Autonomic neuronal receptor pharmacology Flashcards
Noradrenaline is a potent agonist at?
1- and a 2- adrenoceptors, and b1-adrenoceptors
Noradrenaline has little effect at?
B2-adrenoceptors
Adrenaline is a potent agonist at?
All adrenoceptors
Acetylcholine activates all?
All muscarinic receptor subtypes (M1, M2, M3) and both nicotinic receptor subtypes (neuronal, skeletal muscle)
Adrenoceptors are all coupled to?
Coupled to G-proteins
G-proteins interact with?
A variety of intracellular mechanisms
Activation of A1-adrenoceptors results in?
Results in activation of phospholipase C
Activation of phospholipase C increases?
Increases levels of the intracellular second messengers inositol triphosphate and diacylglycerol
A2-adrenoceptor activation results in?
Results in an inhibition of adenylyl cyclase
Inhibition of adenylyl cyclase results in?
A decrease in intracellular cAMP
Activation of B1- and B2-adrenoceptors activates?
Adenylyl cyclase
Activated adenylyl cyclase results in?
elevated intracellular cAMP
Agonist drugs which mimic noradrenaline and adrenaline at adrenoceptors include?
- Phenylephrine
- Clonidine
- Isoprenaline
- Dobutamine
- Salbutamol
Phenylephrine is selective for?
A1-adrenoceptor
Clonidine is selective for?
A2-adrenoceptor
Isoprenaline is selective for?
B1- and B2-adrenoceptors
Dobutamine is selective for?
B1-adrenoceptors
Salbutamol is selective for?
B2-adrenoceptors
Drugs which act as competitive antagonists at adrenoceptors include?
- Labetalol
- Phentolamine
- Prazosin
- Propranolol
- Metoprolol
Labetalol is selective for?
Non-selective
Pentolamine is selective for?
A1- and A2-adrenoceptors
Prazosin is selective for?
A1-adrenoceptors
Propranolol is selective for?
B1- and B2-adrenoceptors
Metoprolol is selective for?
B1-adrenoceptors
Principal effector cell actions mediated by A1-adrenoceptors include?
- Smooth muscle contraction (vascular, gastrointestinal sphincters, bladder trigone, urethral internal sphincter, iris radial).
- Relaxation of gastrointestinal non-sphincter smooth muscle
- K+ rich saliva secretion
- Glycogenolysis
Main actions mediated by A2-adrenoceptors are?
- Prejunctional inhibition of nordarenaline release from sympathetic postganglionic nerve terminals (autoinhibition) and platelet aggregation
Effector cell actions resulting from B1-adrenoceptor activation include?
- Increases in heart rate and force of contraction
- Relaxation of gastrointestinal non-sphincter smooth muscle
- Amylase-rich saliva secretion and lipolysis