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[PMID]:19812350
[Au] Autor:Johansson T; Weidolf L; Popp F; Tacke R; Jurva U
[Ad] Endereço:Discovery DMPK, AstraZeneca Research and Development, SE-43183 Mölndal, Sweden. tovjoh@chem.gu.se
[Ti] Título:In vitro metabolism of haloperidol and sila-haloperidol: new metabolic pathways resulting from carbon/silicon exchange.
[So] Source:Drug Metab Dispos;38(1):73-83, 2010 Jan.
[Is] ISSN:1521-009X
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The neurotoxic side effects observed for the neuroleptic agent haloperidol have been associated with its pyridinium metabolite. In a previous study, a silicon analog of haloperidol (sila-haloperidol) was synthesized, which contains a silicon atom instead of the carbon atom in the 4-position of the piperidine ring. In the present study, the phase I metabolism of sila-haloperidol and haloperidol was studied in rat and human liver microsomes. The phase II metabolism was studied in rat, dog, and human hepatocytes and also in liver microsomes supplemented with UDP-glucuronic acid (UDPGA). A major metabolite of haloperidol, the pyridinium metabolite, was not formed in the microsomal incubations with sila-haloperidol. For sila-haloperidol, three metabolites originating from opening of the piperidine ring were observed, a mechanism that has not been observed for haloperidol. One of the significant phase II metabolites of haloperidol was the glucuronide of the hydroxy group bound to the piperidine ring. For sila-haloperidol, the analogous metabolite was not observed in the hepatocytes or in the liver microsomal incubations containing UDPGA. If silanol (SiOH) groups are not glucuronidated, introducing silanol groups in drug molecules could provide an opportunity to enhance the hydrophilicity without allowing for direct phase II metabolism. To provide further support for the observed differences in metabolic pathways between haloperidol and sila-haloperidol, the metabolism of another pair of C/Si analogs was studied, namely, trifluperidol and sila-trifluperidol. These studies showed the same differences in metabolic pathways as between sila-haloperidol and haloperidol.
[Mh] Termos MeSH primário: Haloperidol/análogos & derivados
Haloperidol/metabolismo
Desintoxicação Metabólica Fase II/fisiologia
Desentoxicação Metabólica Fase I/fisiologia
Compostos de Organossilício/metabolismo
[Mh] Termos MeSH secundário: Animais
Cromatografia Líquida
Cães
Feminino
Haloperidol/farmacocinética
Hepatócitos/metabolismo
Seres Humanos
Masculino
Microssomos Hepáticos/metabolismo
Modelos Químicos
Estrutura Molecular
Compostos de Organossilício/farmacocinética
Ratos
Espectrometria de Massas em Tandem
Trifluperidol/análogos & derivados
Trifluperidol/metabolismo
Trifluperidol/farmacocinética
Uridina Difosfato Ácido Glucurônico/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Organosilicon Compounds); 0 (sila-haloperidol); 2616-64-0 (Uridine Diphosphate Glucuronic Acid); J6292F8L3D (Haloperidol); R8869Q7R8I (Trifluperidol)
[Em] Mês de entrada:1003
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:091009
[St] Status:MEDLINE
[do] DOI:10.1124/dmd.109.028449


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[PMID]:15591644
[Au] Autor:Kowalski J; Labuzek K; Herman ZS
[Ad] Endereço:Department of Clinical Pharmacology, Medical University of Silesia, Medyków 18, PL 40-752 Katowice, Poland. farmklin@infomed.slam.katowice.pl
[Ti] Título:Flupentixol and trifluperidol reduce interleukin-1 beta and interleukin-2 release by rat mixed glial and microglial cell cultures.
[So] Source:Pol J Pharmacol;56(5):563-70, 2004 Sep-Oct.
