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Cards (106)
What are the two main types of cholinergic receptors discussed?
Nicotinic
and
muscarinic
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What is the effect of muscarinic agonists, and what is one clinical use?
Physiological
effects;
clinical uses
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What is a presynaptic target for pharmacological intervention in cholinergic neurons?
Within
cholinergic
neurons
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What are the two main types of neuromuscular blocking agents?
Depolarising
and
non-depolarising
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What is the physiological effect of cholinesterase inhibitors?
Enhance
cholinergic
transmission
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What neurotransmitter acts at autonomic ganglia?
Acetylcholine
(ACh)
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What neurotransmitter acts at neuroeffector junctions in the parasympathetic nervous system?
Acetylcholine
(ACh)
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What neurotransmitter acts at the neuromuscular junction (NMJ)?
Acetylcholine
(ACh)
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How is the action of acetylcholine terminated?
By
acetylcholinesterase
(
AChE
)
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What are the two types of activity that Dale distinguished for Acetylcholine?
Nicotinic
and
muscarinic
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What substance mimics the effects of ACh at nicotinic receptors?
Nicotine
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What type of channels are nicotinic receptors?
Ligand-gated ion channels
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What ions do nicotinic receptors conduct?
Na+
and
K+
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How many subunits compose nicotinic receptors?
5
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How many ACh binding sites do nicotinic receptors have?
2
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What is the effect of stimulating nicotinic receptors in the adrenal medulla?
Adrenaline secretion
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Where are nicotinic receptors found?
NMJ
,
autonomic ganglia
,
CNS
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What substance mimics the effects of ACh at muscarinic receptors?
Muscarine
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What substance blocks the effects of ACh at muscarinic receptors?
Atropine
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What type of receptors are muscarinic receptors?
G-protein coupled receptors
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Where are muscarinic receptors found?
Neuroeffector junctions of parasympathetic NS
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Where else are muscarinic receptors found?
Cholinergic
sympathetic receptors,
CNS
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How many muscarinic receptors have been cloned?
Five
(
m1-m5
)
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What is another name for the M1 muscarinic receptor?
Neural
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What is the effect of M1 receptor activation?
Activates
phospholipase C
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What is the downstream effect of phospholipase C activation by M1 receptors?
↑
IP3
,
DAG
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What physiological response is mediated by M1 receptors?
Gastric secretion
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What effect do M1 receptors have at ganglia?
Slow excitatory effects
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What causes the slow excitatory effects at ganglia mediated by M1 receptors?
↓
K+
conductance
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Where do M1 receptors cause excitation?
CNS
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What is another name for the M2 muscarinic receptor?
Cardiac
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What is the effect of M2 receptor activation?
Inhibit
adenylate cyclase
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What is the downstream effect of adenylate cyclase inhibition by M2 receptors?
↓
cAMP
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What effect do M2 receptors mainly have?
Mainly
inhibitory
effects
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What causes the inhibitory effects of M2 receptors?
Increase in
K+
and decrease in
Ca2+
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What physiological response is mediated by M2 receptors?
Cardiac inhibition
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What is the effect of M2 receptors on ACh release?
Autoinhibition
of ACh release
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What drug specifically inhibits M2 receptors?
Gallamine
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What is another name for the M3 muscarinic receptor?
Glandular
/
smooth muscle
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What is the effect of M3 receptor activation?
Activates
phospholipase C
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See all 106 cards
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