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991.
992.
Karolina Pytka Anna Partyka Magdalena Jastrz?bska-Wi?sek Agata Siwek Monika G?uch-Lutwin Barbara Mordyl Grzegorz Kazek Anna Rapacz Adrian Olczyk Adam Ga?uszka Marian B?achuta Anna Waszkielewicz Henryk Marona Jacek Sapa Barbara Filipek Anna Weso?owska 《PloS one》2015,10(11)
The aim of this study was to further characterize pharmacological properties of two phenylpiperazine derivatives: 1-{2-[2-(2,6-dimethlphenoxy)ethoxy]ethyl}-4-(2-methoxyphenyl)piperazynine hydrochloride (HBK-14) and 2-[2-(2-chloro-6-methylphenoxy)ethoxy]ethyl-4-(2- methoxyphenyl)piperazynine dihydrochloride (HBK-15) in radioligand binding and functional in vitro assays as well as in vivo models. Antidepressant-like properties were investigated in the forced swim test (FST) in mice and rats. Anxiolytic-like activity was evaluated in the four-plate test in mice and elevated plus maze test (EPM) in rats. Imipramine and escitalopram were used as reference drugs in the FST, and diazepam was used as a standard anxiolytic drug in animal models of anxiety. Our results indicate that HBK-14 and HBK-15 possess high or moderate affinity for serotonergic 5-HT2, adrenergic α1, and dopaminergic D2 receptors as well as being full 5-HT1A and 5-HT7 receptor antagonists. We also present their potent antidepressant-like activity (HBK-14—FST mice: 2.5 and 5 mg/kg; FST rats: 5 mg/kg) and (HBK-15—FST mice: 1.25, 2.5 and 5 mg/kg; FST rats: 1.25 and 2.5 mg/kg). We show that HBK-14 (four-plate test: 2.5 and 5 mg/kg; EPM: 2.5 mg/kg) and HBK-15 (four-plate test: 2.5 and 5 mg/kg; EPM: 5 mg/kg) possess anxiolytic-like properties. Among the two, HBK-15 has stronger antidepressant-like properties, and HBK-14 displays greater anxiolytic-like activity. Lastly, we demonstrate the involvement of serotonergic system, particularly 5-HT1A receptor, in the antidepressant- and anxiolytic-like actions of investigated compounds. 相似文献
993.
A prospective study of adolescent eating in the absence of hunger and body mass and fat mass outcomes 下载免费PDF全文
994.
995.
996.
The activities of monoamine and diamine oxidases in various organs and tissues and the amine levels in plasma and urine were determined in chronically uremic and pair-fed control rats. Plasma amine levels were elevated in uremic animals while the urinary excretion of amines was decreased. In uremic as compared to control animals, monomaine oxidase activity was decreased in kidney and muscle, increased in heart and plasma and not altered in liver and cerebrum. Diamine oxidase activity in uremic rats was decreased in kidney, increased in plasma and unchanged in liver and muscle. These alterations of amine oxidase activities in renal failure may affect the metabolism of many amines and thus contribute to the pathogenesis of the uremic syndrome. 相似文献
997.
Marian Stamp Dawkins 《Applied animal behaviour science》1988,20(3-4):209-225
A key issue in animal welfare is whether keeping animals in conditions where they cannot or do not perform behaviour typical of more naturally-kept members of their species causes them to suffer. Various measures have been used to resolve this issue. The cost an animal is prepared to pay for the opportunity to perform different behaviour can be used as a measure of the importance of that behaviour to the animal. Manipulation of time-budgets is the most reliable method of measuring such costs and of relating “deprivation” to “suffering”. 相似文献
998.
Marian Wiwart 《Mycotoxin Research》1987,3(1):17-20
The extend of physiological variability of five Isolates of Fusarium nivale /Fr./ Ces. using a tandem — crossed Immunoelectrophoresis was studied. In the homological reaction of antiserum antl-F. nivale fourteen precipiration lines were obtained. The variability of antigens originated from different isolates was found. The studied isolates showed differentiation In pathogenicity to three rye genotypes. 相似文献
999.
Chenyin Wang Laura Engelke David Bickel Alexandra Hamacher Marian Frank Peter Proksch Holger Gohlke Matthias U. Kassack 《Bioorganic & medicinal chemistry》2019,27(19):115044
Platinum compounds are the first-line therapy for many types of cancer. However, drug resistance has frequently been reported for and is a major limitation of platinum-based chemotherapy in the clinic. In the current study, we examined the anti-tumor activity of phomoxanthone A (PXA), a tetrahydroxanthone dimer isolated from the endophytic fungus Phomopsis longicolla, in several solid cancer cell lines and their cisplatin-resistant sub-cell lines. PXA showed strong cytotoxic effects with IC50 values in the high nanomolar or low micromolar range in MTT assays. IC50 values of PXA were lower than those of cisplatin. Remarkably, equipotent anti-cancer activity was found in cisplatin-sensitive and respective cisplatin-resistant cells. Anticancer effects of PXA were studied in further detail in ovarian cancer (A2780) and bladder cancer (J82) cell pairs. PXA led to rapid depolarization of the mitochondrial membrane potential and strong activation of caspase 3 and 7, eventually resulting in strong induction of apoptosis. These effects occurred again both in sensitive and resistant cell lines. IC50 values of PXA from MTT and mitochondrial membrane depolarization assays were in good agreement. Configurational free energy computations indicate that both the neutral and singly negatively charged PXA show membrane partitioning and can penetrate the inner mitochondrial membrane. PXA treatment did not damage the plasma membranes of cancer cells, thus excluding unspecific membrane effects. Further, PXA had neither an effect on intracellular ROS nor on reduction of ROS after hydrogen peroxide treatment. In conclusion, our studies present PXA as a natural compound with strong apoptotic anticancer effects against platinum-resistant solid cancers. This may open new treatment options in clinically resistant malignancies. 相似文献