[Is] ISSN:1230-6002
[Cp] País de publicação:Poland
[La] Idioma:eng
[Ab] Resumo:Neuroleptics penetrate into the brain, where they act not only on neurons but probably also on glial cells. In the available literature, there are no reports on the effect of neuroleptics on cytokine release in glia cultures. The aim of this study was to evaluate the effect of neuroleptics on the release of proinflammatory cytokines (IL-1beta and IL-2) by mixed glial and microglial cell cultures. Trifluperidol at 20 and 2 muM reduced IL-beta secretion by mixed glial cultures after 3 days of exposure. Trifluperidol at 20, 2 and 0.2 muM diminished IL-beta secretion after 1 day of incubation. Trifluperidol at 20 and 2 muM reduced IL-2 release after 1 and 3 days of exposure. Flupentixol at 20 and 2 muM reduced IL-1beta by mixed glial cell cultures after 3 days of exposure. Flupentixol at 20, 2 and 0.2 muM caused diminution of IL-1beta release after 1 day of exposure. Flupentixol at 20 and 2 muM reduced IL-2 release after 1 day of incubation. Flupentixol at 20, 2 and 0.2 muM diminished IL-2 release after 3 days of exposure. Flupentixol at 20, 10, 2 and 0.2 muM reduced IL-1beta release by microgial cell cultures. Flupentixol at 20, 10 and 2 muM reduced release of IL-2 by microglial cells after 1 day of exposure. The results of the present study suggest that neuroleptics have an inhibiting effect on the release of glial cytokines, but clinical significance this results remains to be elucidated.
[Mh] Termos MeSH primário: Flupentixol/farmacologia
Interleucina-1/secreção
Interleucina-2/secreção
Neuroglia/efeitos dos fármacos
Neuroglia/secreção
Trifluperidol/farmacologia
[Mh] Termos MeSH secundário: Animais
Células Cultivadas
Interleucina-1/antagonistas & inibidores
Interleucina-2/antagonistas & inibidores
Microglia/efeitos dos fármacos
Microglia/secreção
Ratos
Ratos Wistar
[Pt] Tipo de publicação:COMPARATIVE STUDY; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Interleukin-1); 0 (Interleukin-2); FA0UYH6QUO (Flupenthixol); R8869Q7R8I (Trifluperidol)
[Em] Mês de entrada:0507
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:041214
[St] Status:MEDLINE


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[PMID]:12620286
[Au] Autor:Kowalski J; Labuzek K; Herman ZS
[Ad] Endereço:Department of Clinical Pharmacology, Medical University of Silesia, 40-752 Katowice, 18, Medyków, Poland. farmklin@infomed.slam.katowice.pl
[Ti] Título:Flupentixol and trifluperidol reduce secretion of tumor necrosis factor-alpha and nitric oxide by rat microglial cells.
[So] Source:Neurochem Int;43(2):173-8, 2003 Jul.
[Is] ISSN:0197-0186
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Tumor necrosis factor-alpha (TNF-alpha) and nitric oxide (NO), both of which are produced by activated microglial cells, are involved in the neuropathogenesis of many diseases affecting the central nervous system (CNS). There is a need to develop drugs that inhibit neurotoxic processes in neurodegenerative diseases. The aim of this study was to evaluate the effect of two neuroleptics, flupentixol and trifluperidol, on the release of pro-apoptotic TNF-alpha and NO by LPS-activated rat microglial cells. Flupentixol and trifluperidol reduced the TNF-alpha and NO release by cultured microglia exposed to LPS for 6 and 24h. The results suggest that flupentixol and trifluperidol, which are well-known antipsychotic drugs, may be used in the treatment of CNS diseases associated with excessive TNF-alpha and NO release.
[Mh] Termos MeSH primário: Flupentixol/farmacologia
Neurônios/secreção
Óxido Nítrico/metabolismo
Trifluperidol/farmacologia
Fator de Necrose Tumoral alfa/secreção
[Mh] Termos MeSH secundário: Animais
Animais Recém-Nascidos
Encéfalo/efeitos dos fármacos
Encéfalo/fisiologia
Células Cultivadas
Neurônios/efeitos dos fármacos
Ratos
Ratos Wistar
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Tumor Necrosis Factor-alpha); 31C4KY9ESH (Nitric Oxide); FA0UYH6QUO (Flupenthixol); R8869Q7R8I (Trifluperidol)
[Em] Mês de entrada:0306
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:030307
[St] Status:MEDLINE


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[PMID]:10572345
[Au] Autor:Bischof F; Melms A; Fetter M
[Ad] Endereço:Department of Immunology, Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, the Netherlands.
