mAChR

Muscarinic acetylcholine receptors (mAChRs) are a class of G protein-coupled receptors (GPCRs) found in the central and peripheral nervous systems, as well as in various other tissues and organs throughout the body. These receptors are named after muscarine, a natural alkaloid compound found in certain mushrooms, which was one of the first substances discovered to activate them.

There are five subtypes of muscarinic receptors, designated as M1 through M5, each with distinct tissue distribution and functions. Here's an overview of their roles:

  • M1 Receptors: Predominantly found in the central nervous system, particularly in regions associated with cognitive functions. Activation of M1 receptors is linked to memory and learning.
  • M2 Receptors: Found in the heart, where they play a crucial role in regulating heart rate and cardiac contractility. Activation of M2 receptors slows heart rate and reduces the force of cardiac contractions.
  • M3 Receptors: Present in smooth muscle tissues, such as those in the gastrointestinal tract, urinary bladder, and bronchial airways. Activation of M3 receptors leads to smooth muscle contraction.
  • M4 Receptors: Distributed mainly in the central nervous system and involved in modulating neurotransmitter release. Their role in cognition and neuropsychiatric disorders is of interest.
  • M5 Receptors: Located in certain areas of the brain and implicated in the modulation of dopamine release. Research suggests they may be relevant to Parkinson's disease and addiction.

Muscarinic receptors are activated by the neurotransmitter acetylcholine and play a vital role in regulating a wide range of physiological processes, including heart rate, smooth muscle contraction, glandular secretion, and neurotransmitter release. They are targets for various drugs, including anticholinergic agents, which block their activity, and drugs used to treat conditions like bradycardia and neurodegenerative disorders.

Understanding the functions and regulation of muscarinic acetylcholine receptors is essential for developing therapies that modulate their activity and for advancing our knowledge of how they contribute to various physiological and pathological processes in the body.

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  1. Muscarinic receptor agonist

    贝他尼可是一种副交感神经兴奋剂胆碱类氨基甲酸酯,它选择性地刺激毒蕈碱受体,而对烟碱型受体没有任何影响。
  2. M1/M3 receptor agonist

    Cevimeline (AF-102B) 是一种副交感神经兴奋剂毒蕈碱激动剂,对 M3 受体具有特别的作用;用于治疗与sjogren综合症相关的口干症状。
  3. Nicotinic receptor agonist

    Metanicotine 是一种神经性尼古丁受体激动剂,对 α4β2 亚型显示出高度选择性(Ki=26 nM);与 α7 受体相比具有超过1000倍的选择性(Ki=36000 nM)。
  4. mAChR agonist

    AC260584 是一种 M1 毒蕈碱受体异位激动剂,具有 pEC50 为 7.6。
  5. mAChR agonist

    Xanomeline oxalate 是一种强效的毒蕈碱型乙酰胆碱受体激动剂(EC50 值分别为 M1、M2、M3、M4 和 M5 的 0.3、92.5、5、52 和 42 nM)。
  6. M1 mAChR agonist

    TBPB 是一种 M1 mAChR 配体,具有 EC50 值为 89 nM,能够调节淀粉样蛋白的处理,并在大鼠中产生类抗精神病活性。
  7. M2/M4 AChR agonist

    LY2119620 是一种特异性的、变构激动剂,针对人类的 M2 和 M4 乙酰胆碱能毒蕈碱受体
  8. AchR agonist

    Nitenpyram 是一种烟碱型乙酰胆碱受体 (AchR) 激动剂
  9. M1 agonist

    盐酸西维拉明半水合物是一种新型毒蕈碱受体激动剂,是治疗Sjogren综合症中干燥综合症(xerostomia)的候选药物。
  10. Muscarinic receptor agonist

    氯化甲胆碱是一种合成的胆碱酯,它作为副交感神经系统中的非选择性毒蕈碱受体激动剂
  11. mAChR agonist

    Cevimeline (Evoxac) Hcl 是一种副交感神经兴奋剂毒蕈碱激动剂,特别作用于M3受体;用于治疗与Sjogren综合症相关的口干症状。
  12. muscarinic agonist

    Talsaclidine 是一种具有优先神经刺激特性的毒蕈碱激动剂。Talsaclidine 在 M1 亚型上是全激动剂,在 M2 和 M3 亚型上则是部分激动剂。
  13. hM3Dq agonist.

    DREADD 激动剂 21 是一种强效的人类毒蕈碱乙酰胆碱 M3 受体(hM3Dq)激动剂(EC50=1.7 nM)。
  14. Sigma-1 receptor agonist/muscarinic M1 agonist

    Blarcamesine,也被称为 AVex-73 和 AE-37,是一种胆碱能M1受体激动剂,可能用于治疗阿尔茨海默病。它是一个ς受体配体。
  15. mAChR agonist

    Oxotremorine M iodide 是一种强效且非选择性的毒蕈碱乙酰胆碱受体(mAChR)激动剂
  16. hM3Dq DREADD agonist

    Perlapine 是一种强效且选择性的 hM3Dq DREADD 激动剂(EC50 = 2.8 nM)。这种药物对 hM3Dq 的选择性超过 hM3 10,000倍

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