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1.
Fertilization initiates in the egg a dramatic increase in intracellular calcium that opens ion channels and causes exocytosis. To explore the possibility that these events might involve a receptor-mediated pathway, receptors for serotonin or acetylcholine (M1 muscarinic) were expressed in the Xenopus egg; serotonin or acetylcholine then could initiate a series of responses similar to those normally initiated by sperm. Thus, there may be an endogenous receptor in the egg membrane that is activated by sperm, and the serotonin or M1 muscarinic receptor may replace the sperm receptor in this pathway.  相似文献   

2.
The effects of long-term lithium administration on pre- and postsynaptic processes involved in serotonergic neurotransmission were measured in rat hippocampus and cerebral cortex. Long-term lithium administration increased both basal and potassium chloride-stimulated release of endogenous serotonin from the hippocampus but not from the cortex. Serotonergic receptor binding was reduced in the hippocampus but not in the cortex. These results suggest a mechanism by which lithium may stabilize serotonin neurotransmission.  相似文献   

3.
Neurotransmitter receptors are usually restricted to neuronal cells, but the signaling pathways activated by these receptors are widely distributed in both neural and non-neural cells. The functional consequences of activating a brain-specific neurotransmitter receptor, the serotonin 5HT1c receptor, in the unnatural environment of a fibroblast were examined. Introduction of functional 5HT1c receptors into NIH 3T3 cells results, at high frequency, in the generation of transformed foci. Moreover, the generation and maintenance of transformed foci requires continued activation of the serotonin receptor. In addition, the injection of cells derived from transformed foci into nude mice results in the generation of tumors. The serotonin 5HT1c receptor therefore functions as a protooncogene when expressed in NIH 3T3 fibroblasts.  相似文献   

4.
对5-羟色胺及其受体进行介绍,并阐述了昆虫5-羟色胺受体结构和功能以及5-HT受体的信号转导机制的国内外研究现状及其发展动态。最后,分析基于5-羟色胺受体分子靶标的新药剂的研发现状。  相似文献   

5.
The role of serotonin axons in modulating the norepinephrine neurotransmission system in rat brain was investigated. Selective lesions of the forebrain serotonergic system were made by injecting 5,7-dihydroxytryptamine into the midbrain raphe nuclei. Four to six weeks after the lesion, the uptake of 3H-labeled serotonin in the frontal cortex and the hippocampus was reduced by more than 90 percent, while neither the uptake of 3H-labeled norepinephrine nor the content of norepinephrine was affected in either tissue. The number of beta-adrenergic receptors, as measured by radioligand binding with 3H-labeled dihydroalprenolol, was increased in the frontal cortex and hippocampus of rats with lesions. Similarly, specific lesions of central serotonin axons produced by systemically administered p-chloramphetamine resulted in an increase in the binding of 3H-labeled dihydroalprenolol to beta-adrenergic receptors and in the production of adenosine 3',5'-monophosphate in response to isoproterenol. These results indicate that serotonin axons may regulate beta-adrenergic receptor number and function in brain.  相似文献   

6.
Antidepressants compete at several neurotransmitter receptor binding site, but drug affinities do not correlate with clinical efficacy. Long-term, but not short-term, antidepressant treatment decreases the numbers of both serotonin and beta-adrenergic receptors. The decrease in the number of receptor sites is most marked for [3H]spiroperidol-labeled serotonin receptors and is characteristic for antidepressants of several classes.  相似文献   

7.
Various chronic antidepressant treatments increase adult hippocampal neurogenesis, but the functional importance of this phenomenon remains unclear. Here, using genetic and radiological methods, we show that disrupting antidepressant-induced neurogenesis blocks behavioral responses to antidepressants. Serotonin 1A receptor null mice were insensitive to the neurogenic and behavioral effects of fluoxetine, a serotonin selective reuptake inhibitor. X-irradiation of a restricted region of mouse brain containing the hippocampus prevented the neurogenic and behavioral effects of two classes of antidepressants. These findings suggest that the behavioral effects of chronic antidepressants may be mediated by the stimulation of neurogenesis in the hippocampus.  相似文献   

8.
The pathophysiology of depression remains enigmatic, although abnormalities in serotonin signaling have been implicated. We have found that the serotonin 1B receptor [5-hydroxytryptamine (5-HT1B) receptor] interacts with p11. p11 increases localization of 5-HT1B receptors at the cell surface. p11 is increased in rodent brains by antidepressants or electroconvulsive therapy, but decreased in an animal model of depression and in brain tissue from depressed patients. Overexpression of p11 increases 5-HT1B receptor function in cells and recapitulates certain behaviors seen after antidepressant treatment in mice. p11 knockout mice exhibit a depression-like phenotype and have reduced responsiveness to 5-HT1B receptor agonists and reduced behavioral reactions to an antidepressant.  相似文献   

