RESUMO
Enantioselective synthesis and absolute configuration of (-)-1-(benzofuran-2-yl)-2-propylaminopentane ((-)-BPAP), which is a highly potent and selective catecholaminergic activity enhancer (CAE) substance, are described. The synthetic approach consists of the coupling reaction of benzofuran with (R)-N-tosyl-2-propylazirizine or (R)-N-methoxy-N-methylnorvaliamide, followed by appropriate modifications of the resulting coupling products. As the results, (-)-BPAP turned out to have the R configuration, which was finally confirmed by X-ray crystallographic analysis.
Assuntos
Azirinas/química , Benzofuranos/química , Benzofuranos/síntese química , Benzofuranos/farmacologia , Catecolaminas/agonistas , Benzofuranos/metabolismo , Catecolaminas/metabolismo , Cristalografia por Raios X , Conformação Molecular , Estrutura Molecular , EstereoisomerismoRESUMO
1. The rapid cell death of cortical neurons in serum-free culture was rescued by the condition medium from the high-density culture, but not by brain-derived neurotrophic factor or basic fibroblast growth factor. 2. Similar rescue was observed by the addition of (-)BPAP, an impulse enhancer, and (+)-pentazocine, a sigma receptor agonist. These actions were blocked by BD1063, a sigma receptor antagonist. 3. (-)BPAP showed a weak displacement activity in the [3H]pentazocine binding to synaptic membranes from rat cerebral cortex. 4. These findings suggest that (-)BPAP and (+)-pentazocine have unique survival activity on cortical neurons through sigma receptors.
Assuntos
Benzofuranos/farmacologia , Sobrevivência Celular/efeitos dos fármacos , Córtex Cerebral/citologia , Neurônios/citologia , Pentazocina/farmacologia , Receptores sigma/fisiologia , Animais , Células Cultivadas , Córtex Cerebral/fisiologia , Meios de Cultura Livres de Soro , Feto , Cinética , Neurônios/efeitos dos fármacos , Neurônios/fisiologia , Ratos , Ratos Wistar , Receptores sigma/agonistasRESUMO
Oligonucleotides of 5-fluoro-2'-deoxyuridine (FUdR) 1 and 5-fluorouridine (FUR) 2 have been prepared by the standard phosphoramidite method. Homo oligomers (24 mer) of 1, 2 and hetero oligomers of those will be described.