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[PMID]:22786790
[Au] Autor:Beuck S; Sigmund G; Koch A; Schänzer W; Pokrywka A; Kwiatkowska D; Thevis M
[Ad] Endereço:Institute of Biochemistry, German Sport University Cologne, Cologne, Germany.
[Ti] Título:Identification and characterization of urinary prenylamine metabolites by means of liquid chromatography-tandem mass spectrometry.
[So] Source:Drug Test Anal;4(9):701-16, 2012 Sep.
[Is] ISSN:1942-7611
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Prenylamine is a vasodilator of phenylalkylamine structure and was used for the treatment of angina pectoris, until reports of undesirable effects including ventricular tachycardia led to a decreasing use of the drug in the 1980s. Metabolic N-dealkylation of orally ingested prenylamine can liberate amphetamine in humans and cause positive findings for amphetamine in doping and forensic analysis. In 2010, the World Anti-Doping Agency (WADA) classified prenylamine as a non-specified stimulant according to the 2010 Prohibited List, thus banning its use in sports in-competition. Supporting the development of a liquid chromatography-tandem mass spectrometry (LC-MS/MS) based detection method, a post-administration urine sample following a single oral prenylamine ingestion (Segontin(®) 60 mg) was analyzed for urinary metabolites. The LC-separated analytes were ionized in positive electrospray ionization (ESI) mode and detected as protonated ions using an AB Sciex TripleTOF 5600 quadrupole-time-of-flight hybrid mass spectrometer. Over 40 phase I metabolites were detected, including previously unknown mono- bis-, tris- and tetra-hydroxylated prenylamine, several hydroxylated and methoxylated prenylamine metabolites and (hydroxylated) diphenylpropylamine. Investigation of the collision-induced dissociation behaviours of the metabolites by high resolution/high accuracy mass spectrometry allowed for the assignment of the nature and the site of observed metabolic transformations. The most abundant phase I metabolite was confirmed as p-hydroxy-prenlyamine by chemical synthesis and stable isotope labelling of reference material. An existing routine screening assay based on direct injection and LC-MS/MS analysis of urine was modified and validated according to common guidelines, in order to allow for the detection of p-hydroxy-prenylamine in sports drug testing. The assay demonstrated the ability to detect the target metabolite at 0.1 ng/ml at intra- and inter-day imprecisions below 10%.
[Mh] Termos MeSH primário: Adrenérgicos/metabolismo
Adrenérgicos/urina
Prenilamina/metabolismo
Prenilamina/urina
Espectrometria de Massas em Tandem/métodos
[Mh] Termos MeSH secundário: Cromatografia Líquida/métodos
Doping nos Esportes
Seres Humanos
Limite de Detecção
Masculino
Meia-Idade
Detecção do Abuso de Substâncias/métodos
Vasodilatadores/metabolismo
Vasodilatadores/urina
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T; VALIDATION STUDIES
[Nm] Nome de substância:
0 (Adrenergic Agents); 0 (Vasodilator Agents); K2OH82Z000 (Prenylamine)
[Em] Mês de entrada:1302
[Cu] Atualização por classe:160511
[Lr] Data última revisão:
160511
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:120713
[St] Status:MEDLINE
[do] DOI:10.1002/dta.1388


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[PMID]:17082184
[Au] Autor:Lohmann A; Schöttler MA; Bréhélin C; Kessler F; Bock R; Cahoon EB; Dörmann P
[Ad] Endereço:Department of Molecular Physiology, Max Planck Institute of Molecular Plant Physiology, Am Mühlenberg 1, 14476 Potsdam, Germany.
[Ti] Título:Deficiency in phylloquinone (vitamin K1) methylation affects prenyl quinone distribution, photosystem I abundance, and anthocyanin accumulation in the Arabidopsis AtmenG mutant.
[So] Source:J Biol Chem;281(52):40461-72, 2006 Dec 29.
