Cholinoreceptors Flashcards
What are the types of cholinergic receptors according to their affinity to ligands?
M&N cholinergic receptors
what are M Cholinergic receptors?
- They are muscarinic receptors which are selectively activated by muscarine and can be blocked by atropine.
- They are also metabotropic receptors which are coupled with G-proteins.
what are N Cholinergic receptors?
- They are nicotinic receptors which are selectively activated by small doses of nicotine and blocked by high doses of nicotine.
-They are ionic receptors Which need 2 acetylcholine molecules to bind to each receptor to be able to open them.
What type of M1 Cholinergic receptors do we have?
Neuronal with a postsynaptic location
What type of M2 Cholinergic receptors do we have?
- Postsynaptic or cardiac
- Presynaptic
What type of M3 Cholinergic receptors do we have?
- Postsynaptic or glandular
- extra synaptic
What is the transduction mechanism of M1 Cholinergic receptors?
They couple with Gq proteins which activate force for lipase C in turn activating the secretion of DG and IP3 leading to an increase of calcium quantity which as a result we have a stimulatory action.
Where can we find M1 Cholinergic receptors?
- CNS, limbic system, reticular formation, and basal ganglion
- autonomic ganglia
- enterochromaffin cells
what is the action of M1 Cholinergic receptors in CNS?
Activation and regulation of psychomotor activity as well as activation of weakening reactions and learning process
what is the action of M1 Cholinergic receptors in autonomic ganglia?
Depolarization and development of slow EPSP
what is the action of M1 Cholinergic receptors in enterochromaffin cells?
Stimulation of the secretory function through the release of histamine
What is the transaction mechanism of M2 Postsynaptic Cholinergic receptors?
They couple with Gi proteins at which they lead to the inactivation of adenylate cyclase and decrease of cyclic AMP quantity as a result inhibitory action is developed
Where can we find post synaptic M2 Cholinergic receptors?
- SA node
- Atriums
- AV node
- ventricular muscle
what is the action of post synaptic M2 Cholinergic receptors on the SA node?
It decreases the frequency of spontaneous diastolic depolarization leading to bradycardia
what is the action of post synaptic M2 Cholinergic receptors on the atriums?
It shortens the potential action duration in atrial muscle leading to the decrease in contractility of atrial muscle