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Aplicação da catálise de trasnferência de fase na avaliação de rotas alternativas para obtenção industrial da dicicloverina caramifeno e amiodarona; The use of phase transfer catalysis, in the development of alternative routes for industrial production of dicycloverine, caramiphen and amiodarone

Polakiewicz, Bronislaw
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Tese de Doutorado Formato: application/pdf
Publicado em 20/12/1994 Português
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38.41%
O emprego da catálise de transferência de fase substituindo uma ou mais etapas da síntese de um fármaco, pode ser um recurso vantajoso sob o ponto de vista tecnológico. Empregado na síntese de importantes fármacos que são a dicicloverina, caramifeno eamiodarona, a catálise de transferência de fase revelou-se muito vantajosa na síntese dos dois primeiros. A dicicloverina e o caramifeno tiveram as suas rotas de obtenção verticalizadas, com bons resultados e custos bem mais baixos quando comparados com os atualmente adquiridos no exterior. Ficou evidente que a catálise de transferência de fase pode ser aplicada com sucesso na produção destes e outros fármacos em associação com técnicas já conhecidas com ótimos resultados.; The phase transfer catalysis application replacing one or more steps in the drug synthesis, can be of advantage in the technologycal approach. Applied to the synthesis of important drugs such as diciclomine, caramiphen,and amiodarone, the phase transfer catalysis resulted in a very advantageous method in the first two drugs. The diciclomine and the caramiphen, gets their obtention routes from raw materiaIs wi th good resul ts and low coasts, when compared wi th the drugs presently purchassed in foreign countries. It is clear that the phase transfer catalysis...

The anticonvulsant actions of σ receptor ligands in the Mg2+-free model of epileptiform activity in rat hippocampal slices

Thurgur, Claire; Church, John
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /07/1998 Português
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18.69%
The anticonvulsant potency of a series of structurally-dissimilar compounds which possess nanomolar affinities for high-affinity σ binding sites was examined in the Mg2+-free model of epileptiform activity in rat hippocampal slices. Extracellular field potential recordings in the CA1 region were employed to examine the effects of test compounds on spontaneous epileptiform activity and multiple population spikes evoked by stimulation of the Schaffer collateral-commissural pathway.Applied at σ site-selective (i.e. nanomolar) concentrations, dextromethorphan, ditolylguanidine, caramiphen and opipramol failed to modify Mg2+-free epileptiform activity; neither pro- nor anticonvulsant effects were observed. However, applied at micromolar concentrations, these and additional test compounds reversibly inhibited orthodromically-evoked epileptiform field potentials with a rank order potency (IC50 values in μM): dextrorphan (1.5)>ifenprodil (6.3)>dextromethorphan (10)>ditolylguanidine (15)>loperamide (28)>carbetapentane (38)>caramiphen (46)>opipramol (52). Micromolar concentrations of the same compounds also inhibited spontaneous epileptiform bursts recorded during perfusion with Mg2+-free medium.Co-application of ropizine (10 μM), an allosteric modulator of dextromethorphan binding to high-affinity σ receptors...

The protective actions of some anticholinergic drugs in sarin poisoning

Brimblecombe, R. W.; Green, D. M.; Stratton, June A.; Thompson, Pamela B. J.
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /08/1970 Português
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17.01%
1. The central and peripheral anticholinergic activities of a series of drugs comprising atropine, hyoscine, caramiphen and one of its analogues, and three glycollic acid esters, have been measured.

Blockade by sigma site ligands of N-methyl-D-aspartate-evoked responses in rat and mouse cultured hippocampal pyramidal neurones.

Fletcher, E. J.; Church, J.; Abdel-Hamid, K.; MacDonald, J. F.
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /12/1995 Português
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17.01%
1. The effects of a range of structurally-dissimilar compounds which possess affinity for sigma binding sites were examined on the responses of cultured hippocampal pyramidal neurones to the excitatory amino acid analogues N-methyl-D-aspartate (NMDA), kainate and (RS)-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA). 2. In mouse hippocampal neurones under whole-cell voltage-clamp, the compounds tested reversibly attenuated NMDA-, but not kainate- or AMPA-, evoked currents with a rank order potency (IC50 values in microM): ifenprodil (0.8) > (+)-N-allylnormetazocine (1.1) > dextromethorphan (1.8) = haloperidol (1.9) > (+)-pentazocine (7.2) > 1S,2R-(-)-cis-N-methyl-N-[2-(3, 4-dichlorophenyl) ethyl]-2-(1-pyrrolidinyl)cyclohexylamine (17) = rimcazole (18) > 1,3-di(2-tolyl)guanidine (37) > opipramol (96) > caramiphen (110) = carbetapentane (112) > > (+)-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine (485). 3. The attenuation of NMDA-evoked responses was not mediated through interactions with the agonist, glycine (except haloperidol) or polyamine (except ifenprodil) binding sites on the NMDA receptor-channel complex but, in the light of the voltage- and, in some cases, use-dependent nature of their antagonism, an interaction with the ion channel appears to be a likely mechanism of action for many of the compounds. 4. Micromolar concentrations of selected sigma site ligands also reduced NMDA-evoked rises in intracellular free calcium concentration in Fura-2-loaded cultured hippocampal neurones of the rat with the same rank order potency as observed in the electrophysiological studies. 5. The data indicate that...

Blockade by sigma site ligands of high voltage-activated Ca2+ channels in rat and mouse cultured hippocampal pyramidal neurones.

Church, J.; Fletcher, E. J.
Fonte: PubMed Publicador: PubMed
Tipo: Artigo de Revista Científica
Publicado em /12/1995 Português
Relevância na Pesquisa
17.77%
1. The effects of a series of structurally-dissimilar sigma site ligands were examined on high voltage-activated Ca2+ channel activity in two preparations of cultured hippocampal pyramidal neurones. 2. In mouse hippocampal neurones under whole-cell voltage-clamp, voltage-activated Ca2+ channel currents carried by barium ions (IBa) were reduced with the rank order (IC50 values in microM): 1S,2R-(-)-cis-N-methyl-N-[2-(3,4-dichlorophenyl)ethyl]- 2-(1-pyrrolidinyl)cyclohexylamine (7.8) > rimcazole (13) > haloperidol (16) > ifenprodil (18) > opipramol (32) > carbetapentane (40) = 1-benzylspiro[1,2,3,4-tetrahydronaphthalene-1,4-piperidine] (42) > caramiphen (47) > dextromethorphan (73). At the highest concentrations tested, the compounds almost abolished IBa in the absence of any other pharmacological agent. 3. The current-voltage characteristics of the whole-cell IBa were unaffected by the test compounds. The drug-induced block was rapid in onset and offset, with the exceptions of carbetapentane and caramiphen where full block was achieved only after two to three voltage-activated currents and was associated with an apparent increase in the rate of inactivation of IBa. 4. In rat hippocampal neurones loaded with the Ca(2+)-sensitive dye Fura-2...

Neuroprotective efficacy of caramiphen against soman and mechanisms of its action

Figueiredo, TH; Aroniadou-Anderjaska, V; Qashu, F; Apland, JP; Pidoplichko, V; Stevens, D; Ferrara, TM; Braga, MFM
Fonte: Blackwell Publishing Ltd Publicador: Blackwell Publishing Ltd
Tipo: Artigo de Revista Científica
Publicado em /11/2011 Português
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17.01%