基因组胺H1受体介导的NMDA受体调节信号响应
1Université de Paris, SPPIN - Saints-Pères Paris Institute for the Neurosciences, CNRS, Paris, France.
Pharmacology research & perspectives
|October 8, 2024
概括
组胺H1受体通过与NMDA受体相互作用来影响. 反向激动剂延迟NMDA循环,可能解释前性作用,而组胺激活显示抗性质.
科学领域:
- 神经科学是一个神经科学.
- 药理学 药理学是指药理学的学科.
背景情况:
- 是一种神经系统疾病,其特点是经常性发作.
- 组胺H1受体在神经元刺激性中起作用.
- 在中H1受体的构成性活性尚未完全理解.
研究的目的:
- 为了研究组胺H1受体在中的作用.
- 探索H1受体激动剂和逆激动剂对神经元培养中的NMDA和GABA电流的影响.
- 在的背景下阐明H1和NMDA受体之间的相互作用.
主要方法:
- 使用初级神经元培养来研究NMDA或GABA诱导的电流过剩.
- 评估了H1受体逆agonists (mepyramine,triprolidine) 和一个agonist (2,3-bromophenyl histamine) 的作用.
- 通过免疫光检测检查了NMDA和H1受体的同位化.
- 用选择性免疫试验测量了内源性组胺水平.
主要成果:
- H1受体逆agonists增加了NMDA电流,并延迟了其运行,这表明它具有前效应.
- 胰岛素管理逆转了逆agonists的效果,表明构成性H1受体活性.
- 发现H1和NMDA受体在大多数培养神经元中都具有同位素.
- 基因组胺和逆激动剂都没有影响GABA循环.
结论:
- 组胺H1受体与NMDA受体相互作用,影响神经元刺激性.
- 反向激动剂对H1受体的非激活可能导致发作中的前性效应.
- 构成性H1受体活性和组胺激活表明在调节活动中发挥作用,可能通过抗机制.
相关概念视频
Ligand-Gated Ion Channel Receptor: Gating Mechanism
2.2K
Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
2.2K
Ligand-gated Ion Channels
12.2K
Ligand-gated ion channels are transmembrane proteins with a channel for ions to pass through and a binding site for a ligand. The channel opens only when a ligand attaches to the binding site.
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that...
Three Subfamilies of Ligand-gated Ion Channels
Ligand-gated ion channels fall into three subfamilies. The 'Cys-loop' includes the nicotinic acetylcholine receptors, γ-aminobutyric acid (GABA), glycine, and 5-hydroxytryptamine receptors. The second one is the 'Pore-loop' channels that...
12.2K
Drugs Acting on Autonomic Ganglia: Stimulants
1.3K
Ganglionic stimulants activate NM nicotinic receptors in autonomic ganglia, falling into two categories: nicotine mimetics [e.g., lobeline, dimethylpiperazine, tetramethylammonium] and muscarinic receptor agonists [e.g., muscarine, methacholine]. The first category's action is rapid and blocked by nicotinic receptor antagonists, while the second category's action is delayed and blocked by atropine-like agents. Nicotine, an alkaloid, affects the heart rate by stimulating...
1.3K
Excitatory and Inhibitory Effects of Neurotransmitters
9.9K
When an action potential reaches the presynaptic axon terminal, it releases neurotransmitters from the neuron into the synaptic cleft at a chemical synapse. The released neurotransmitter can be excitatory or inhibitory. The critical criteria commonly used to determine whether a molecule is a neurotransmitter at a chemical synapse are the molecule's presence in the presynaptic neuron. Second, its release is in response to strong presynaptic depolarization. And lastly, the presence of...
9.9K
Neurochemical Transmission: Sites of Drug Action
2.1K
Neurochemical transmission, the conduction of electrical impulses between neurons mediated by neurotransmitters, plays a vital role in various physiological processes. Autonomic drugs exert their effects by modulating neurotransmission within the autonomic nervous system. For instance, drugs such as hemicholinium block the precursor uptake necessary for synthesizing acetylcholine, an essential autonomic neurotransmitter. Following synthesis, neurotransmitters are stored in vesicles. Metyrosine...
2.1K
Acid Suppressive Drugs for Peptic Ulcer Disease: Histamine H2-Receptor Antagonists
409
Histamine H2 receptors, which are intricately located on the basolateral membrane of parietal cells, play a crucial role in modulating gastric acid secretion. When released from enterochromaffin-like cells, histamine engages H2 receptors, initiating the cyclic AMP (cAMP) pathway. In this pathway, adenylyl cyclase converts ATP into cAMP, elevating intracellular cAMP levels. The activation of protein kinase A follows, stimulating the proton pump. This stimulation prompts the secretion of hydrogen...
409


