Adrenergic effects Flashcards
What are sympathomimetics?
Drug that recreates the stimulation of a sympathetic nerve
Either they’re directly acting or they act indirectly by boosting the level of noradrenaline
What is isoprenaline?
• Isoprenaline is a synthetic chemical which was developed for research purposes
Potency in alpha and beta adrenergic receptors
- In Alpha, noradrenaline more potent than adrenaline which is more potent than isoprenaline
- In Beta, isoprenaline more potent than adrenaline which is more potent than noradrenaline
What are all adrenoreceptors examples of?
All adrenoreceptors are examples of GPCR
REFER TO NOTES FOR RECEPTORS AND THERE EFFECTS
1
What do alpha 1 adrenoreceptor contract?
• Contract vascular smooth muscle
What do alpha 1 adrenoreceptor increase?
Increase total peripheral resistance
What do alpha 1 adrenoreceptors look like?
Looks like beads on strings-Varicosities
What do varicosities spray out?
Varicosities spray out transmitter
Pathway of alpha 1 adrenoreceptor?
- IP3 binds to its own receptor which is a Ca2+ channel thus causing the release of Ca2+ from the internal calcium stores
- DAG tends to stay in the lipid phase and can activate ion channels itself or activate PKC
What other tissues are alpha 1 adrenoreceptors found in?
• Are found in other tissue:
○ Leading to contraction of the seminal vesicles
○ Contraction of Iris muscle which results in diluted pupils
Contraction of pilomotor muscle which controls hair
Main role of alpha 2 adrenoreceptor?
Main role is the inhibition of neurotransmitter release
Mechanism of adrenoreceptor 2
• Negative feedback mechanism which tends to be a receptor located on the nerve terminals or the varicosities
○ Decreased likely hood of the Ca2+ ion channel being opened and it becomes less sensitive to voltage
○ Adenylate cyclase becomes inhibited so the cAMP goes down and PKA goes down
○ The beta subunits stimulate some potassium channels so a cell becomes calmer. Potassium leaves a cell and the membrane potential becomes more negative
This is where the neurone can be hyperpolarised, reducing the activity of the Ca2+ channels
Beta 1 adrenoreceptors
• Sympathetic innervation is throughout the heart
• Innervation of the SAN, AVN, atria and ventricles
An increase in heart rate
What happens when sympathetic nerve stimulated?
○ When the sympathetic nerve is stimulated, it depolarised the action potential and it becomes briefer
Results in a larger but shorter contraction which is more powerful