9.
Molecular biology of synaptic receptors   总被引:18,自引:0,他引:18  
A special proteolipid (a hydrophobic protein) has been extracted and purified from nerve-ending membranes and total particulate matter of gray areas of the central nervous system. Such a proteolipid shows a high affinity for binding d-tubocurarine, serotonin, and atropine and has been called receptor proteolipid. The interaction of this proteolipid with atropine sulfate was studied with light scattering and polarization of fluorescence. The changes observed, which follow a cooperative type of curve, were attributed to the aggregation of the proteolipid macromolecules. Such a phenomenon was then observed under the electron microscope. A receptor proteolipid having a high affinity for binding acetylcholine, hexamethonium, and other cholinergic drugs was isolated and purified from electric tissue of fishes and from electroplax membranes. Such a proteolipid was also extracted from membranes from which acetylcholinesterase had been removed, and it was concluded that this enzyme and the receptor proteolipid are two different macromolecules. A high affinity binding site with a dissociation constant of K1 equal to 10(-7) and about ten sites with K2 equal to 10(-5) were recognized in the receptor proteolipid. Under the electron microscope the receptor proteolipid of brain appears as a rod-shaped macromolecule which may assume paracrystalline arrays with 10(-8) molar atropine sulfate. Similarly the receptor proteolipid from electric tissue and from skeletal muscle may form paracrystalline arrays under the action of acetylcholine and hexamethonium. A model of the cholinergic receptor based on the properties of the proteolipid is presented. Preliminary work indicates the possibility of obtaining a biophysical response to acetylcholine when the receptor proteolipid is embedded in artificial bilayered lipid membrance.  相似文献   

10.
The activity of N-acetyltransferase in the rat pineal gland is more than 15 times higher at night than during the day. This circadian rhythm persists in complete darkness, or in blinded animals, and is suppressed in constant lighting. The N-acetyltransferase rhythm is 180 degrees out of phase with the serotonin rhythm and is similar to the norepinephrine and melatonin rhythms. Experiments in vitro indicate that norepinephrine, not serotonin, regulates the activity of N-acetyl-transferase through a highly specific receptor.  相似文献   

11.
The anxiety-reducing effects of minor tranquilizers in the rat conflict test were mimicked by serotonin antagonists and by p-chlorophenylalanine, an inhibitor of serotonin synthesis; the depressant effects of the minor tranquilizers were mimicked by norepinephrine antagonists. Intraventricular injections of serotonin led to a suppression of behavior, and also antagonized the anxiety-reducing action of benzodiazeprines. Intraventricular injections of norepinephrine led to a release of punished behavior from suppression, and also antagonized the depressant action of benzodiazepines. The anxiety-reducing activity, and the decrease in serotonin turnover induced by benzodiazepines, were maintained over repeated doses, whereas depressant activity, and the decrease induced in norepinephrine turnover, both rapidly underwent tolerance. Tranquilizers may exert their anxiety-reducing effects by a reduction of serotonin activity in a behaviorally suppressive punishment system, and they may exert their depressant effects by a reduction of norepinephrine activity in a behaviorally facilitatory reward system.  相似文献   

12.
一个重要的精子受体—猪透明带糖蛋白β-D-半乳糖残基   总被引:1,自引:0,他引:1  
 【目的】证明末端半乳糖残基在猪透明带糖蛋白中的分布以及它在精子结合和侵入中的作用。【方法】体外成熟的猪卵母细胞去除周围卵丘细胞,用异硫氰酸荧光素(fluorescein isothiocyanate,FITC) 络合西非单叶豆凝集素(Bandeiraea simplicifolia lectin-I,BS-I) 或蓖麻凝集素(Ricinus communis agglutinin,RCA-I)处理30min,分别观察末端-D-半乳糖残基或-D-半乳糖残基在透明带中的定位分布。荧光显微镜观察显示,BS-I和RCA-I都标记于整个透明带上且比较集中于透明带的外层,其中BS-I显示微弱荧光反应,而RCA-I呈强荧光反应且在透明带的外层反应尤为强烈。植物凝集素处理的卵母细胞用于体外受精,分别在受精2h或12h观察精-卵结合和精子入卵情况。【结果】RCA-I处理组卵母细胞平均精子结合数显著低于对照组(18 vs 95),而精子入卵则完全被阻断;可是BS-I处理组的卵母细胞的精子结合数少量被抑制(59 vs 95),而且精子入卵率与对照组无显著差异。【结论】猪透明带末端-D-半乳糖残基作为精子受体的重要组成成分,参与精-卵结合和受精。  相似文献   

