COMPARISION OF MUSCARINIC RECEPTORS

Type Function Effectors Agonists Antagonists

M1 EPSP in autonomic ganglia Gq acetylcholine atropine
secretion from salivary glands and stomach (Gi) oxotremorine scopolamine
In CNS (memory?) (Gs): muscarine dicycloverine
Slow EPSP. carbachol tolterodine
K+ conductance McNA343 oxybutynin
77-LH-28-1 ipratropium
mambatoxin
pirenzepine
telenzepine
M2 slow heart rate Gi acetylcholine atropine[
reduce contractile forces of atrium K+ conductance methacholine dicycloverine
reduce conduction velocity of AV node Ca2+ conductance carbachol tolterodine
In CNS oxotremorine oxybutynin
homotropic inhibition muscarine ipratropium
methoctramine
tripitamine
gallamine
M3 smooth muscle contraction Gq acetylcholine atropine
Increase intracellular calcium in vascular bethanechol dicycloverine
endothelium carbachol tolterodine
increased endocrine and exocrine gland sec oxotremorine oxybutynin
retions, e.g. salivary glands and stomach pilocarpine (in eye) ipratropium
In CNS darifenacin
Eye accommodation tiotropium
vasodilation
induce emesis
M4 Activation of M4 causes decreased Gi acetylcholine atropine
locomotion K+ conductance carbachol dicycloverine
In CNS Ca2+ conductance oxotremorine tolterodine
oxybutynin
ipratropium
mambatoxin
M5 In CNS Gq acetylcholine atropine
carbachol dicycloverine
oxotremorine tolterodine
oxybutynin
ipratropium

Histamine receptors
Receptor Mechanism Function Antagonists
H1 Gq ileum contraction ,modulate circadian cycle ,itching Diphenhydramine
systemic vasodilatation , bronchoconstriction (asthma) Loratadine
Cetirizine
Fexofenadine
H2 Gs speed up sinus rhythm , Stimulation of gastric acid secretion, Smooth Ranitidine
Ca2+ muscle relaxation, Inhibit antibody synthesis, T-cell proliferation Cimetidine
and cytokine production
H3 Gi Neurotransmitter in CNS ABT-239
Presynaptic autoreceptors Ciproxifan
Clobenpropit
Thioperamide
H4 Gi mediate mast cell chemotaxis.[2] Thioperamide
JNJ 7777120

BY- SHRIKANT THAKUR PHARMA WORLD CLASSES 9907862994