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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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  • June 8, 2023
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  • 2019/2020
  • Summary
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Adrenoreceptor Agonists and Antagonists

Classification

 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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