[Ti] Título:Persistent cerebellar deterioration in a patient with lobar pneumonia under lithium, carbamazepine, and trifluperidol treatment.
[So] Source:Eur Psychiatry;14(3):175-6, 1999 Jun.
[Is] ISSN:0924-9338
[Cp] País de publicação:France
[La] Idioma:eng
[Ab] Resumo:We report on a patient with schizoaffective disorder who was on combination therapy of lithium, carbamazepine, and the neuroleptic trifluperidol. He experienced a lobar pneumonia and developed an acute and persistent cerebellar deterioration which was most likely due to lithium toxicity, while the serum lithium level was within the therapeutic range. The combination of lithium, carbamazepine, and neuroleptics is common, and is generally considered to be safe. The reported case suggests that this regimen might increase the risk of intoxication with potentially disabling side-effects.
[Mh] Termos MeSH primário: Antipsicóticos/efeitos adversos
Carbamazepina/efeitos adversos
Doenças Cerebelares/etiologia
Lítio/efeitos adversos
Pneumonia Pneumocócica/complicações
Pneumonia Pneumocócica/microbiologia
Transtornos Psicóticos/tratamento farmacológico
Trifluperidol/efeitos adversos
[Mh] Termos MeSH secundário: Antibacterianos/uso terapêutico
Progressão da Doença
Quimioterapia Combinada
Seres Humanos
Masculino
Meia-Idade
Pneumonia Pneumocócica/tratamento farmacológico
Índice de Gravidade de Doença
Infecções Estreptocócicas/complicações
Infecções Estreptocócicas/tratamento farmacológico
Resultado do Tratamento
[Pt] Tipo de publicação:CASE REPORTS; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Bacterial Agents); 0 (Antipsychotic Agents); 33CM23913M (Carbamazepine); 9FN79X2M3F (Lithium); R8869Q7R8I (Trifluperidol)
[Em] Mês de entrada:0005
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:991126
[St] Status:MEDLINE


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[PMID]:9247064
[Au] Autor:Wible B; Murawsky MK; Crumb WJ; Rampe D
[Ad] Endereço:Hoechst Marion Roussel, Inc., Cincinnati, OH 45215, USA.
[Ti] Título:Stable expression and characterization of the human brain potassium channel Kv2.1: blockade by antipsychotic agents.
[So] Source:Brain Res;761(1):42-50, 1997 Jun 27.
[Is] ISSN:0006-8993
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:We have cloned the cDNA encoding the voltage-dependent K+ channel Kv2.1 from human brain (hKv2.1). RNase protection and RT-PCR (reverse transcriptase-PCR) experiments reveal abundant Kv2.1 transcripts in human brain with virtually no expression detectable in human heart. hKv2.1 has been stably transfected into a human glioblastoma cell line, and transformed cells display large, slowly activating outward currents. The kinetics, steady-state activation and inactivation parameters, and external tetraethylammonium sensitivity were all similar to those described previously for hKv2.1 channels transiently expressed in Xenopus oocytes or other mammalian cell lines. A number of dopamine receptor antagonist/antipsychotic agents were shown to block hKv2.1. Trifluoperizine, trifluperidol and pimozide produced time-dependent blockade of hKv2.1 with IC50 values of approx. 1-2 microM. The diphenylbutylpiperidine fluspirilene was shown to be 4-5-fold more potent than the other agents tested inhibiting hKv2.1 current with an IC50 value of 297 nM. The block produced by fluspirilene was both time- and frequency-dependent. Furthermore, fluspirilene (1 microM) shifted the midpotential of the hKv2.1 steady-state inactivation curve by approx. 15 mV in the hyperpolarizing direction. These results demonstrate the usefulness of this transfection system for the pharmacological characterization of hKv2. 1. Fluspirilene proved to be a relatively potent blocker of hKv2.1 and may provide a useful starting point for the development of more potent and selective agents active against this brain K+ channel.
