Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 6 de 6
Filtrar
Mais filtros










Base de dados
Intervalo de ano de publicação
1.
Mol Clin Oncol ; 1(1): 143-147, 2013 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-24649137

RESUMO

The present study presents a novel near-infrared optical probe for the sentinel lymph node (SLN) detection in breast cancer patients, based on the recording of scattered photons. The aim of this study was to improve the detection of patent blue V (PBV), a dye routinely injected during clinical practice. A combined injection of the dye and radioactive colloid was used in the 24 patients enrolled in the study. The clinical results of the ex vivo detection of 70 dye-marked SLNs are reported, subsequent to the injection of various quantities of PBV (0.25-2 ml). The accuracy and success rate of an isotopic probe for the detection of radioactive colloid tracer, the eye visibility threshold of the surgeon and the use of a new optical probe were examined. The radio-labeled and dye-marked sentinel lymph nodes were all detected by the radio-isotopic probe, as opposed to the 75% detected by the eye visibility threshold of the surgeon. The optical probe detected all of the nodes, regardless of the volume of the dye injected. The relative PBV concentration computed by the probe facing SLNs with infravisible/visually undetectable dye-mark was relatively constant at 5.5±1.4 µmol/l. The optical detection of the sentinel lymph nodes using PBV and the probe presented in this study have the potential to reduce the false negative detection rate. This instrument is likely to provide surgeons with a simple diagnostic tool, without significantly changing their surgical procedures.

2.
Bioorg Med Chem ; 6(2): 195-208, 1998 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-9547943

RESUMO

Isomeric norbornane-derived rigid analogs mimicking different potential conformations of ACPD (1-aminocyclopentane-1,3-dicarboxylic acid) and glutamic acid have been synthesized, via the hydantoin route, to be used as conformational probes for bioactive conformations at the glutamatergic receptors of the central nervous system. Activities on metabotropic receptors mGluR1 and mGluR2 are reported and discussed.


Assuntos
Cicloleucina/análogos & derivados , Ácidos Dicarboxílicos/síntese química , Ácido Glutâmico/análogos & derivados , Norbornanos/química , Norbornanos/síntese química , Receptores de Glutamato Metabotrópico/efeitos dos fármacos , Cromatografia Líquida de Alta Pressão , Cicloleucina/química , Cicloleucina/farmacologia , Ácidos Dicarboxílicos/farmacologia , Cromatografia Gasosa-Espectrometria de Massas , Ácido Glutâmico/farmacologia , Isomerismo , Modelos Químicos , Conformação Molecular , Norbornanos/farmacologia
3.
J Med Chem ; 40(19): 3119-29, 1997 Sep 12.
Artigo em Inglês | MEDLINE | ID: mdl-9301676

RESUMO

The four stereoisomers of 1-aminocyclopentane-1,3,4-tricarboxylic acid {ACPT-I (18) and -II (19), (3R, 4R)-III [(-)-20], and (3S,4S)-III [(+)-20]} have been synthesized and evaluated for their effects at glutamate receptors subtypes. ACPTs are ACPD analogues in which a third carboxylic group has been added at position 4 in the cyclopentane ring. None of the ACPT isomers showed a significant effect on ionotropic NMDA, KA, and AMPA receptors. On the other hand, ACPT-II (19) was found to be a general competitive antagonist for metabotropic receptors (mGluRs) and exhibited a similar affinity for mGluR1a (KB = 115 +/- 2 microM), mGluR2 (KB = 88 +/- 21 microM), and mGluR4a (KB = 77 +/- 9 microM), the representative members of group I, II and III mGluRs, respectively. Two other isomers, ACPT-I (18) and (+)-(3S,4S)-ACPT-III [(+)-20], were potent agonists at the group III receptor mGluR4a (EC50 = 7.2 +/- 2.3 and 8.8 +/- 3.2 microM) and competitive antagonists with low affinity for mGluR1a and mGluR2 (KB > 300 microM). Finally, (-)-(3R,4R)-ACPT-III [(-)-20] was a competitive antagonist with poor but significant affinity for mGluR4a (KB = 220 microM). These results demonstrate that the addition of a third carboxylic group to ACPD can change its activity (from agonist to antagonist) and either increase or decrease its selectivity and/or affinity for the various mGluR subtypes.


