Receptor subtype |
Second messenger |
Organ/tissue |
Response |
M1
|
IP3/DAG↑ |
autonomic ganglion including myenteric plexus |
depolarization, slow EPSP increased gastric acid secretion via vagus nerve |
M2
|
cAMP↓ and direct coupling to K+ channel |
vas deferens (rabbit) brain (cerebral cortex) canine saphenous vein heart - |
reduced twitch height and NA release binding sites contraction |
atrium |
reduced rate (negative chronotropy) |
sinu-atrial node prejunctional at autonomic nerve endings |
reduced rate (negative chronotropy) reduced NA or Ach release |
ileum smooth muscle |
predominant binding sites - uncertain
function |
M3
|
IP3/DAG↑ |
smooth muscle -gut urinary bladder trachea iris circular muscle blood vessels- |
contraction
minor binding sites |
endothelium smooth muscle glands - |
release of NO and vasodilatation
contraction |
oxyntic cells (gastric acid) salivary glands pancreatic β cells |
increased acid secretion salivation insulin release |
M4
|
cAMP↓ |
guinea-pig uterus |
contraction |
rabbit anococcygeus muscle |
NO-dependent relaxation |
rabbit lung |
binding sites |
M5
|
IP3/DAG↑ |
brain regions |
binding sites after all others occluded |
|
Abbreviations: Ach, acetylcholine; cAMP, cyclic adenosine 3',5'-monophosphate; DAG, 1,2-diacylglycerol; EPSP, slow depolarization; IP3, inositol 1,4,5-triphosphate; NA, noradrenaline; NO, nitric oxide. |