Piperazines

Publication Title: 
Cell Death & Disease

Overexpression of Bcl-2 contributes to resistance of cancer cells to human cytotoxic lymphocytes (CL) by blocking granzyme B (GraB)-induced mitochondrial outer membrane permeabilization (MOMP). Drugs that neutralise Bcl-2 (e.g., ABT-737) may therefore be effective adjuvants for immunotherapeutic strategies that use CL to kill cancer cells. Consistent with this we found that ABT-737 effectively restored MOMP in Bcl-2 overexpressing cells treated with GraB or natural killer cells.

Author(s): 
Sutton, V. R.
Sedelies, K.
Dewson, G.
Christensen, M. E.
Bird, P. I.
Johnstone, R. W.
Kluck, R. M.
Trapani, J. A.
Waterhouse, N. J.
Publication Title: 
Neuroscience Letters

Blonanserin is a second-generation antipsychotic drug for schizophrenia. The pharmacological actions of blonanserin are shown to be the antagonism of dopamine receptor 2 and serotonin receptors. However, its molecular mechanisms in brain cells have not been fully characterized. Accumulating evidence suggests that antipsychotic drugs and mood stabilizers show epigenetic effects on a wide range of genes in animal and cellular models. We performed genome-wide DNA methylation analysis targeting 479,814 CpG sites of cultured human neuroblastoma cells administered with blonanserin.

Author(s): 
Murata, Yui
Nishioka, Masaki
Bundo, Miki
Sunaga, Fumiko
Kasai, Kiyoto
Iwamoto, Kazuya
Publication Title: 
Archives Internationales De Pharmacodynamie Et De Thérapie

The interaction of four imidazole antimycotics clotrimazole, econazole, ketoconazole and miconazole with other drugs was studied in in vivo models known to reveal inhibition and induction of microsomal enzymes. In rats the duration of methohexital hypnosis and the prothrombin time prolongation induced by acenocoumarol were changed after oral administration of all four antimycotics. The oral ED50-values of miconazole, econazole and clotrimazole for prolongation of methohexital hypnosis in female rats (acute inhibiton of microsomal enzymes) were 3.55, 3.56 and 10.7 mg/kg.

Author(s): 
Niemegeers, C. J.
Levron, J. C.
Awouters, F.
Janssen, P. A.
Publication Title: 
Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica

The effect of oxatomide, an antiallergic drug, on the central and peripheral nervous systems were investigated, and the following results were obtained: Oxatomide at oral doses of 30-100 mg/kg produced little or no effect on the spontaneous and cooperative movements in mice, hexobarbital-induced hypnosis in mice, body temperature in rats, and did not induce muscle relaxation, the analgesic effect, anticonvulsive effects and anti-physostigmine effect. Oxatomide at doses of 300 mg/kg or more produced sedation followed by an increase in the responses to stimuli in mice and rats.

Author(s): 
Ohmori, K.
Ishii, H.
Shuto, K.
Nakamizo, N.
Publication Title: 
Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica

The effects of 1-[2-[bis (4-fluorophenyl)methoxy]ethyl]-4-(3- phenylpropyl) piperazine dihydrochloride (I-893) on the central nervous system were behaviorally and electroencephalographically investigated. Intraperitoneally injected I-893 (5-10 mg/kg) dose-dependently increased spontaneous motor activity in mice, but repeated injections did not affect the increase in the locomotor activity. In reserpinized mice, spontaneous motor activity was not increased by oral I-893.

Author(s): 
Nagase, T.
Hotta, K.
Morita, S.
Sakai, K.
Yamane, M.
Omote, M.
Mizusawa, H.
Publication Title: 
Naunyn-Schmiedeberg's Archives of Pharmacology

DM235 (sunifiram), a new compound structurally related to piracetam, prevented the amnesia induced by scopolamine (1.5 mg kg(-1) i.p.), after intraperitoneal (0.001-0.1 mg kg(-1)) or oral (0.01-0.1 mg kg(-1)) administration, as shown by a passive avoidance test in mice. The antiamnesic effect of DM235 was comparable to that of well-known nootropic drugs such as piracetam (30-100 mg kg(-1) i.p.), aniracetam (100 mg kg(-1) p.o.) or rolipram (30 mg kg(-1) p.o.).

Author(s): 
Ghelardini, C.
Galeotti, N.
Gualtieri, F.
Romanelli, M. N.
Bucherelli, C.
Baldi, E.
Bartolini, A.
Publication Title: 
CNS neuroscience & therapeutics

OBJECTIVES: To evaluate hypnosedative action of Zopiclone by using animal models for hypnosis and sedation (anxiolysis); and to further evaluate whether this hypnosedation impairs memory-learning in albino mice like conventional hypnosedatives. METHODS: For evaluation of hypnosedation, following experiments were performed in albino mice: (1) righting reflex test, (2) pentobarbitone sleeping time potentiation, (3) open field apparatus behavior, and (4) elevated plus maze performance.

Author(s): 
Kadam, Uma
Bhosale, Anand
Publication Title: 
The Journal of Infectious Diseases

The increasing spread of drug-resistant malaria strains underscores the need for new antimalarial agents with novel modes of action (MOAs). Here, we describe a compound representative of a new class of antimalarials. This molecule, ACT-213615, potently inhibits in vitro erythrocytic growth of all tested Plasmodium falciparum strains, irrespective of their drug resistance properties, with half-maximal inhibitory concentration (IC(50)) values in the low single-digit nanomolar range.

Author(s): 
Brunner, Ralf
Aissaoui, Hamed
Boss, Christoph
Bozdech, Zbynek
Brun, Reto
Corminboeuf, Olivier
Delahaye, Stephane
Fischli, Christoph
Heidmann, Bibia
Kaiser, Marcel
Kamber, Jolanda
Meyer, Solange
Papastogiannidis, Petros
Siegrist, Romain
Voss, Till
Welford, Richard
Wittlin, Sergio
Binkert, Christoph
Publication Title: 
Antimicrobial Agents and Chemotherapy

Neurocysticercosis (NCC), an infection of the brain with the larval stage of the Taenia solium tapeworm, is responsible for an estimated one-third of adult-onset epilepsy cases in regions of the world where it is endemic. Currently, anthelmintic drugs used for treatment of NCC are only partially effective, and there is, therefore, a pressing need for new therapeutic agents. Discovery of new anthelmintics with activity against T. solium has been limited by the lack of suitable sensitive assays that allow high-throughput screening.

Author(s): 
Mahanty, Siddhartha
Madrid, Elise M.
Nash, Theodore E.
Publication Title: 
Journal of Pharmaceutical and Biomedical Analysis

Ayurvedic/herbal healthcare products are considered safe under the impression that they are derived from natural products. But recently, there have been several reports worldwide on the adulteration of synthetic PDE-5 inhibitors in aphrodisiac herbal formulations. Therefore, the objective of the present study was to explore the presence of synthetic PDE-5 inhibitors (sildenafil, tadalafil and/or vardenafil) in ayurvedic/herbal healthcare products sold in Indian market for aphrodisiac/related uses. In total, 85 herbal formulations (HFs) were included in the study.

Author(s): 
Savaliya, Akash A.
Shah, Ravi P.
Prasad, Bhagwat
Singh, Saranjit

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