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M: GPCR

CHOLINERGIC RECEPTORS N: ion channels

RESULTS OF
RECEPTOR NAME TYPICAL LOCATIONS EFFECTS
LIGAND BINDING
!IP3 / DAG CNS Increased cognitive function
Gq Muscarinic M1
! Ca Ganglia Depolarization
Opening of K channels Heart (Atria) Cardiac inhibition
Gi Muscarinic M2 Closing of Ca Channels
"cAMP Presynaptic nerve terminals Inhibition of ACh & NE release
Smooth muscle Contraction
!IP3 / DAG
Gq Muscarinic M3 Vascular endothelium [indirect] Vasodilation (via NO) cGMP
! Ca
Secretory glands Secretion
Autonomic ganglia Ganglionic transmission
Nicotinic NN Opening of cation channels,
Adrenal medulla Secretion of catecholamines
depolarization
CNS Undefined
Nicotinic NM Opening of cation channels,
Neuromuscular junction Neuromuscular transmission
depolarization

ADRENERGIC RECEPTORS
ADRENERGIC RESULTS OF
TYPICAL LOCATIONS EFFECTS
RECEPTORS LIGAND BINDING
Gq α1 !IP3 / DAG Vascular smooth muscle Contraction
! Ca Genitourinary smooth muscle Contraction
Intestinal smooth muscle Relaxation
Liver ! Glycogenolysis
! Gluconeogenesis
Gi α2 [autoregulation] " cAMP Presynaptic nerve terminals Inhibition of ACh & NE release
pancreas: α2 > ß2
" Ca channels Platelets Aggregation
+ Adipocytes Inhibition of lipolysis
! K channels
Pancreatic islets (β cells) Decreased insulin secretion
! Ca Vascular smooth muscle Contraction
Gs β1 ! cAMP Heart !Heart rate
"KASH"
• kidney
! Ca !Heart force
• adipose
• 
!AV nodal conduction velocity
• heart Juxtaglomerular cells !Renin release
Gs β2 ! cAMP Smooth muscle relax detrusor Relaxation
cutaneous
(flush)
(vascular, bronchial, GIT & GUT)
Skeletal muscle !Glycogenolysis !Uptake of K+
Pancreatic islets (β cells) ! Insulin secretion
Pancreatic islets (α cells) ! Glucagon secretion
Liver ! Glycogenolysis
! Gluconeogenesis
Gs β3 ! cAMP Adipocytes ! Lipolysis

DOPAMINE RECEPTORS
RESULTS OF
RECEPTOR TYPICAL LOCATIONS EFFECTS
LIGAND BINDING
Gs D 1, D 5 ! cAMP Brain
Smooth muscle of renal vascular bed Relaxation of renal vascular smooth
muscle
Gi D2 " cAMP Brain,
+ Effector tissues: especially smooth muscle; Presynaptic nerve terminals
!K conductance
Gi D3 " cAMP Brain
Gi D4 " cAMP Brain, cardiovascular system

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