P-4-71 Efficacy and safety of sertindole in two double-blind, placebo-controlled trials of schizophrenic patients

Perspectives on the role of serotonergic mechanisms in the pharmacology of schizophrenia

“…The literature in this area is currently expanding, as further information is being gathered from large-scale clinical studies investigating the effects of novel, potent 5-HT2 blocking antipsychotics (Targum et al, 1995;Link et al, 1995;Beasley et al, 1996;van Kammen et al, 1996). We predict that the integration of these data with functional imaging and molecular pharmacological studies will consolidate the role of 5-HT2 receptors as a crucial site of therapeutic activity in schizophrenia.…”

Ethyl 2,6-bis(4-chlorophenyl)-4-(4-fluoroanilino)-1-(4-fluorophenyl)-1,2,5,6-tetrahydropyridine-3-carboxylate

“…For the biological activity of functionalized piperidine derivatives, see: Zhou et al (2007); Misra et al (2009); Bin et al (2001); Agrawal & Somani (2009); Dekus et al (2007). For general applications of densely functionalized piperidines, see: Targum et al (1995); Schotte et al (1996). For general background to functionalized piperidiones, see: Desai et al (1992); Pinder (1992); Watson et al (2000); Breman et al (2001); Kamei et al (2005).…”

“…Functionalized piperidines are found to constitute a very important core in numerous natural products (Desai et al, 1992;Pinder, 1992), synthetic pharmaceuticals (Breman et al, 2001;Watson et al, 2000), and a wide variety of biologically active compounds. In particular, 1,4-disubstituted piperidine scaffolds find useful applications as established drugs (Targum et al, 1995;Schotte et al,1996), and they exhibit a wide range of pharmacological activities including antibacterial (Zhou et al, 2007), antimalarial (Misra et al, 2009), anticonvulsant, anti-inflammatory (Bin et al, 2001), and enzyme inhibitory activity (Agrawal & Somani, 2009;Dekus et al, 2007). Moreover a large number of compounds bearing piperidine scaffold have entered into preclinical and clinical trials over the last few years (Kamei et al, 2005).…”

In vitro evaluation and in silico screening of synthetic acetylcholinesterase inhibitors bearing functionalized piperidine pharmacophores

“…4 A large number of compounds bearing piperidine scaffold have entered into preclinical and clinical trials over the last few years. 5 In particular, 1,4-disubstituted piperidine scaffolds find useful applications as established drugs such as donepezil (Aricept ® , an acetylcholinesterase inhibitor in the treatment of Alzheimer's disease), naratriptan (Naramig ® , an agonist of 5-hydroxytryptamine (serotonin) receptor 1D and 5-hydroxytryptamine receptor 1B in the treatment of migraine headaches), risperidone (Risperdal ® ) and sertindole (Serdolect ® ) (both nonselective 5-hydroxytryptamine receptor 2A/dopamine D 2 receptor (5-HT/D 2 ) antagonists, currently in the treatment of schizophrenia), 6,7 and exhibit anti-hypertensive, 8 antibacterial, 9 antimalarial, 10 anticonvulsant, and anti-inflammatory activities. 11 Moreover, some of them have been found to possess enzyme inhibitory activity against farnesyl transferase (FTase is believed to play an important role in development of progeria and various forms of cancers) 10 or dihydroorotate dehydrogenase (DHODH) 5 and also found to be useful in Parkinson's disease involving the MAO-based mechanism.…”