Assuntos
Ciclopentanos/síntese química , Agonistas GABAérgicos/síntese química , Antagonistas GABAérgicos/síntese química , Receptores de Glutamato Metabotrópico/antagonistas & inibidores , Ácidos Tricarboxílicos/síntese química , Animais , Ligação Competitiva , Linhagem Celular , Células Cultivadas , Cerebelo/efeitos dos fármacos , Cerebelo/fisiologia , Ciclopentanos/química , Ciclopentanos/farmacologia , Agonistas GABAérgicos/química , Agonistas GABAérgicos/farmacologia , Antagonistas GABAérgicos/química , Antagonistas GABAérgicos/farmacologia , Humanos , Indicadores e Reagentes , Inositol/metabolismo , Fosfatos de Inositol/metabolismo , Cinética , Camundongos , Conformação Molecular , Estrutura Molecular , Neurônios/efeitos dos fármacos , Neurônios/fisiologia , Receptores de Glutamato Metabotrópico/classificação , Receptores de Glutamato Metabotrópico/metabolismo , Proteínas Recombinantes/metabolismo , Estereoisomerismo , Relação Estrutura-Atividade , Transfecção , Ácidos Tricarboxílicos/química , Ácidos Tricarboxílicos/farmacologia
4.
J Chem Ecol ; 22(6): 1103-21, 1996 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-24225931

RESUMO

(Z,E)-9,11-tetradecadienal (Z9,E11-14: Ald; 11%), (Z,E)-9,11,13-tetradecatrienal (Z9,E11, 13-14: Ald; 67%), (Z,E)-9,11-tetradecadienyl acetate (Z9,E11-14: Ac, 5.5%), and (Z,E)-9,11,13-tetradecatrienyl acetate (Z9,E11,13-14: Ac; 16.5%) were identified in the extracts of female pheromone glands ofStenoma cecropia (Lepidoptera: Elachistidae). From electroantennograms and single sensillum recordings, receptors toZ9,E11,13-14:Ald andZ9,E11-14: Ald were found on male antenna. Behavioral data were obtained from olfactometric tests in the laboratory and field trapping experiments in Colombia. It appeared that a blend ofZ9,E11,13-14:Ald (83%) andZ9,E11-14:Ald (17%) was attractive to males. These aldehydes are assumed to be components of the sex pheromone ofS. cecropia, whereas the acetates found in gland extracts might be precursors of the pheromone.

5.
J Chem Ecol ; 20(3): 489-503, 1994 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-24242106

RESUMO

Pest monitoring and control of the codling moth,Cydia pomonella L., have been developed using the main pheromone component of this species, (E,E)-8,10-dodecadienol (codlemone). However, the activity of codlemone is not satisfactory for pest control by mating disruption. Thus, we have synthesized halogenated analogs of codlemone to see if they could be used as new agents for pest control of the codling moth. Their biological activity was measured by electrophysiological techniques. In EAG screening, codlemone was the most active compound. F(10,11)-codlemone [(E,E)-10,11-difluoro-8,10-dodecadienol] and Cl-codlemone [(E,E)-11-chloro-8,10-undecadienol] elicited significant EAG responses, F(10,11)-codlemone triggering responses not significantly different from responses to codlemone. EAG cross-adaptation experiments and single sensillum recordings revealed that these compounds were detected by the same receptor neuron type as codlemone. No competitive inhibition with codlemone was observed from nonactive compounds. In field trapping, F(10,11)-codlemone and Cl-codlemone were more attractive to male codling moths than codlemone itself. Possible explanations of this activity are discussed.

6.
J Chem Ecol ; 18(2): 183-96, 1992 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-24254908

RESUMO

The workers of the leaf-cutting antAtta laevigata were found to mark a territory around their nest and along trunk trails. Elsewhere, we reported that the territorial mark had orientation and agonistic functions. The presence of this mark induced an alarm behavior in intruder workers and stimulated the residents' aggressiveness. Of the parts of the body tested, only the extracts from gaster or Dufour gland were able to induce the same agonistic behavior. The compoundsn-heptadecane, (Z)-9-nonadecene, 8,11-nonadecadiene, and (Z)-9-tricosene, secreted by Dufour gland were identified on foraging trails in the field as components of the territorial odor.

SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...