[Mh] Termos MeSH primário: Antipsicóticos/farmacologia
Bloqueadores dos Canais de Potássio
Canais de Potássio Corretores do Fluxo de Internalização
Canais de Potássio/genética
[Mh] Termos MeSH secundário: Animais
Química Encefálica/fisiologia
Clonagem Molecular
Feminino
Fluspirileno/farmacologia
Expressão Gênica/fisiologia
Glioblastoma
Seres Humanos
Ativação do Canal Iônico/fisiologia
Dados de Sequência Molecular
Miocárdio/química
Oócitos/fisiologia
Técnicas de Patch-Clamp
Pimozida/farmacologia
Reação em Cadeia da Polimerase
RNA Mensageiro/análise
Trifluoperazina/farmacologia
Trifluperidol/farmacologia
Células Tumorais Cultivadas/química
Células Tumorais Cultivadas/efeitos dos fármacos
Células Tumorais Cultivadas/fisiologia
Xenopus
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antipsychotic Agents); 0 (Kcnj10 (channel)); 0 (Potassium Channel Blockers); 0 (Potassium Channels); 0 (Potassium Channels, Inwardly Rectifying); 0 (RNA, Messenger); 1HIZ4DL86F (Pimozide); 214IZI85K3 (Trifluoperazine); C5QA4GLR9M (Fluspirilene); R8869Q7R8I (Trifluperidol)
[Em] Mês de entrada:9710
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:970627
[St] Status:MEDLINE


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[PMID]:9023267
[Au] Autor:Coughenour LL; Cordon JJ
[Ad] Endereço:Department of Neurological and Neurodegenerative Disease, Parke-Davis Pharmaceutical Research, Ann Arbor, Michigan 48105, USA.
[Ti] Título:Characterization of haloperidol and trifluperidol as subtype-selective N-methyl-D-aspartate (NMDA) receptor antagonists using [3H]TCP and [3H]ifenprodil binding in rat brain membranes.
[So] Source:J Pharmacol Exp Ther;280(2):584-92, 1997 Feb.
[Is] ISSN:0022-3565
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:[3H]TCP and [3H]ifenprodil binding to N-methyl-D-aspartate (NMDA) receptors in rat forebrain membranes was used to compare the inhibition of haloperidol and trifluperidol with that of ifenprodil and eliprodil. In the [3H]TCP binding assay, inhibition curves of ifenprodil, eliprodil, haloperidol and trifluperidol revealed two affinity states in the presence of glutamate, glycine and spermidine. The potency of these agents to inhibit the high-affinity fraction of the binding agreed with the results of other studies investigating their potency to block glutamate-induced current at recombinant NR1a/NR2B NMDA receptors expressed in Xenopus oocytes. These agents also inhibited [3H]ifenprodil binding in a biphasic manner, whether in the absence or the presence of either the sigma site ligand GBR-12909 or spermidine. Spermidine reduced the fraction of high-affinity sites labeled with [3H]ifenprodil. The only alteration in the affinity was a decrease in the IC50 value of haloperidol to inhibit the high-affinity fraction of [3H]ifenprodil binding. GBR-12909 also reduced the fraction of [3H]ifenprodil sites inhibited by these compounds with high affinity, with no change in the affinity for either fraction. These data suggest that spermidine is neither a competitive antagonist at the fraction of the binding inhibited by these agents with high affinity, nor is this fraction of the binding to sigma sites. Haloperidol and trifluperidol represent a new class of agent that interacts at a site that is labeled by [3H]ifenprodil as well as [3H]TCP in rat brain membranes and that closely reflects ifenprodil's voltage-independent site on the recombinant NR1a/NR2B subtype of the NMDA receptor.