[Is] ISSN:0021-9258
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Phylloquinone (vitamin K(1)) is synthesized in cyanobacteria and in chloroplasts of plants, where it serves as electron carrier of photosystem I. The last step of phylloquinone synthesis in cyanobacteria is the methylation of 2-phytyl-1,4-naphthoquinone by the menG gene product. Here, we report that the uncharacterized Arabidopsis gene At1g23360, which shows sequence similarity to menG, functionally complements the Synechocystis menG mutant. An Arabidopsis mutant, AtmenG, carrying a T-DNA insertion in the gene At1g23360 is devoid of phylloquinone, but contains an increased amount of 2-phytyl-1,4-naphthoquinone. Phylloquinone and 2-phytyl-1,4-naphthoquinone in thylakoid membranes of wild type and AtmenG, respectively, predominantly localize to photosystem I, whereas excess amounts of prenyl quinones are stored in plastoglobules. Photosystem I reaction centers are decreased in AtmenG plants under high light, as revealed by immunoblot and spectroscopic measurements. Anthocyanin accumulation and chalcone synthase (CHS1) transcription are affected during high light exposure, indicating that alterations in photosynthesis in AtmenG affect gene expression in the nucleus. Photosystem II quantum yield is decreased under high light. Therefore, the loss of phylloquinone methylation affects photosystem I stability or turnover, and the limitation in functional photosystem I complexes results in overreduction of photosystem II under high light.
[Mh] Termos MeSH primário: Antocianinas/metabolismo
Proteínas de Arabidopsis/metabolismo
Deleção de Genes
Metiltransferases/metabolismo
Naftoquinonas/metabolismo
Complexo de Proteína do Fotossistema I/metabolismo
Prenilamina/análogos & derivados
Prenilamina/metabolismo
Vitamina K 1/metabolismo
[Mh] Termos MeSH secundário: Arabidopsis/enzimologia
Arabidopsis/genética
Arabidopsis/metabolismo
Proteínas de Arabidopsis/genética
Luz
Metilação
Metiltransferases/deficiência
Metiltransferases/genética
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Anthocyanins); 0 (Arabidopsis Proteins); 0 (Naphthoquinones); 0 (Photosystem I Protein Complex); 84-80-0 (Vitamin K 1); EC 2.1.1.- (Methyltransferases); EC 2.1.1.- (S-adenosylmethionine-dependent phosphate methyltransferase); K2OH82Z000 (Prenylamine)
[Em] Mês de entrada:0702
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:061104
[St] Status:MEDLINE


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[PMID]:16169232
[Au] Autor:Molinari A; Oliva A; Ojeda C; Miguel del Corral JM; Castro MA; Cuevas C; San Feliciano A
[Ad] Endereço:Instituto de Química, Pontificia Universidad Católica de Valparaíso, Avenida Brasil 2950, Valparaíso, Chile. amolinar@ucv.cl
[Ti] Título:New cytotoxic-antineoplastic prenyl-1,2-naphthohydroquinone derivatives.
[So] Source:Bioorg Med Chem;13(24):6645-50, 2005 Dec 15.
[Is] ISSN:0968-0896
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Several new prenylnaphthohydroquinone derivatives have been prepared through the Diels-Alder condensation between alpha-myrcene and 1,2-benzoquinone and evaluated for their cytotoxic activity against A-549, HT-29 and MB-231 cultured cell lines. All of them have shown GI50 values in the microM level.
[Mh] Termos MeSH primário: Antineoplásicos/química
Antineoplásicos/toxicidade
Naftoquinonas/química
Naftoquinonas/toxicidade
Prenilamina/análogos & derivados
[Mh] Termos MeSH secundário: Linhagem Celular Tumoral
Sobrevivência Celular/efeitos dos fármacos
Seres Humanos
Concentração Inibidora 50
Isomerismo
Estrutura Molecular
Naftoquinonas/síntese química
Prenilamina/síntese química
Prenilamina/química
Prenilamina/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Naphthoquinones); 0 (prenyl-1,2-naphthohydroquinone); K2OH82Z000 (Prenylamine)
[Em] Mês de entrada:0601
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:050920
[St] Status:MEDLINE


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[PMID]:12669999
[Au] Autor:Kraemer T; Roditis SK; Peters FT; Maurer HH
[Ad] Endereço:Department of Experimental and Clinical Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, University of Saarland, D-66421 Homburg (Saar), Germany.
