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. mAChR antagonist

    阿托品是毒蕈碱型乙酰胆碱受体M1、M2、M3、M4和M5的竞争性拮抗剂。
  2. muscarinic receptor antagonist

    Biperiden hydrochloride 是一种毒蕈碱受体拮抗剂,对 M1 亚型显示出一定的选择性。
  3. AChR antagonist

    Fesoterodine fumarate 是一种药物,用于治疗尿急,减少排尿次数和急迫性尿失禁
  4. mAChR M2 antagonist

    Gallamine Triethiodide 是一种具有显著心脏选择性的 mAChR M2 拮抗剂。
  5. 异丙托溴铵是一种毒蕈碱拮抗剂支气管扩张剂,是阿托品的N-异丙基盐。
  6. AchR antagonist

    Rocuronium Bromide 是一种竞争性 AchR 拮抗剂,用于现代麻醉。
  7. muscarinic receptor antagonist

    SVT-40776 是一种新型的 M3 muscarinic receptor antagonist,用于治疗 overactive bladder
  8. muscarinic acetylcholine receptor (mAChR) antagonist

    Tiotropium Bromide (BA679 BR) 是一种毒蕈碱型乙酰胆碱受体(mAChR)拮抗剂,它阻止乙酰胆碱配体的结合和随后的配体门控离子通道的开启。
  9. muscarinic receptor antagonist

    托特罗定酒石酸盐(Detrol LA)是一种毒蕈碱受体拮抗剂,用于治疗尿失禁
  10. muscarinic receptor antagonist

    5-羟甲基托特罗定是托特罗定的代谢产物,托特罗定是一种用于治疗尿失禁的毒蕈碱受体拮抗剂
  11. muscarinic M3 receptor antagoinst

    索利那新琥珀酸盐是一种毒蕈碱M3受体拮抗剂,用于治疗尿失禁。
  12. NMDA receptor antagonist

    奥芬那林柠檬酸盐是一种 NMDA 受体拮抗剂,其Ki值为6.0 +/- 0.7 μM,同时也是 HERG 钾通道阻断剂
  13. acetylcholine receptor antagonist

    Beperidium iodide 表现出对乙酰胆碱受体的竞争性拮抗作用,其 pA2 值为 7.93。
  14. muscarinic antagonist

    格列溴铵是一种竞争性毒蕈碱拮抗剂,用作抗痉挛药
  15. muscarinic AChR antagonist

    Flavoxate 结合并抑制胆碱能受体,从而抑制排尿反射并通过改变位于脑干的排尿中枢来增加膀胱容量。
  16. muscarinic M(3) receptor antagonist

    PF-3635659 是一种强效的毒蕈碱M(3)受体拮抗剂
  17. mAChR antagonist

    AF-DX 384 是一种药物,它作为毒蕈碱乙酰胆碱受体的选择性拮抗剂。
  18. M2/M3 antagonist

    Diphenidol HCl 是一种强效的抗胆碱能M2和M3受体拮抗剂,其pKb值分别为6.72和7.02。
  19. Muscarinic receptor antagonist

    溴化乌美克利尼(GSK573719A)是一种毒蕈碱受体拮抗剂,用于治疗慢性阻塞性肺病(COPD)。
  20. muscarinic receptor antagonist

    Revefenacin 是一种强效且选择性的毒蕈碱受体拮抗剂,目前正在开发中,用于治疗慢性阻塞性肺病(COPD)
  21. Muscarinic Receptor Antagonist

    索利那新是一种新型毒蕈碱受体拮抗剂,其对M1、M2和M3受体的pKi分别为7.6、6.9和8.0。
  22. muscarinic antagonist

    Anisotropine methylbromide 是一种胆碱能拮抗剂抗痉挛药。Anisotropine methylbromide 是一种季铵化合物。它作为消化性溃疡治疗辅助药物的使用已被更有效的药物所取代。
  23. Muscarinic antagonist

    Procyclidine hydrochloride 是一种 muscarinic antagonist,能够穿过 blood-brain barrier,用于治疗药物引起的 extrapyramidal disordersParkinsonism
  24. Muscarinic antagonist

    Mepenzolate Bromide 是一种胆碱能拮抗剂,用于治疗胃肠道疾病。它可以减轻由弹性蛋白酶引起的气腔扩大和呼吸功能障碍的严重程度。
  25. M1 muscarinic receptor antagonist

    Pirenzepine dihydrochloride (LS519) 是一种选择性的 M1 muscarinic receptor antagonist
  26. mAChR antagonist

    阿托品甲基溴化物是一种毒蕈碱受体(mAChR)拮抗剂,它是阿托品的季铵盐,并用作眼科检查时扩张瞳孔的散瞳剂。由于其高极性特性,该药物用于缓解婴儿的幽门痉挛。与阿托品相比,它不容易渗透到中央神经系统中。
  27. mAChR antagonist

    溴化西米曲布(DA-3177)是一种mAChR拮抗剂,用于长期治疗肠易激综合症
  28. mAChR antagonist

    Elucaine es un antagonista del receptor muscarínico de acetilcolina con actividad antiulcerosa.
  29. M3 muscarinic receptor antagonist

    YM-58790 是一种强效的 M3 muscarinic receptor 拮抗剂,其 Ki 为 15 nM。
  30. mAChR antagonist

    mAChR-IN-1 hydrochloride 是一种强效的毒蕈碱胆碱能受体(mAChR)拮抗剂,其 IC50 为 17 nM。
  31. M3 muscarinic receptor antagonist

    Tarafenacin D-tartrate (SVT-40776 D-tartrate) 是一种高度选择性的 M3 muscarinic receptor antagonist(Ki= 0.19 nM),对 M2 receptor 的选择性约为200倍。
  32. mAChR antagonist

    mAChR-IN-1 是一种强效的毒蕈碱胆碱能受体(mAChR)拮抗剂,其 IC50 为 17 nM。
  33. Muscarinic Receptor Antagonist

    Biperiden(KL 373) 是一种抗帕金森病药物,它是选择性的中枢 M1 胆碱能受体 阻断剂。
  34. muscarinic antagonist

    Aclidinium Bromide(LAS 34273;LAS-W 330)是一种长效吸入型毒蕈碱拮抗剂,用作慢性阻塞性肺病(COPD)的维持治疗。
  35. muscarinic acetylcholine receptor antagonist

    Benzetimide hydrochloride 是一种胆碱能受体拮抗剂
  36. mAChR antagonist

    Nor-benzetimide 是 Benzetimide 的主要代谢物。Benzetimide 是一种具有抗胆碱能活性的 mAChR 拮抗剂。

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