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Adrenergic and Cholinergic receptor
Adrenergic/Cholinergic receptors and their intrinsic mechanism
22
Pharmacology
Professional
10/23/2010

Additional Pharmacology Flashcards

 


 

Cards

Term

Cholinergic Receptors

Definition

 

  • 2 types
    • Nicotinic receptors
      • Ligand gated channels
    • Muscarinic receptors
      • G-protein coupled receptors  

 

Term

Nicotinic Receptors 

(Ligand gated channels)

Definition
  • Autonomic ganglia (Nn)
  • Neuromuscular junction (Nm)

 

Term

Muscarinic receptors 

(G-protein coupled receptors)

Definition
  • Found on most effector organs
  • M1
  • M2
  • M3
  • M4- presynaptic terminals and CNS- Gi/Go protein-inhibition

 

Term

M2 receptors

Definition
  • Predominately in heart (SA & AV nodes, some atrial tissue, minimal in ventricles)
  • Presynaptic
  • CNS
  • Gi/Go protein-inhibition

 

Term

M3 receptors

Definition
  • Vascular (endothelial cells) and nonvascular (epithelial cells) smooth muscle
  • Secretory glands
  • CNS
  • Gq/11 protein- contraction or relaxation

 

Term

Adrenergic receptors

Definition
  • All are G-protein coupled receptors
  • 2 types
    • α
      • There are 2 subtypes of α receptors
    • β
      • There are 3 subtypes of β receptors
      • β3 receptors are found on adipose tissue (Gs-lipolysis)

 

Term

Alpha one receptors

Definition
  • Vascular and nonvascular smooth muscles
  • Gq protein-contraction

 

Term

Alpha two receptors

Definition
  • Presynaptic nerve terminal
  • Pancreatic beta cells
  • Vascular smooth muscle
  • Gi/Go protein-inhibitory most of the time (except on vascular smooth muscle)

 

Term

Beta one receptors

Definition
  • Heart
  • J-G cells within kidneys
  • Gs protein-excitatory

 

Term

Beta two receptors

Definition
  • Smooth muscle (vascular, bronchial, GI & UT)
  • Gs protein-inhibitory

 

Term

α1A

Definition
  • Contraction of smooth muscle 
  • High density in prostate
  • Also found on arteries and veins

 

Term

α1B

 

Definition
  • Most abundant type in heart (function ???)
  • May be involved with α1A in cardiac growth & structure
  • May be more abundant in blood vessels as we get older
  • α1C = α1B

 

Term

α1D

 

Definition
  • Found on coronary blood vessels and aorta

 

Term

 

α2A

 

Definition

 

  • Inhibitory autoreceptor found on presynaptic nerve endings of sympathetic and also parasympathetic nerves
  • Found in CNS and stimulation associated with hypotension and antinociceptive responses
  • Same affect as α1A on smooth muscle

 

Term

 

α2B

 

Definition

 

  • On peripheral blood vessels
  • Low density
  • Can produce constriction

 

Term

 

α2C

 

Definition

 

  • Predominately inhibitory- found in adrenal medulla and on nerve endings to inhibit release of Epi and Dopamine

 

Term

M2 receptor intrinsic mechanism

Definition
  • Gi/Go- inhibits adenylyl cyclase
  • Inactivates Ca2+ channels
  • Increase K+ efflux-hyperpolarization
  • Inhibitory

 

Term

M3 receptor intrinsic mechanism

 

Definition
  • Gq/11 proteins- increase PLC activity
  • Increase formation of IP3 and DAG
  • Increase intracellular Ca2+
  • Contraction (in most cells-exception-vascular smooth muscle cells)

 

Term

α1 receptor intrinsic mechanism

 

Definition
  • Gq/11 proteins- increase PLC activity
  • Increase formation of IP3 and DAG
  • Increase intracellular Ca2+
  • Contraction 

 

Term

α2 receptor intrinsic mechanism

 

Definition
  • Gi/Go- inhibits adenylyl cyclase
  • Inactivates Ca2+ channels
  • Increase K+ efflux-hyperpolarization
  • Inhibitory

 

Term

β1 receptor intrinsic mechanism

 

Definition

 

  • Gs protein- increase activity of adenylyl cyclase activity
  • Increase intracelllular Ca2+ 
  • Excitatory- contraction of the heart

 

Term

β2 receptor intrinsic mechanism

 

Definition

 

  • Gs protein- increase activity of adenylyl cyclase activity in most smooth muscle cells
  • Decrease intracellular Ca2+
  • Inhibitory-cause relaxation of smooth muscles

 

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