[Ti] Título:Amphetamine concentrations in human urine following single-dose administration of the calcium antagonist prenylamine-studies using fluorescence polarization immunoassay (FPIA) and GC-MS.
[So] Source:J Anal Toxicol;27(2):68-73, 2003 Mar.
[Is] ISSN:0146-4760
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Prenylamine (R,S-N-(3,3-diphenylpropyl-methyl-2-phenethylamine), a World Health Organization class V calcium antagonist, is known to be metabolized to amphetamine. In this study, amphetamine concentrations after a single-dose administration of prenylamine were determined to check if they reached values that could be of analytical and/or pharmacological importance in clinical and forensic toxicology. Enantiomeric composition of amphetamine was also studied. Five volunteers received a single 120-mg oral dose of prenylamine. Urine samples were analyzed using the Abbott TDx immunoassay Amphetamine/Methamphetamine II and using our routine systematic toxicological analysis (STA) gas chromatography-mass spectrometry (GC-MS) procedure. For quantitation purposes, GC-MS was used in the selected-ion monitoring (SIM) mode (ions m/z 118, 122, 240, 244) after solid-phase extraction (Isolute Confirm HCX) and derivatization (heptafluorobutyric anhydride). Amphetamine-d5 was used as internal standard (IS). Chiral separation of the heptafluorobutyrated amphetamine enantiomers was achieved using an Astec Chiraldex G-PN column. The TDx results showed a great variability for the different volunteers. A urine sample of one volunteer showed results as high as 3200 ng/mL, whereas the urine samples of another volunteer never gave results greater than the TDx detection limit (100 ng/mL). Using the STA procedure, the presence of amphetamine could be confirmed in all urine samples with TDx results greater than the cutoff value (300 ng/mL). Using the GC-MS SIM method, amphetamine concentrations up to 1280 ng/mL were determined. Chiral analysis revealed that both enantiomers of amphetamine were present in the samples with a surplus of the S(+)-enantiomer in the early phase of excretion. Forensic implications are discussed.
[Mh] Termos MeSH primário: Anfetamina/urina
Bloqueadores dos Canais de Cálcio/metabolismo
Estimulantes do Sistema Nervoso Central/urina
Prenilamina/metabolismo
[Mh] Termos MeSH secundário: Bloqueadores dos Canais de Cálcio/farmacocinética
Imunoensaio de Fluorescência por Polarização
Cromatografia Gasosa-Espectrometria de Massas
Seres Humanos
Prenilamina/farmacocinética
Fatores de Tempo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Calcium Channel Blockers); 0 (Central Nervous System Stimulants); CK833KGX7E (Amphetamine); K2OH82Z000 (Prenylamine)
[Em] Mês de entrada:0310
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:030403
[St] Status:MEDLINE


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[PMID]:12223231
[Au] Autor:Kerr DI; Ong J; Puspawati NM; Prager RH
[Ad] Endereço:Department of Anaesthesia and Intensive Care, The University of Adelaide, Adelaide, South Australia 5005, Australia.
[Ti] Título:Arylalkylamines are a novel class of positive allosteric modulators at GABA(B) receptors in rat neocortex.
[So] Source:Eur J Pharmacol;451(1):69-77, 2002 Sep 06.
[Is] ISSN:0014-2999
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:Using grease-gap recording from rat neocortical slices, the gamma-aminobutyric acid(B) (GABA(B)) receptor agonists baclofen (3-100 microM) and SKF 97541 (3-aminopropyl-methylphosphinic acid) (1-30 microM) elicited reversible and concentration-dependent hyperpolarizing responses, with EC(50) values of 10 and 3 microM, respectively. The hyperpolarizations were antagonised by the GABA(B) receptor antagonist Sch 50911 ((+)-(S)-5,5-dimethylmorpholinyl-2-acetic acid) (1, 5 and 10 microM). Fendiline (N-[3,3-diphenylpropyl)-alpha-methylbenzylamine) (5-50 microM) and its congeners, prenylamine (N-[3,3-diphenylpropyl)-alpha-methylphenylethylamine) (10-100 microM) and F551 (N-[3,3-diphenylpropyl)-alpha-methyl-3-methoxybenzylamine) (1-30 microM) reversibly enhanced hyperpolarizing responses to the agonists; such effects were reduced by Sch 50911. These arylalkylamines produced leftward shifts of the concentration-response curves, with a marked increase in the maximal hyperpolarization obtained, compared with the agonists alone, F551 being the most potent. These findings suggest that these arylalkylamines represent a new class of positive modulators of GABA(B) receptor-mediated function.
