Summary
Summary Adrenoreceptor agonists and antagonists
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Neurophysiology, synaptic pharmacology and endocrinology - 1st semester Includes bullet points, key diagrams and images
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Adrenoreceptor Agonists and AntagonistsClassification
GPCRs
Secondary messengers:
α1- activates PLC producing IP3 and DAG
α2- inhibits adenylyl cyclase decreasing cAMP production
β- stimulate adenylyl cyclase to produce cAMP
Effect of Receptors:
α1- vasoconstriction, relaxation of GIT, salivary secretion and glycogenolysis
α2-inhibit release of NA and Ach from autonomic nerves, platelet aggregation,
contraction of vascular smooth muscle and inhibit insulin secretion
β1- increase cardiac rate and force plus delayed cardiac hypertrophy
β2- bronchodilation, vasodilation, relaxation of visceral smooth muscle,
glycogenolysis and tremor
β3- lipolysis
, Physiological Effects of Adrenoreceptors
α1
More responsive to NA than ADR
Found on: vascular smooth muscle, dilator muscle of iris and erector pili muscles
Increasing neurotransmitter increases activity of cell
α2
On post-synaptic membrane of adrenergic receptors
Neurotransmitter binds to receptors on pre and post-synaptic membrane
Negative feedback effect so pre-synaptic response is to decrease secretion of NA
Inhibit release of NA
β1
Increasing neurotransmitter increases activity of cell
Found on: SAN, myocardium, salivary gland and eccrine/apocrine seat glands
β2
Located on smooth muscle of: GIT, bladder, skeletal muscles and bronchioles of
coronary vessels
Inverse relationship between neurotransmitter and cell response so increasing
transmitter will decrease their response
Facilitates release of NA
β3
Found on adipose tissue and urinary vascular smooth muscle (decreases their
tone)
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