[Mh] Termos MeSH primário: Encéfalo/metabolismo
Haloperidol/farmacologia
Fenciclidina/análogos & derivados
Piperidinas/metabolismo
Receptores de N-Metil-D-Aspartato/antagonistas & inibidores
Trifluperidol/farmacologia
[Mh] Termos MeSH secundário: Animais
Ligação Competitiva
Membrana Celular/metabolismo
Feminino
Cinética
Oócitos/fisiologia
Fenciclidina/metabolismo
Piperidinas/farmacologia
Ensaio Radioligante
Ratos
Receptores de N-Metil-D-Aspartato/efeitos dos fármacos
Receptores de N-Metil-D-Aspartato/metabolismo
Proteínas Recombinantes/efeitos dos fármacos
Proteínas Recombinantes/metabolismo
Drogas Ilícitas
Xenopus
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Piperidines); 0 (Receptors, N-Methyl-D-Aspartate); 0 (Recombinant Proteins); 0 (Street Drugs); 8BQ45Q6VCL (tenocyclidine); J1DOI7UV76 (Phencyclidine); J6292F8L3D (Haloperidol); R8869Q7R8I (Trifluperidol); R8OE3P6O5S (ifenprodil); YW62A6TW29 (eliprodil)
[Em] Mês de entrada:9703
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:970201
[St] Status:MEDLINE


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[PMID]:8988026
[Au] Autor:Moebius FF; Bermoser K; Reiter RJ; Hanner M; Glossmann H
[Ad] Endereço:Institut für Biochemische Pharmakologie, Universität Innsbruck, Austria.
[Ti] Título:Yeast sterol C8-C7 isomerase: identification and characterization of a high-affinity binding site for enzyme inhibitors.
[So] Source:Biochemistry;35(51):16871-8, 1996 Dec 24.
[Is] ISSN:0006-2960
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The yeast gene ERG2 encodes a sterol C8-C7 isomerase and is essential for ergosterol synthesis and cell proliferation. Its striking homology with the so-called sigma1 receptor of guinea pig brain, a polyvalent steroid and drug binding protein, suggested that the yeast sterol C8-C7 isomerase (ERG2) carries a similar high affinity drug binding domain. Indeed the sigma ligands [3H]haloperidol (Kd = 0.3 nM) and [3H]ifenprodil (Kd = 1.4 nM) bound to a single population of sites in ERG2 wild type yeast microsomes (Bmax values of 77 and 61 pmol/mg of protein, respectively), whereas binding activity was absent in strains carrying ERG2 gene mutations or disruptions. [3H]Ifenprodil binding was inhibited by sterol isomerase inhibitors such as fenpropimorph (Ki = 0.05 nM), tridemorph (Ki = 0.09 nM), MDL28,815 (Ki = 0.44 nM), triparanol (Ki = 1.5 nM), and AY-9944 (Ki = 5.8 nM). [3H]Haloperidol specifically photoaffinity-labeled a protein with an apparent molecular weight of 27400, in agreement with the molecular mass of the sterol C8-C7 isomerase (24900 Da). 9E10 c-myc antibodies specifically immunoprecipitated the c-myc tagged protein after [3H]haloperidol photolabeling, unequivocally proving that the drug binding site is localized on the ERG2 gene product. Haloperidol, trifluperidol, and ifenprodil inhibited the growth of Saccharomyces cerevisiae and reduced the ergosterol content of cells grown in their presence. Our results demonstrate that the yeast sterol C8-C7 isomerase has a polyvalent high-affinity drug binding site similar to mammalian sigma receptors and that in yeast sigma ligands inhibit sterol biosynthesis.