[Mh] Termos MeSH primário: Baclofeno/farmacologia
Fendilina/farmacologia
Agonistas dos Receptores de GABA-B
Neocórtex/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Sinergismo Farmacológico
Masculino
Prenilamina/farmacologia
Ratos
Ratos Sprague-Dawley
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (GABA-B Receptor Agonists); H789N3FKE8 (Baclofen); K2OH82Z000 (Prenylamine); S253D559A8 (Fendiline)
[Em] Mês de entrada:0302
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:020912
[St] Status:MEDLINE


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[PMID]:12024689
[Au] Autor:Cody JT
[Ad] Endereço:Academy of Health Sciences, MCCS-HMP PA Branch, 3151 Scott Road, Ft Sam, Houston, TX 78234-6138, USA. john.cody@amedd.army.mil
[Ti] Título:Precursor medications as a source of methamphetamine and/or amphetamine positive drug testing results.
[So] Source:J Occup Environ Med;44(5):435-50, 2002 May.
[Is] ISSN:1076-2752
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Medical Review Officer interpretation of laboratory results is an important component of drug testing programs. The clinical evaluation of laboratory results to assess the possibility of appropriate medical use of a drug is a task with many different facets, depending on the drug class considered. This intercession prevents the reporting of positive results unless it is apparent that drugs were used illicitly. In addition to the commonly encountered prescribed drugs that yield positive drug testing results, other sources of positive results must be considered. This review describes a series of compounds referred to as "precursor" drugs that are metabolized by the body to amphetamine and/or methamphetamine. These compounds lead to positive results for amphetamines even though neither amphetamine nor methamphetamine were used, a possibility that must be considered in the review of laboratory results. Description of the drugs, their clinical indications, and results seen following administration are provided. This information allows for the informed evaluation of results with regard to the potential involvement of these drugs.
[Mh] Termos MeSH primário: Anfetamina/metabolismo
Cafeína/análogos & derivados
Metanfetamina/análogos & derivados
Metanfetamina/metabolismo
Pró-Fármacos/metabolismo
Pirazolonas
Detecção do Abuso de Substâncias
Teofilina/análogos & derivados
[Mh] Termos MeSH secundário: Anfetamina/química
Anfetaminas/metabolismo
Benzfetamina/metabolismo
Cafeína/metabolismo
Furanos/metabolismo
Seres Humanos
Metanfetamina/química
Estrutura Molecular
Prenilamina/metabolismo
Pró-Fármacos/química
Pirazóis/metabolismo
Selegilina/metabolismo
Sidnonas/metabolismo
Teofilina/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Amphetamines); 0 (Furans); 0 (Prodrugs); 0 (Pyrazoles); 0 (Pyrazolones); 0 (Sydnones); 022YON1XMX (ethylamphetamine); 0M3S43XK27 (Benzphetamine); 17590-01-1 (amphetaminil); 2K1V7GP655 (Selegiline); 3AO7AC8C6K (fencamine); 3G6A5W338E (Caffeine); 44RAL3456C (Methamphetamine); 4A5352XI2A (clobenzorex); C137DTR5RG (Theophylline); CK833KGX7E (Amphetamine); HN0NCX453C (famprofazone); IYE3F3MHCU (dimethylamphetamine); K2OH82Z000 (Prenylamine); K98M4N387W (mefenorex); UMT8MP2NDU (sidnocarb); W0194S5FOA (fenproporex); X83CZ0Y5TF (furfenorex); YZ0N7VL5R3 (fenethylline)
[Em] Mês de entrada:0211
[Cu] Atualização por classe:171116
[Lr] Data última revisão:
171116
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:020525
[St] Status:MEDLINE


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[PMID]:11684990
[Au] Autor:Mujtaba MG; Gerner P; Wang GK
[Ad] Endereço:Department of Anesthesia Research Laboratories, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts 02115, USA. mujtaba@zeus.bwh.harvard.edu
[Ti] Título:Local anesthetic properties of prenylamine.