13.
Entamoeba histolytica causes intestinal secretion: role of serotonin   总被引:4,自引:0,他引:4  
Lysates of the protozoan parasite Entamoeba histolytica altered active electrolyte transport when present on the serosal surface of rabbit ileum and rat colon. The lysate-induced effects on electrolyte transport were similar to those caused by serotonin, and were blocked by bufotenine, an analog known to inhibit the action of serotonin. The transport effects were partially inhibited by antibody to serotonin. The amebic lysates were shown to contain serotonin by radioimmunoassay, high-performance liquid chromatography, and thin-layer chromatography. These results suggest that the serotonin present in Entamoeba histolytica may be important in the diarrhea seen in amebiasis.  相似文献   

14.
L-Dopa-induced release of cerebral monoamines   总被引:10,自引:0,他引:10  
L-Dopa markedly increased the efflux of tritiated dopamine and tritiated serotonin from rat brain slices. This action appeared contingent on the decarboxylation of L-dopa to dopamine, since it could be blocked by an inhibitor of L-amino acid decarboxylase. Selective destruction of catecholamine-containing nerve terminals by 6-hydroxydopamine significantly decreased the uptake and release of tritiated dopamine but not that of tritiated serotonin. These observations support the hypothesis that a portion of exogenously administered L-dopa may enter central serotonin terminals and undergo decarboxylation to the amine with resultant displacement of the endogenous indoleamine from vesicular stores.  相似文献   

15.
Effects of serotonin on memory impairments produced by ethanol   总被引:1,自引:0,他引:1  
Subjects treated with low or high doses of ethanol demonstrated impaired memory, particularly in tests involving the recall of poorly learned information. Zimelidine, an inhibitor of serotonin reuptake, reversed this ethanol-induced impairment. The serotonin neurotransmitter system may mediate learning and memory in humans and may determine some of the effects of alcohol on higher mental functions.  相似文献   

16.
Vascular smooth muscle reactivity in normotensive and hypertensive rats   总被引:2,自引:0,他引:2  
Aortic strips from spontaneously hypertensive rats were less responsive than normal animals to the contractile effects of norepinephrine, serotonin, and potassium chloride but more reactive to the relaxant effects of the stimulant of beta receptors, isoproterenol. Thus, hypertension is not the result of an absence of beta receptor or a hypersensitivity of the vascular smooth muscle.  相似文献   

17.
The histochemical fluorescence of those neurons in brainstem raphe nuclei which are presumed to contain serotonin is selectively and stereospecifically enhanced by L-tryptophan at doses that also produce an elevation in the concentration of serotonin. However, contrary to our assumptions, the increase in raphe fluorescence is not prevented by p-chlorophenylalanine, an inhibitor of serotonin synthesis. These results suggest that under some conditions derivatives of tryptophan other than, or in addition to, serotonin may be of significance in raphe neurons.  相似文献   

18.
试验研究了用于检测磺胺二甲基嘧啶(SM2)残留的免疫生物传感器的最关键组成,即感受器部件的制备方法、最佳检测条件,并对所制备感受器部件的性能进行了测试。利用二醋酸纤维素作为载体支架结构,戊二醛为交联剂,己二胺为制孔剂,制备了最佳条件符合标准的载体膜。采用双盲评分法测定其性能,选取性能良好的载体膜包被SM2抗体制成抗体膜。将酶标抗原和SM2标准品联到抗体膜上,应用溶解氧分析仪测定体系中过氧化氢减少量。结果表明,质控膜和测定膜的电流变化值差异显著(P<0.05),感受器部件反应灵敏,最低检测限达5μg·L-1。  相似文献   

19.
Rats with electrodes implanted in the medial forebrain bundle stimulated their own brains at sharply reduced rates after systemic administration of disulfiram or intraventricular administration of diethyldithiocarbamate. Both drugs inhibit dopamine-beta-hydroxylase, the enzyme responsible for the final step in the biosynthesis of norepinephrine. The suppressed behavior was reinstated by intraventricular injections of 1-norepinephrine, but not by injection of its biologically inactive isomer, d-norepinephrine. Intraventricular administration of dopamine and serotonin did not restore self-stimulation. The rewarding effect of medial forebrain bundle stimulation may depend on the availability of norepinephrine as a transmitter, but not on dopamine or serotonin.  相似文献   

20.
The aspartate receptor of Escherichia coli and Salmonella typhimurium is a cell surface sensory transducer that binds extracellular aspartate and sends a transmembrane signal to the inside of the bacterium. The flexibility and allostery of this receptor was examined by placing sulfhydryl groups as potential cross-linking sites at targeted locations in the protein. Seven different mutant receptors were constructed, each containing a single cysteine residue at a different position in the primary structure. Intramolecular disulfide bond formation within oligomers of these mutant receptors is shown to trap structural fluctuations and to detect ligand-induced changes in structure. The results indicate that the receptor oligomer has a flexible, dynamic structure which undergoes a global change upon aspartate binding.  相似文献   

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