排序方式: 共有27条查询结果,搜索用时 15 毫秒
1.
Jean-Charles Schwartz Sverine Morisset Agns Rouleau Joël Tardivel-Lacombe Florence Gbahou Xavier Ligneau Anne Hron Astrid Sasse Holger Stark Walter Schunack Robin C. Ganellin Jean-Michel Arrang 《European neuropsychopharmacology》2001,11(6)
The histamine H3 receptor was characterized in the 1980s as an autoreceptor regulating histamine release in brain. Since then, selective drugs have been designed, many of them displaying a high potency in vivo, and used in many studies to delineate the implications of cerebral histaminergic systems in physiological functions such as arousal or cognitive functions. The recent cloning of the H3 receptor, more than 15 years later, has allowed to start molecular studies that led to important findings for optimization of drug design. In agreement some ligands display distinct affinities for the recombinant rat and human H3 receptors, a difference that we assign to two amino acids in the third transmembrane domain. In addition, H3 autoreceptors present in the brain display high constitutive activity including in vivo. As a consequence, inverse agonists enhance histamine neuron activity and constitute a novel potential therapeutic approach to schizophrenia and Alzheimer’s disease. 相似文献
2.
Maya Ando-Yamamoto Hiroshi Kiyama Hideyuki Hayashi Hiroyuki Fukui Masaya Tohyama Takehiko Watanabe Wada Hiroshi 《Brain research》1987,410(2)
The existence ofl-histidine decarboxylase (HDC, EC 4.1.1.22)-like immunoreactive (HDC-I) cells in guinea pig retina was demonstrated using antiserum raised against HDC purified from fetal rat liver. The anti-HDC antiserum partially cross-reacted guinea pigl-DOPA decarboxylase (DDC, EC 4.1.1.28), so the histaminergic neurons ware carefully identified. (1) Comparison of HDC-I and DDC-like immunoreactive (DDC-I) cell types in adjacent sections revealed that HDC-I structures were found in some horizontal cells and amacrine cells, and (2) double-staining procedures with anti-HDC antiserum and monoclonal anti-DDC antibody showed that HDC-I horizontal cells had no DDC-I structures, but all the HDC-I amacrine cells had DDC-I structures. From the results, some horizontal cells (with HDC-like immunoreactivities but without DDC-like immunoreactivities) were concluded to be histaminergic. 相似文献
3.
The influence of pharmacological modifications of the functional activity of the central histaminergic system was studied on the susceptibility of mice to pentylenetetrazolinduced minimal (clonic) and maximal (tonic) seizures. Enhancement in the functional activity of the system by central administration of histamine or 4-methylhistamine or peripheral l-histidine loading failed to modify the risk of seizures. By contrast, reduction in histaminergic function was found to alter seizure susceptibility. Brocresine, an inhibitor of histamine synthesis, decreased and increased the risk of pentylenetetrazol-induced minimal and maximal seizures, respectively. Many, but not all, classical antihistamines (H1 antagonists) and metiamide (H2 antagonist) increased minimal seizure susceptibility after peripheral and intraventricular administration, respectively. 相似文献
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The present study investigated the effect of interactions between histamine receptor agents and the opioid peptidergic system on memory retention of passive avoidance learning in rats. Post-training intracerebroventricular (i.c.v.) injections were carried out in all the experiments. Administration of histamine (20 micro g/rat) reduced, but the histamine H(1) receptor antagonist, pyrilamine (20 and 50 micro g/rat), and the histamine H(2) receptor antagonist, cimetidine (10 and 50 micro g/rat), increased memory retention in rats. The histamine receptor antagonists decreased the response induced by histamine. Morphine (1-10 micro g/rat) reduced, while pentazocine (5 and 10 micro g/rat) or the opioid receptor antagonist, naloxone (5 and 15 micro g/rat), increased memory retention. The combination of histamine with morphine showed potentiation. Effects of pyrilamine and cimetidine were attenuated by morphine. The responses to pentazocine and naloxone also were decreased by histamine. It is concluded that the histaminergic system has an interaction with opioidergic system that is involved in the memory retention process. 相似文献
6.
R. Tamiya M. Hanada N. Narita S. Inagaki M. Tohyama H. Takagi 《Experimental brain research. Experimentelle Hirnforschung. Expérimentation cérébrale》1994,79(2):261-265
Summary The synaptic connections between histaminergic neurons and substance P (SP) afferents in the caudal magnocellular nucleus (CM) of the hypothalamus were examined using an immunoelectron microscopic mirror method. SP-immunoreactive (SP-IR) terminals made synaptic contacts with the somata, somatic spines and dendrites of histidine decarboxylase immunoreactive (HDC-IR) neurons. This suggests that SP afferents exert monosynaptic influence on the central histaminergic neuronal system. 相似文献
7.