[So] Source:Anesthesiology;95(5):1198-204, 2001 Nov.
[Is] ISSN:0003-3022
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Local anesthetics that produce analgesia of long duration with minimal impairment of autonomic functions are highly desirable for pain management in the clinic. Prenylamine is a known calcium channel blocker, but its local anesthetic blocking effects on voltage-gated sodium channels have not been studied thus far. METHODS: The authors characterized the tonic and use-dependent prenylamine block of native Na(+) channels in cultured rat neuronal GH3 cells during whole cell voltage clamp conditions and the local anesthetic effect of prenylamine by neurologic evaluation of sensory and motor functions of sciatic nerve during neural block in rats. RESULTS: Prenylamine elicits both use-dependent block of Na(+) channels during repetitive pulses (3 microm prenylamine produced 50% block at 5 Hz) and tonic block for both resting and inactivated Na(+) channels. The 50% inhibitory concentration for prenylamine was 27.6 +/- 1.3 microm for resting channels and 0.75 +/- 0.02 microm for inactivated channels. Furthermore, in vivo data show that 10 mm prenylamine produced a complete sciatic nerve block of motor function, proprioceptive responses, and nociceptive responses that lasted approximately 27, 34, and 24 h, respectively. Rats injected with 15.4 mm bupivacaine, a known local anesthetic currently used for pain management, had a significantly shorter duration of blockade (< 2 h) compared with rats injected with prenylamine. CONCLUSIONS: The data presented here demonstrate that prenylamine possesses local anesthetic properties in vitro and elicits prolonged local anesthesia in vivo.
[Mh] Termos MeSH primário: Anestésicos Locais/farmacologia
Bupivacaína/farmacologia
Bloqueadores dos Canais de Cálcio/farmacologia
Prenilamina/farmacologia
Canais de Sódio/efeitos dos fármacos
[Mh] Termos MeSH secundário: Animais
Células Cultivadas
Masculino
Bloqueio Nervoso
Dor/prevenção & controle
Técnicas de Patch-Clamp
Ratos
Ratos Sprague-Dawley
Nervo Isquiático/efeitos dos fármacos
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, U.S. GOV'T, P.H.S.
[Nm] Nome de substância:
0 (Anesthetics, Local); 0 (Calcium Channel Blockers); 0 (Sodium Channels); K2OH82Z000 (Prenylamine); Y8335394RO (Bupivacaine)
[Em] Mês de entrada:0112
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:AIM; IM
[Da] Data de entrada para processamento:011031
[St] Status:MEDLINE


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[PMID]:11152392
[Au] Autor:Ichida S; Abe J; Zhang YA; Sugihara K; Imoto K; Wada T; Fujita N; Sohma H
[Ad] Endereço:Department of Biological Chemistry, Faculty of Pharmaceutical Sciences, Kinki University, Higashi-Osaka, Japan.
[Ti] Título:Characteristics of the inhibitory effect of calmodulin on specific [125i]omega-conotoxin GVIA binding to crude membranes from chick brain.
[So] Source:Neurochem Res;25(12):1629-35, 2000 Dec.
