawionej pracy dokonano przeglądu leków anorektycznych działających ośrodkowo poprzez hamowanie uczucia głodu i wykorzystywanych do farmakologicznego leczenia otyłości. Omówiono problem otyłości jako choroby cywilizacyjnej, która dotyka coraz więcej osób na świecie. Opisano prawdopodobne przyczyny takiego stanu rzeczy, skutki zdrowotne oraz wskazania do farmakoterapii ze zwróceniem szczególnej uwagi na mechanizm odczuwania głodu i sytości. Zaprezentowano preparaty dostępne zarówno na terenie Stanów Zjednoczonych, jak i w Unii Europejskiej. Skupiono się na przybliżeniu mechanizmów ich działania, skutków ubocznych, oraz efektach terapeutycznych uzyskanych z przeprowadzonych badań. Uwzględniono również leki stosowane w przeszłości, wyjaśniając dlaczego zostały wycofane z obrotu.The presented study reviews the possibilities of pharmacological obesity treatment through the use of anorectic drugs - acting on the central nervous system by reducing appetite. The problem of obesity as a civilization disease that affects more and more people in the world was discussed. The likely causes of such a state of affairs, health effects and indications for pharmacotherapy have been described, paying particular attention to the mechanism of feeling hungry and satiety. Preparations available both in the United States and in the European Union were presented. The focus was on the mechanism of their action, therapeutic effects resulting from the research and side effects. Medicines used in the past are also included, explaining why they were withdrawn from the market
Synthesis and Pharmacological Evaluation of Novel 1-(1,4-Alkylaryldisubstituted-4,5-dihydro-1H-imidazo)-3-substituted Urea Derivatives
Novel 1-(1,4-alkylaryldisubstituted-4,5-dihydro-1H-imidazo)-3-substituted urea derivatives have been synthesized and evaluated for their central nervous system activity. Compounds 3a–m were prepared in the reaction between the respective 1-alkyl-4-aryl-4,5-dihydro-1H-imidazol-2-amines 1a–c and appropriate isocyanates 2 in dichloromethane. The compounds were subjected to in silico ADMET studies in order to select best candidates for in vivo experiments. The effects of the compounds on the spontaneous locomotor activity and amphetamine-evoked hyperactivity were estimated. Analgesic activity, without or in the presence of naloxone, was assessed in the writhing test. The tendency to change the HTR, evoked by l-5-HTP and the involvement in alteration in body temperature in mice was studied. Additionally, to check possible occurrence of drug-induced changes in the muscle relaxant activity of mice, which may have contributed to their behaviour in other tests, the rota-rod and chimney tests were performed. The new urea derivatives exerted significant activities in the performed pharmacological tests, although the presented results show a preliminary estimation, and thus, need to be extended for identification and understanding the complete pharmacological profile of the examined compounds