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蕈毒鹼型乙醯膽鹼受體
来自维基百科,自由的百科全书
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毒蕈鹼型乙醯膽鹼受器(muscarinic acetylcholine receptors)是一大類固定在細胞膜上的乙醯膽鹼受器,其對毒蕈鹼比對菸鹼(尼古丁)更為敏感。反過來對菸鹼比較敏感的則稱為菸鹼型乙醯膽鹼受體。毒蕈鹼與菸鹼兩者皆為生物鹼(alkaloid)。許多藥品與其他類物質(例如匹魯卡品與東莨菪鹼)常以促進劑或拮抗劑的角色發生作用,並且其作用是僅單一針對毒蕈鹼受器或單一針對菸鹼受器,使得這樣的受器分類顯得有用。




背景
生理學
蕈毒鹼型受器的型態
受器形式的多樣性
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M2毒蕈鹼受體位於心臟,在心臟中,它們通過減慢去極化速度,使心率降至正常基線竇性心律以下。在休息條件下的人類中,迷走神經活動高於交感神經活動。因此,抑制M2受體(例如,阿托品)會導致心率升高。它們還適度降低了心房肌肉的收縮力,並降低了房室結的傳導速度。它也可以稍微降低心室肌肉的收縮力。
通常,M2毒蕈鹼受體通過Gi型受體起作用,這會導致細胞內cAMP的降低,電壓門控Ca2+通道的抑制和K+外排的增加,通常會導致抑制型效應。
![]() | 此章節需要擴充。 |
M4受體在中樞神經系統中被發現。M4受體通過Gi受體起作用,從而降低細胞中的cAMP,因此通常產生抑制作用。如果受到毒蕈鹼興奮劑刺激可能導致支氣管痙攣。M4受體也位於外周組織的紅系祖細胞中。M4受體調節cAMP通路從而調控紅系祖細胞分化。靶向M4受體治療對紅血球生成素治療無效的骨髓增生異常症候群和貧血。
M5受體的位置尚不清楚。
參見
文獻
- ^ Simon MI, Strathmann M, Gautam N. Diversity of G proteins in signal transduction. Science. 1991, 252 (5007): 802–8. PMID 1902986. Fulltext (PDF, subscription required) (頁面存檔備份,存於網際網路檔案館)
- ^ Mark L Dell'Acqua, Reed C Carrol, Ernest G Peralta. Transfected m2 muscarinic acetylcholine receptors couple to G alpha i2 and G alpha i3 in Chinese hamster ovary cells. Activation and desensitization of the phospholipase C signaling pathway. Journal of Biomedical Chemistry. 1993, 268 (8): 5676–85. PMID 8449930. Free Fulltext (PDF)
- ^ Messer, Jr, William S. Acetylcholine. 20 Jan 2000. University of Toledo. Accessed 11 September 2005.
- ^ Johnson, Gordon E. PDQ Pharmacology. 2nd edition. BC Decker. 2002. ISBN 1550091093
- ^ Richelson, Elliot. Cholinergic Transduction. The Fourth Generation of Progress. The American College of Neuropsychopharmacology. 2000.
- ^ see Johnson, 2002.
- ^ see Richelson, 2000.
- ^ G protein diversity and complexity in G-protein Signaling. RA Fisher. University of Iowa, Lecture Notes, 2004.
- ^ see Richelson, 2000.
- ^ Burford NT, Nahorski SR. Muscarinic m1 receptor-stimulated adenylate cyclase activity in Chinese hamster ovary cells is mediated by Gs alpha and is not a consequence of phosphoinositidase C activation. Biochemistry Journal. 1996, 315 (Pt 3): 883–8. PMID 8645172. Fulltext (subscription required)
- ^ University of Sydney lecture notes on the M2 receptors, 2005.
- ^ University of Sydney lecture notes on the M3 receptors, 2005.
- Dittman AH, Weber JP, Hinds TR, Choi EJ, Migeon JC, Nathanson NM, Storm DR. A novel mechanism for coupling of m4 muscarinic acetylcholine receptors to calmodulin-sensitive adenylyl cyclases: crossover from G protein-coupled inhibition to stimulation. Biochemistry. 1994, 33 (4): 943–51. PMID 8305442.
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