[Is] ISSN:0364-3190
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The characteristics of the inhibitory effect of calcium ion (Ca2+)/calmodulin (CaM) on specific [125I]-omega-conotoxin GVIA (125I-omega-CTX) binding and on the labeling of 125I-omega-CTX to crude membranes from chick brain were investigated. The inhibitory effect of Ca2+/CaM depended on the concentrations of free Ca2+ and CaM. The IC50 values for free Ca2+ and CaM were about 2.0 x 10(-8) M and 3.0 microg protein/ml, respectively. The inhibitory effect of Ca2+/CaM was attenuated by the CaM antagonists W-7, prenylamine and CaM-kinase II fragment (290-309), but not by the calcineurin inhibitor FK506. Ca2+/CaM also inhibited the labeling of a 135-kDa band (which was considered to be part of N-type Ca2+ channel alpha1 subunits) with 125I-omega-CTX using a cross-linker. These results suggest that Ca2+/CaM affects specific 125I-omega-CTX binding sites, probably N-type Ca2+ channel alpha1 subunits, in crude membranes from chick whole brain.
[Mh] Termos MeSH primário: Encéfalo/metabolismo
Bloqueadores dos Canais de Cálcio/metabolismo
Calmodulina/farmacologia
ômega-Conotoxina GVIA/antagonistas & inibidores
[Mh] Termos MeSH secundário: Animais
Animais Recém-Nascidos
Cálcio/metabolismo
Canais de Cálcio Tipo N/efeitos dos fármacos
Canais de Cálcio Tipo N/metabolismo
Proteínas Quinases Dependentes de Cálcio-Calmodulina/antagonistas & inibidores
Proteínas Quinases Dependentes de Cálcio-Calmodulina/farmacologia
Calmodulina/antagonistas & inibidores
Galinhas
Inibidores Enzimáticos/farmacologia
Radioisótopos do Iodo
Isoenzimas/farmacologia
Masculino
Membranas/metabolismo
Fragmentos de Peptídeos/farmacologia
Prenilamina/farmacologia
Ratos
Ratos Wistar
Sulfonamidas/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Calcium Channel Blockers); 0 (Calcium Channels, N-Type); 0 (Calmodulin); 0 (Enzyme Inhibitors); 0 (Iodine Radioisotopes); 0 (Isoenzymes); 0 (Peptide Fragments); 0 (Sulfonamides); 65595-90-6 (W 7); 92078-76-7 (omega-Conotoxin GVIA); EC 2.7.11.17 (Calcium-Calmodulin-Dependent Protein Kinases); K2OH82Z000 (Prenylamine); SY7Q814VUP (Calcium)
[Em] Mês de entrada:0104
[Cu] Atualização por classe:171030
[Lr] Data última revisão:
171030
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:010111
[St] Status:MEDLINE


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[PMID]:11065218
[Au] Autor:Cerbai E; Sartiani L; DePaoli P; Matucci R; Davoli G; DiCiolla F; Lisi G; Maccherini M; Sani G; Mugelli A
[Ad] Endereço:Center of Molecular Medicine (CIMMBA) and Department of Preclinical and Clinical Pharmacology of the University of Firenze, Italy.
[Ti] Título:Electrophysiologic effects of lercanidipine on repolarizing potassium currents.
[So] Source:J Cardiovasc Pharmacol;36(5):584-91, 2000 Nov.
[Is] ISSN:0160-2446
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Blockade of cardiac repolarizing potassium channels by drugs may result in QT-interval prolongation, eventually degenerating into "torsades de pointes," a life-threatening arrhythmia. Lercanidipine (LER) is a recently introduced lipophilic calcium antagonist with no cardiodepressant activity and long-lasting antihypertensive action. Its chemical structure is characterized by the presence of a diphenylpropylaminoalkyl group, which is present in some of the drugs that have been reported to cause QT-interval prolongation. Our previous data demonstrated that LER blocks L-type calcium channels without affecting sodium current; however, no data are available concerning its effects on cardiac potassium channels. Transient outward (I(to)), delayed rectifier (I(K)), background currents, and action potential (AP) profile were measured from patch-clamped ventricular myocytes isolated from rat, guinea pig, or human hearts using enzymatic dissociation procedures. LER did not affect I(K) (and I(Kr)) density and activation curve in guinea pig myocytes; the reversal potential of the background current (I(K1)) and its slope were not changed by the drug. Maximal diastolic potential (MDP) and duration of the AP measured at -60 mV (APD(-60)) were not significantly changed. I(to) density and activation curves measured in rat myocytes were similar in the absence and presence of 1 or 10 microM LER. Finally, the effect of LER was tested in human ventricular myocytes: superfusion with 1 microM LER did not affect MDP and APD(-60). I(to) density and the midpoint of activation and inactivation curves were similar in the absence and presence of LER. In conclusion, our data demonstrate that LER does not affect repolarizing potassium currents and action potential profile recorded from guinea pig, rat, and human ventricular myocytes. It is unlikely that LER could cause QT prolongation in vivo.