[Mh] Termos MeSH primário: Saccharomyces cerevisiae/enzimologia
Esteroide Isomerases/antagonistas & inibidores
[Mh] Termos MeSH secundário: Animais
Sequência de Bases
Sítios de Ligação
Primers do DNA/genética
Inibidores Enzimáticos/metabolismo
Inibidores Enzimáticos/farmacologia
Ergosterol/biossíntese
Cobaias
Haloperidol/metabolismo
Haloperidol/farmacologia
Cinética
Ligantes
Mutação
Piperidinas/metabolismo
Piperidinas/farmacologia
Receptores sigma/química
Receptores sigma/genética
Receptores sigma/metabolismo
Saccharomyces cerevisiae/efeitos dos fármacos
Saccharomyces cerevisiae/genética
Esteroide Isomerases/química
Esteroide Isomerases/genética
Trifluperidol/metabolismo
Trifluperidol/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (DNA Primers); 0 (Enzyme Inhibitors); 0 (Ligands); 0 (Piperidines); 0 (Receptors, sigma); EC 5.3.3.- (Steroid Isomerases); EC 5.3.3.- (delta(8)-delta(7)-sterol isomerase); J6292F8L3D (Haloperidol); R8869Q7R8I (Trifluperidol); R8OE3P6O5S (ifenprodil); Z30RAY509F (Ergosterol)
[Em] Mês de entrada:9701
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:961224
[St] Status:MEDLINE


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[PMID]:7925603
[Au] Autor:Hariton C
[Ad] Endereço:Ciba-Vision Ophthalmics, International Ophtha R&D, Bülach, Switzerland.
[Ti] Título:Ocular hypotension induced by topical dopaminergic drugs and phosphodiesterase inhibitors.
[So] Source:Eur J Pharmacol;258(1-2):85-94, 1994 Jun 02.
[Is] ISSN:0014-2999
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:The aim of this work was to investigate the ocular hypotensive activity of some topically administered cAMP-phosphodiesterase inhibitors alone and in combination with dopaminergic compounds. Experiments were performed with ocular normotensive rabbits and during transitory induced ocular hyper- or hypotension. An ocular hypotensive effect was observed after instillation of aminophylline, dyphylline, pentoxifylline, caffeine, and iso-caffeine, but not following topical hydroxypropyl-1,3-dimethylxanthine. Dopaminergic compounds were also studied in order to be combined with phosphodiesterase inhibitors as ocular anti-hypertensive treatment. Significant ocular hypotensive activity was observed after topical application of trifluperidol, fluphenazine, thiothixene, and the S(-) enantiomer of 3-(3-hydroxyphenyl)-N-n-propylpiperidine (3-PPP). Of the cAMP-phosphodiesterase inhibitors that were tested, pentoxifylline was the most interesting compound, with good ocular tolerance, significant reduction in intra-ocular pressure, and potential retinal microvascular benefits. After allowing adequate time for pentoxifylline to reach its maximal activity, trifluperidol or S(-)-3-PPP was also instilled. A more pronounced ocular hypotensive effect was then observed. The findings of this study may suggest that administration of eye-drops combining drugs acting by separate ways on second messengers involved in the regulation of intra-ocular pressure (e.g. cyclic AMP) could be used to reduce intra-ocular pressure during glaucoma.
[Mh] Termos MeSH primário: Dopaminérgicos/farmacologia
Hipotensão Ocular/induzido quimicamente
Inibidores de Fosfodiesterase/farmacologia
[Mh] Termos MeSH secundário: Administração Tópica
Animais
Dopaminérgicos/administração & dosagem
Glucose/administração & dosagem
Glucose/farmacologia
Masculino
Soluções Oftálmicas
Pentoxifilina/farmacologia
Inibidores de Fosfodiesterase/administração & dosagem
Piperidinas/farmacologia
Coelhos
Estereoisomerismo
Trifluperidol/farmacologia
Xantinas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Dopamine Agents); 0 (Ophthalmic Solutions); 0 (Phosphodiesterase Inhibitors); 0 (Piperidines); 0 (Xanthines); 9V2O6CRQ6Z (preclamol); IY9XDZ35W2 (Glucose); R8869Q7R8I (Trifluperidol); SD6QCT3TSU (Pentoxifylline)
[Em] Mês de entrada:9410
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:940602
[St] Status:MEDLINE


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[PMID]:1363957
[Au] Autor:Skrinskaia IuA; Nikulina EM; Popova NK
[Ti] Título:[The role of the genotype in the cataleptogenic effect of neuroleptics].
[Ti] Título:Rol' genotipa v kataleptogennom éffekte neiroleptikov..
[So] Source:Eksp Klin Farmakol;55(6):7-9, 1992 Nov-Dec.
