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4.
Bioorg Med Chem ; 4(3): 479-88, 1996 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-8733630

RESUMO

Several analogues of (Z)-8-dodecenyl acetate (1a), the major pheromone component of the Oriental fruit moth, Cydia molesta, with chloroformate and lactone functional groups in place of the acetate moiety, were synthesized and investigated for their biological activity at four evaluation levels, i.e. by electroantennography (EAG), electrosensillography (ESG), short-range sexual stimulation and activation in the flight-tunnel. We found very strict requirements on the shape as well as on the electron distribution of the acetate group for a productive interaction with the receptor. The behavioral results showed that, among the analogues investigated, the chloroformate 1b, alken-4-olide 2a and also dodecyl acetate (1c) possess significant (60-85%) inhibitory activities. Based on electrophysiological evidence demonstrating that (i) only 1b is competing with the major pheromone component 1a for the same receptor sites on the male antennal sensilla, (ii) 1c elicits moderate EAG but no ESG responses and (iii) 2a does not produce any electrophysiological response at all, three possible inhibitory mechanisms by which these analogues are acting could be distinguished.


Assuntos
Ácidos Graxos Monoinsaturados/química , Mariposas/fisiologia , Atrativos Sexuais/química , Animais , Relação Dose-Resposta a Droga , Eletrofisiologia , Masculino , Mimetismo Molecular , Comportamento Sexual Animal , Relação Estrutura-Atividade
6.
Sci Total Environ ; 38: 69-77, 1984 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-6523126

RESUMO

The concentrations of Co, Fe, Rb, Se and Zn were analysed, by means of neutron activation analysis, in the brains of three patients with alcohol abuse, of one patient with endogeneous psychosis and of one patient with schizophrenia. The patients with alcohol abuse suffered from the Wernicke-Korsakoff syndrome. The data were compared with results from brains which were not diseased ("normals"). Patients with alcohol abuse had diminished values of rubidium in nearly all analysed samples of cerebral nuclei (greater than 30% compared to normals), whereas the Rb values were normal or diminished in cortical regions. The cobalt values were reduced (greater than 20%) in eight out of 14 nuclei and in five out of nine cortical regions. Differences in the Fe and Se values were mainly located in the cerebral nuclei. In the caudate nucleus the patient with endogeneous psychosis had highly significant elevated values of all analysed elements. The element concentrations of the patient with schizophrenia did not significantly differ from those of normal controls. The loss of nearly all elements was conspicuous in those regions which show neuro-pathological cell degeneration or atrophy in the case of Wernicke-Korsakoff syndrome. This loss of element concentrations in patients with alcohol abuse is interpreted as a loss of cellular vitality.


Assuntos
Alcoolismo/metabolismo , Química Encefálica , Transtornos Psicóticos/metabolismo , Esquizofrenia/metabolismo , Oligoelementos/análise , Idoso , Transtorno Amnésico Alcoólico/metabolismo , Cobalto/análise , Feminino , Humanos , Masculino , Pessoa de Meia-Idade , Análise de Ativação de Nêutrons , Rubídio/análise , Distribuição Tecidual
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