Pharm 10: Cholinergic Pharm Flashcards
Muscarinic acetylcholine receptor type and location
G-protein
All parasympathetics, few sympathetics, CNS
Nicotinic Acetylcholine receptor type and location
Ligand gated
Post synaptic in excitatory ANS
Presynaptic in CNS
Acetylcholine synthesis _____+______= acetylcholine
what enzyme?
Acetyl CoA+ Choline
Choline acetyltransferase
How does choline get into neuron
NA+/Choline co-transporter
How does choline get into vesicle
AcH/H+ cotransporter
Hemicholinium-3 mechanism
Stops choline from entering the neuron (inhibits Na+/Choline transporter)
AcH can’t be synthesised
Anticholinergic
Vesamicol mechanism
Inhibits H+/ACh antiporter meaning AcH can’t get into vesicle
Anticholinergic
Muscarinic receptor type
G-protein coupled
Nicotinic receptor type
Ligand-gated ion channel
Muscarinic M1 Receptor location and response
Autonomic ganglia/CNS
Arousal, analgesia, late excitatory postsynaptic potential
Muscarinic M2 receptor location and response
Heart
Decreased conductivity, conduction velocity and contractility
Muscarinic M3 receptor location and response
Smooth muscle, contraction
Muscarinic M4 location and response
CNS
Presynaptic autoreceptor. Feedback inhibittion to suppress ACh release
Nicotinic Nm receptor location and response
Skeletal muscle neuromuscular junction
Depolarization and muscle contraction
Nicotinc Nn receptor location response
Autonomic ganglia, adrenal medulla, CNS
Depolarization of postganglionic neuron, catecholamine secretion, arousal/attention/analgesia
Ach is degraded by
AChE acetylcholinestarese
BuChE psyedocholinesterase