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蕈毒鹼型乙醯膽鹼受體

乙酰膽鹼-毒蕈鹼和菸鹼型乙酰膽鹼受體的天然興奮劑。
毒蕈鹼-一種用於區分這兩類受體的興奮劑。通常在體內找不到。
阿托品-一種蕈毒鹼型乙醯膽鹼受體拮抗劑
毒蠅傘(學名:Amanita muscaria)可分離出毒蕈鹼

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酰膽鹼受體。毒蕈鹼與菸鹼兩者皆為生物鹼(alkaloid)。許多藥品與其他類物質(例如匹魯卡品東莨菪鹼)常以促進劑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

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乙醯膽鹼受器中,毒蕈鹼受器是一種次分類,廣泛分布於中樞神經系統自主神經系統。自主神經系統在解剖上與體神經系統相異。

自主神經系統可分成兩個部分:交感神經系統副交感神經系統

生理學

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乙醯膽鹼(Acetylcholine, ACh)是一種神經傳導物質,在腦部與自主神經系統中廣泛存在。

蕈毒鹼型受器的型態

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受器形式的多樣性

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乙醯膽鹼受器,蕈毒鹼型1
識別
符號 CHRM1
Entrez 1128
HUGO 1950
OMIM 118510
RefSeq NM_000738
UniProt P11229
其他資料
基因座 11 q12-q13
乙醯膽鹼受器,蕈毒鹼型2
識別
符號 CHRM2
Entrez 1129
HUGO 1951
OMIM 118493
RefSeq NM_000739
UniProt P08172
其他資料
基因座 7 q35-q36
乙醯膽鹼受器,蕈毒鹼型3
識別
符號 CHRM3
Entrez 1131
HUGO 1952
OMIM 118494
RefSeq NM_000740
UniProt P20309
其他資料
基因座 1 q41-q44
乙醯膽鹼受器,蕈毒鹼型4
識別
符號 CHRM4
Entrez 1132
HUGO 1953
OMIM 118495
RefSeq NM_000741
UniProt P08173
其他資料
基因座 11 p12-p11.2
乙醯膽鹼受器,蕈毒鹼型5
識別
符號 CHRM5
Entrez 1133
HUGO 1954
OMIM 118496
RefSeq NM_012125
UniProt P08912
其他資料
基因座 15 q26

M2受體

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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。

M3受體

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此章节需要扩充


M4受體

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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

M5受體

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M5受體的位置尚不清楚。

參見

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文獻

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  1. ^ 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)页面存档备份,存于互联网档案馆
  2. ^ 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)
  3. ^ Messer, Jr, William S. Acetylcholine. 20 Jan 2000. University of Toledo. Accessed 11 September 2005.
  4. ^ Johnson, Gordon E. PDQ Pharmacology. 2nd edition. BC Decker. 2002. ISBN 1550091093
  5. ^ Richelson, Elliot. Cholinergic Transduction. The Fourth Generation of Progress. The American College of Neuropsychopharmacology. 2000.
  6. ^ see Johnson, 2002.
  7. ^ see Richelson, 2000.
  8. ^ G protein diversity and complexity in G-protein Signaling. RA Fisher. University of Iowa, Lecture Notes, 2004.
  9. ^ see Richelson, 2000.
  10. ^ 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)
  11. ^ University of Sydney lecture notes on the M2 receptors, 2005.
  12. ^ University of Sydney lecture notes on the M3 receptors, 2005.
  13. 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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蕈毒鹼型乙醯膽鹼受體
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