[Is] ISSN:0869-2092
[Cp] País de publicação:Russia (Federation)
[La] Idioma:rus
[Ab] Resumo:The cataleptogenic effects of three neuroleptics from one chemical group was investigated in 8 mice strains (CBA, A/He, C57B1/6, C3H/He, BALB/c, AKR, DD, and CC57Br. Despite significant interstrain, differences in the action of the drugs, haloperidol (0.5 mg/kg) and trifluperidol (0.5 mg/kg) produced much greater cataleptogenic action than fluspirilene (2 mg/kg). At the same time the intensity of catalepsy in various mice strains after haloperidol was not coincident with that after trifluperidol (r = 0.22): CBA mice displayed the maximum catalepsy, but AKR, DD and CC57Br mice, the minimum when haloperidol was given; with trifluperidol, the maximum catalepsy was observed in AKR mice, but absent in DD mice. Fluspirilene induced catalepsy only in CBA and A/He mice. Thus, the presence of catalepsy, a side effect of most neuroleptics, is largely predetermined by hereditary factors.
[Mh] Termos MeSH primário: Antipsicóticos/farmacologia
Catalepsia/induzido quimicamente
Catalepsia/genética
Camundongos Endogâmicos/genética
[Mh] Termos MeSH secundário: Animais
Relação Dose-Resposta a Droga
Fluspirileno/farmacologia
Genótipo
Haloperidol/farmacologia
Masculino
Camundongos
Especificidade da Espécie
Trifluperidol/farmacologia
[Pt] Tipo de publicação:COMPARATIVE STUDY; ENGLISH ABSTRACT; JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antipsychotic Agents); C5QA4GLR9M (Fluspirilene); J6292F8L3D (Haloperidol); R8869Q7R8I (Trifluperidol)
[Em] Mês de entrada:9307
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:921101
[St] Status:MEDLINE


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[PMID]:1302433
[Au] Autor:Chiou GC; Chen YJ
[Ad] Endereço:Department of Medical Pharmacology and Toxicology, Texas A&M University College of Medicine, College Station 77843-1114.
[Ti] Título:Improvement of ocular blood flow with dopamine antagonists on ocular-hypertensive rabbit eyes.
[So] Source:Zhongguo Yao Li Xue Bao;13(6):481-4, 1992 Nov.
[Is] ISSN:0253-9756
[Cp] País de publicação:China
[La] Idioma:eng
[Ab] Resumo:The eyedrops of the ocular-hypotensive dopamine antagonists, trifluperidol, moperone, lenperone, and spiperone, were instilled into an ocular-hypertensive rabbit eye. The blood flows in the choroid, retina, iris root-ciliary body, and iris were measured with colored microspheres at various time periods. It was found that all these dopamine antagonists, at a concentration of 0.5%, increased the blood flow in all eye tissues. Dopamine, at a concentration of 3%, produced a biphasic action by decreasing the blood flow initially at 30 min, then increasing it at 120 min and thereafter. But 1.5% dopamine produced a monophasic action which increased the blood flow after 180 min. Since dopamine antagonists are not cholinergics or adrenolytics, they are not supposed to produce the side effects induced by pilocarpine or timolol. It is hoped that they can become satisfactory drugs for glaucoma and ocular hypertension.
[Mh] Termos MeSH primário: Antagonistas de Dopamina
Olho/irrigação sanguínea
Hipertensão Ocular/fisiopatologia
Trifluperidol/farmacologia
[Mh] Termos MeSH secundário: Animais
Butirofenonas/farmacologia
Pressão Intraocular/efeitos dos fármacos
Hipertensão Ocular/tratamento farmacológico
Soluções Oftálmicas
Coelhos
Fluxo Sanguíneo Regional/efeitos dos fármacos
Espiperona/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Butyrophenones); 0 (Dopamine Antagonists); 0 (Ophthalmic Solutions); 13P4GX22ES (lenperone); 4X6E73CJ0Q (Spiperone); OU730881W5 (moperone); R8869Q7R8I (Trifluperidol)
[Em] Mês de entrada:9306
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:921101
[St] Status:MEDLINE



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