[Mh] Termos MeSH primário: Bloqueadores dos Canais de Cálcio/farmacologia
Di-Hidropiridinas/farmacologia
Coração/efeitos dos fármacos
Canais de Potássio/efeitos dos fármacos
[Mh] Termos MeSH secundário: Potenciais de Ação
Animais
Butilaminas/farmacologia
Difenidramina/farmacologia
Estimulação Elétrica
Cobaias
Coração/fisiologia
Seres Humanos
Prenilamina/farmacologia
Ratos
Especificidade da Espécie
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
[Nm] Nome de substância:
0 (Butylamines); 0 (Calcium Channel Blockers); 0 (Dihydropyridines); 0 (Potassium Channels); 70KG06964W (terodiline); 8GTS82S83M (Diphenhydramine); K2OH82Z000 (Prenylamine); V7XTJ4R0BH (lercanidipine)
[Em] Mês de entrada:0102
[Cu] Atualização por classe:131121
[Lr] Data última revisão:
131121
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:001107
[St] Status:MEDLINE


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Fotocópia
[PMID]:9127964
[Au] Autor:Nakanishi H; Matsuoka I; Ono T; Yoshida H; Uchibori T; Kogi K
[Ad] Endereço:Department of Pharmacology, Fukushima Medical College, Japan.
[Ti] Título:Effect of a prenylamine analog (MG8926) on spontaneous action potentials in isolated rabbit sinoatrial node.
[So] Source:Fukushima J Med Sci;42(1-2):1-10, 1996 Dec.
[Is] ISSN:0016-2590
[Cp] País de publicação:Japan
[La] Idioma:eng
[Ab] Resumo:Effects of verapamil, prenylamine and a prenylamine analog, MG8926 on the intracellular spontaneous action potentials recorded from the isolated rabbit sinoatrial (SA) node were studied. Verapamil (1 microM), a selective inhibitor for slow Ca2+ channels, prolonged the cycle length, decreased the rate of diastolic depolarization, the rate of rise of action potential, the amplitude of action potential and the maximal diastolic potential, and usually arrested showing subthreshold fluctuation of the membrane potential within several ten min. Prenylamine (10 microM), a nonselective inhibitor for slow Ca2+ channels, tended to prolong the cycle length to decrease the diastolic depolarization, the rate of rise of action potential, the amplitude of action potential. However, these changes were statistically insignificant. Prenylamine at the concentration of 10 microM had no effect on the maximal diastolic potential. MG8926 (10 microM) prolonged the cycle length, decreased the rate of diastolic depolarization, the rate of rise of action potential and tended to decrease the amplitude of action potential. MG8926 at the concentration of 10 microM had almost no effect on the maximal diastolic potential. The present findings may indicate that replacement of phenyl residue of prenylamine by cyclohexyl residue increases the inhibitory action on the slow Ca2+ channels in rabbit SA node.
[Mh] Termos MeSH primário: Antiarrítmicos/farmacologia
Prenilamina/análogos & derivados
Nó Sinoatrial/efeitos dos fármacos
[Mh] Termos MeSH secundário: Potenciais de Ação/efeitos dos fármacos
Animais
Feminino
Técnicas In Vitro
Masculino
Prenilamina/farmacologia
Coelhos
Nó Sinoatrial/fisiologia
Verapamil/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Anti-Arrhythmia Agents); 57653-27-7 (droprenylamine); CJ0O37KU29 (Verapamil); K2OH82Z000 (Prenylamine)
[Em] Mês de entrada:9705
[Cu] Atualização por classe:141120
[Lr] Data última revisão:
141120
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:961201
[St] Status:MEDLINE



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