Shan L Bossers K Luchetti S Balesar R Lethbridge N Chazot PL Bao AM Swaab DF 《Neurobiology of aging》2012,33(7):1488.e1-1488.13
Earlier studies showed neuronal histamine production in the hypothalamic tuberomamillary nucleus to be unchanged in Parkinson's disease (PD), whereas the histamine levels and innervation in the substantia nigra (SN) increased. In the present study we used quantitative polymerase chain reaction (qPCR) to assess the changes in the histaminergic system in the SN, caudate nucleus (CN), and putamen (PU) in 7 PD patients and 7 controls. The messenger RNA (mRNA) expression of the histamine receptor-3 (H(3)R), which was localized immunocytochemically in the large pigmented neurons, was significantly decreased in the SN in PD, while histamine receptor-4 (H(4)R)-mRNA expression showed a significant increase in caudate nucleus and PU. In addition, significantly increased mRNA levels of histamine methyltransferase (HMT), a key enzyme involved in histamine metabolism, were found in the SN and in the PU in PD. Moreover, in the SN, the histamine methyltransferase-mRNA showed a strong negative correlation with PD disease duration. Our observations imply the presence of local changes in the histaminergic system that may contribute to PD pathology, and may thus provide a rationale for possible novel therapeutic strategies. 相似文献
8.
J. Costa Neto K.R. Serafim A.C.L. Gianloren?o R. Mattioli 《Brazilian journal of medical and biological research》2013,46(11):943-948
The present study investigated the effect of thioperamide (THIO), an H3
histaminergic receptor antagonist, microinjected into the cerebellar vermis on
emotional memory consolidation in male Swiss albino mice re-exposed to the elevated
plus-maze (EPM). We implanted a guide cannula into the cerebellar vermis using
stereotactic surgery. On the third day after surgery, we performed behavioral tests
for two consecutive days. On the first day (exposure), the mice (n=10/group) were
exposed to the EPM and received THIO (0.06, 0.3, or 1.5 ng/0.1 µL) immediately after
the end of the session. Twenty-four hours later, the mice were re-exposed to the EPM
under the same experimental conditions, but without drug injection. A reduction in
the exploration of the open arms upon re-exposure to the EPM (percentage of number of
entries and time spent in open arms) compared with the initial exposure was used as
an indicator of learning and memory. One-way analysis of variance (ANOVA) followed by
the Duncan post hoc test was used to analyze the data. Upon
re-exposure, exploratory activity in the open arms was reduced in the control group,
and with the two highest THIO doses: 0.3 and 1.5 ng/0.1 µL. No reduction was seen
with the lowest THIO dose (0.06 ng/0.1 µL), indicating inhibition of the
consolidation of emotional memory. None of the doses interfered with the animals''
locomotor activity. We conclude that THIO at the lowest dose (0.06 ng/0.1 µL)
microinjected into the cerebellum impaired emotional memory consolidation in
mice. 相似文献
9.
Previous studies have demonstrated that neuromedin U (NMU) affects cardiovascular functions such as blood pressure (BP) or heart rate (HR) in rats. Here, we examined the effects of the lateral cerebral ventricular (ICV) injection of various doses of NMU on renal sympathetic nerve activity (RSNA) and BP in urethane-anesthetized rats. ICV injection of NMU elevated RSNA, BP and HR in a dose-dependent manner.Moreover, neither ICV pretreatment of thioperamide, an antagonist of histaminergic H3-receptor, or of diphenhydramine, an antagonist of histaminergic H1-receptor, abolished increasing effects of NMU on RSNA, BP and HR In addition, ICV injection of NMU suppressed gastric vagal nerve activity (GVNA) and activated brown adipose tissue sympathetic nerve activity (BAT-SNA) of anesthetized rats, and elevated brown adipose tissue temperature (BAT-T) of conscious rats. Thus, these evidence suggest that NMU affects neural activities of autonomic nerves containing RSNA, GVNA or BAT-SNA, and BP by mediating central mechanism. 相似文献
10.
The cerebellum has been considered only as a classical subcortical center for motor control. However, accumulating experimental and clinical evidences have revealed that the cerebellum also plays an important role in cognition, for instance, in learning and memory, as well as in emotional behavior and in nonsomatic activities, such as visceral and immunological responses. Although it is not yet clear through which pathways such cerebellar nonsomatic functions are mediated, the direct bidirectional connections between the cerebellum and the hypothalamus, a high autonomic center, have recently been demonstrated in a series of neuroanatomical investigations on a variety of mammals and indicated to be potential pathways underlying the cerebellar autonomic modulation. The direct hypothalamocerebellar projections originate from the widespread hypothalamic nuclei/areas and terminate in both the cerebellar cortex as multilayered fibers and the cerebellar nuclei. Immunohistochemistry studies have offered fairly convincing evidence that some of these projecting fibers are histaminergic. It has been suggested that through their excitatory effects on cerebellar cortical and nuclear cells mediated by metabotropic histamine H(2) and/or H(1) receptors, the hypothalamocerebellar histaminergic fibers participate in cerebellar modulation of somatic motor as well as non-motor responses. On the other hand, the direct cerebellohypothalamic projections arise from all cerebellar nuclei (fastigial, anterior and posterior interpositus, and dentate nuclei) and reach almost all hypothalamic nuclei/areas. Neurophysiological and neuroimaging studies have demonstrated that these connections may be involved in feeding, cardiovascular, osmotic, respiratory, micturition, immune, emotion, and other nonsomatic regulation. These observations provide support for the hypothesis that the cerebellum is an essential modulator and coordinator for integrating motor, visceral and behavioral responses, and that such somatic-visceral integration through the cerebellar circuitry may be fulfilled by means of the cerebellar-hypothalamic circuits. 相似文献