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The binding affinities and selectivities of antagonists Figure 1 and Scheme 2 for the α1A-adrenoceptor are dependent on the stereochemical orientation of the groups at the C-4 and C-5 positions of the oxazolidinone ring. The unambiguous assignment of the relative and absolute configurations of the diastereomers of SNAP 7915 (Figure 1 and Scheme 2) is reported.  相似文献   
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By means of radioimmunoassay a clear-cut peak of melatonin concentration was found in the pineal organ of the pigeon at the middle of the scotophase (Coisin et al. 1982a). The aim of the present study was to identify the cell type responsible for the nocturnal indole metabolism, including melatonin synthesis, in the pineal of this avian species. After a short-term incubation or organ culture in the presence of [3H]-indolic precursors, [3H]-5-hydroxytryptophan or [3H]-5-hydroxytryptamine, the relative amounts of deaminated and acetylated products occurring in the pineal organ were measured by the use of thin layer chromatography and liquid-scintillation counting. It was possible to modify the relative amounts of deaminated and acetylated indoles by the application of some inhibitors of monoamine oxidase and cyclic nucleotide phosphodiesterase. Irrespective of the experimental conditions, high-resolution autoradiography combined with the above-mentioned radiochemical experiments showed that the cells of the receptor line (modified photoreceptor cells) are responsible for indole storage and metabolism, and very probably also for melatonin biosynthesis. The other cell types of the pineal parenchyma did not display significant labeling.  相似文献   
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Vocalizations of South African clawed frogs are produced by contractions of laryngeal muscles innervated by motor neurons of the caudal medulla (within cranial nerve nucleus IX-X). We have traced afferents to laryngeal motor neurons in male and female frogs using retrograde axonal transport of horseradish peroxidase conjugated to wheat germ agglutinin (HRP-WGA). After iontophoretic injection of HRP-WGA into n. IX-X, retrogradely labelled neurons were seen in the contralateral n. IX-X, in rhombencephalic reticular nuclei, and in the pre-trigeminal nucleus of the dorsal tegmental area (DTAM) of both males and females.  相似文献   
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Type B photoreceptors of the nudibranch mollusc Hermissenda crassicornis receive excitatory synaptic potentials (EPSPs) whose frequency is controlled by potential changes of a neighboring cell known as the S optic ganglion cell which is thought to be electrically coupled to the presynaptic source of these EPSPs, the E optic ganglion cell. The frequency of the EPSPs increases when a conditioned stimulus (light) is paired with an unconditioned stimulus (rotation) during acquisition of a Pavlovian conditioned response. The results of the present study are consistent with an adrenergic origin for these EPSPs. Noradrenergic agonists (greater than 100 microM), norepinephrine and clonidine, only slightly depolarize the type B cell but clearly prolong its depolarizing response to light. Serotonin, by contrast, causes hyperpolarization of the type B cell's resting potential as well as after a light step. Clonidine reduces voltage-dependent outward K+ currents (IA, an early current, ICa2+-K+, a late Ca2+-dependent current) that control the type B cell's excitability (and thus its light response and membrane potential). These effects of clonidine are reduced or blocked by the alpha 2-receptor antagonist, yohimbine (0.5 microM), but not the alpha 1-blocker, prazosin. The same yohimbine concentration also blocked depolarizing synaptic excitation of the type B cell in response to depolarization of a simultaneously impaled S optic ganglion cell. Histochemical techniques (both the glyoxylic acid method of de la Torre and Surgeon and the formaldehyde-induced fluorescence or Falck-Hillarp method) demonstrated the presence of a biogenic amine(s) within a single neuron in each optic ganglion as well as three or four cells within the vicinity of previously identified visual interneurons. No serotonergic neurons were found within the optic ganglion or in proximity to visual interneurons. A clonidine-like synaptic effect on type B cells, therefore, could amplify conditioning-specific changes of membrane currents by increasing type B depolarization and possibly, as well, by elevating intracellular second messengers.  相似文献   
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A total of 48 French villages were selected for a survey of water quality from February 1983 to June 1984 as part of an epidemiological study conducted in the rural area of the Rh?ne-Alpes region. Water samples were collected and analyzed on a weekly basis in each village. Bacteriological analysis of each water sample included enumeration of standard plate count bacteria, total and thermotolerant coliforms, and fecal streptococci. The water quality regulations are examined as to the analysis frequency, the volume of samples, and the relationship between the various bacterial indicators. Analyzing 300-ml, instead of 100-ml, samples tends to generate better information on single water samples. However, if many samples are analyzed over time from the same community, the value of using large volumes of water samples is diminished. The comparisons between bacterial indicators showed that the information obtained from the various indicators was very similar. However, fecal streptococci had a better predictive value of a negative test than coliforms with respect to the French standards.  相似文献   
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