Adrenergic receptors Flashcards
adrenaline and noradrenaline are
catecholamines
noradrenaline is the main
NT of the sympathetic nerves in cardiovascular system
adrenaline is
the main hormone secreted by the adrenal medulla
adrenoreceptors are located
throughout the body on neuronal and non-neuronal tissue
adrenoreceptors are
GPCR’s
binding of catecholamines to the receptor is responsible for
fight or flight response
name the types of adrenoreceptors
alpha1, alpha2, beta1, beta2, beta3
alpha1
o Vascular smooth muscle
o Visceral smooth muscle
o CNS neurone
alpha2
o Presynaptic terminals o Pancreatic islets o Platelets o Ciliary epithelium o Smooth muscle CNS neurones
beta1
o Myocardium (heart)
o JG cells
o Some presynaptic terminal
CNS neurons
beta2
o Visceral (guts) smooth muscle o Vascular smooth muscle (bronchi) o Liver o Urinary tract o Myocardium Skeletal
beta3
adipose tissue
alpha1 adrenoreceptors are coupled with
Gq
α1 adrenergic receptors (Gq)
1) Adrenaline binds to GPCR
2) Gq activates phospholipase C, which hydrolyses PIP2 IP3 and DAG
3) Increase in IP3 and therefore increase in calcium
4) Calcium binds to calmodulin and activates MLCK, which causes myosin heads to form cross-bridges- contraction
5) Activation of enzyme protein kinase C (PKC) by DAG
6) Phosphorylation of other enzyme
7) Increase or decrease of electrolyte transfer in or out of the cell
when alpha1 blocker is added
hypertension treatment- since cascade does not occur
alpha2 adrenoreceptor linked with
Gi
1) Substrate (adrenaline) binds to GPCR
2) Gi associates with adenylyl cyclase
3) Decrease in CAMP
4) PKA is not activated by cAMP
5) Proteins such as PK cannot be phosphorylated by PKA
6) No activation of glycogen phosphorylase
7) Decreased breakdown of glycogen