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1.
A Tahri-Joutei C Fillion M Bedin J N Hugues G Pointis 《Molecular and cellular endocrinology》1991,79(1-3):R21-R24
Arginine vasopressin (AVP) and beta-endorphin are present within the testis where they could act as paracrine effectors of steroidogenesis. In this study we investigated the effect of naloxone, an opioid receptor antagonist on Leydig cell AVP receptor. Intratesticular injection of increasing doses of naloxone (0.1-100 micrograms) resulted 24 h later in a dose-dependent increase in Leydig cell AVP binding capacity. This effect occurred locally since s.c. injection of similar doses of naloxone did not alter the testicular AVP receptor content and intratesticular injection enhanced AVP receptor density only in the naloxone-treated testis but not in the contralateral vehicle-treated testis. Scatchard plot analysis of the data revealed that naloxone locally injected altered AVP binding capacity without change in affinity. These results suggest that in addition to their known paracrine effects in the testis, endogenous opioid peptides may locally control the testicular AVP system by modulating AVP receptor capacity. 相似文献
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In human cortex and hippocampus area, [3H]5-HT (5 nM) labels 5-HT1A, 5-HT1D and 5-HT1E sites. After masking 5-HT1A receptors by 0.1 μM 8-OH-DPAT, the binding displaced by 0.1 μM 5-CT presumably represented 5-HT1D sites and the remaining binding 5-HT1E sites. In frontal cortex, 5-HT1A receptors represented the main binding in layers II and VI and a lower fraction on other layers. 5-HT1D and 5-HT1E sites, were more homogeneously distributed in layers II to VI (21–34% of specific [3H]5-HT binding). 5-HT1E sites were of similar affinities (KD close to 6–8 nM) in the cortical layers II to VI. In CA1 field of hippocampus, (pyramidal layer, stratum radiatum, molecular layer), CA2 and dentate gyrus, 5-HT1A receptors represented the major fraction, 5-HT1D sites a significant fraction and 5-HT1E a minor fraction of the specific [3H]5-HT binding. In CA3–CA4 fields, 5-HT1A receptors were less densely present, 5-HT1D sites were predominant and 5-HT1E sites represented a significant fraction (27%). The highest densities of 5-HT1E sites have been measured in subiculum, where 5-HT1A, 5-HT1D, and 5-HT1E binding sites were equally represented and in entorhinal cortex where 5-HT1E sites represented the major binding in layer III. They were also present in layers II and IV (29 and 24%) and, to a lesser extent, in layers V and VI. 5-HT1A sites were predominant in layer VI, II and V and were less abundant in other layers. 5-HT1D were homogeneously present in layers II, III, IV and were present in low amounts in other layers. No 5-HT1E were detected in choroid plexus, where [3H]5-HT was dramatically reduced by mesulergine (5-HT2C receptors). No significant displacement of [3H]5-HT by mesulergine was measured in other structures. 相似文献
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Gilles M. B. Fillion Stuart A. Sloragh Brje Uvns 《Acta physiologica (Oxford, England)》1970,78(4):547-560
Fillion , G. M. B., S. A. Slorach and B. Uvnäs . The release of histamine, heparin and granule protein from rat mast cells treated with compound 48/80 i n vitro. Acta physiol. scand. 1970. 78. 547–560. The quantitative relationship between the release of histamine, heparin and granule protein from rat mast cells exposed to compound 48/80 in vitro has been investigated in order to clarify the mechanism of action of this releaser. A correlation was found between the three release curves. The ratio of heparin to granule protein was similar in extruded granules and granules remaining in the cell after compound 48/80 treatment. From these results we conclude that the principal mechanism of histamine release induced by this agent involves an initial extrusion of histamine-containing granules, followed by an exchange of histamine in the granules for cations in the extracellular medium. 相似文献
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Sarciron ME Nebois P Pautet F Pétavy AF Fillion H Walchshofer N 《Parasitology research》2002,88(11):969-971
Quinonic derivatives were tested against a virulent RH strain of Toxoplasma gondii maintained in cell culture in THP-1, a human myelomonocytic cell line. The derivatives were tested at various doses (0.5-4 microg/ml) and compared with the reference molecules clindamycine, sulfadiazine, pyrimethamine and atovaquone. The percentage of parasite growth inhibition was observed after 72 h of incubation. The tested derivatives are bicyclic, tricyclic or tetracyclic quinones. Eight of these compounds exhibit over 70% inhibition of parasite growth; and two were nearly equipotent to pyrimethamine. These data indicate that the most active compounds against the RH strain of T. gondii are bis-heterocyclic quinones. 相似文献