neuropharm last lec Flashcards
Neuropharm test 2 last lec
what is the structural of nACh receptors?
_ at least 2 alpha subunits
_ hill coefficient = 2 (requires at least 2 Ach molecule to activate)
_ do not hyperpolarize neurons
o calcium channel (inward current _ depolarize
Neuropharm test 2 last lec
how does nAch receptor open or close its gate ?
via conformational change
_ General conformational change
Neuropharm test 2 last lec
how does nAch receptor change their conformation?
_ Subunits rotate relative to one another to open/close channel
Neuropharm test 2 last lec
what structure is unique in torpedo fish?
their nicotinic receptor in their electroplax organ which produces a large bolt of electrical current and stun every fish around them
Neuropharm test 2 last lec
what is different of the nicotinic channel in Torpedo fish and human?
the torpedo fish have gram worth of these channels which alow them for the massive electrical current
Neuropharm test 2 last lec
what subunit is specific to nAch receptors?
the alpha subunit of them which makes them nAch receptors
Neuropharm test 2 last lec
how does subunit of nAch receptors different in different region?
alpha subunit is all over the nervous system, beta-2 are all over the place, 3 only in selective places, 4 is found in Habinula
Neuropharm test 2 last lec
how does these subunit change with againg?
Alpha, beta and delta are the ones sen in asult. Early in life instead of delta we had Gamma subunit. We also had Epsilon early in life
Neuropharm test 2 last lec
where are these subunit found?
_ researched showed they were located pre- and post-synapticall. they are also found elsewhere on the axon (pre-terminally _ axolemnal locations)
Neuropharm test 2 last lec
how is the overal Hill coeficient of nAChR receptors?
More nAChR diversity, Different Hill coefficients
Neuropharm test 2 last lec
what is the relationship of nAChR alpha 7 receptors and smoking?
requirement to activate the receptors seems to go down with experience to nicotine
Neuropharm test 2 last lec
what kind of sununits are used in Alpha 7 receptors?
theyahve all 5 subunits identical
Neuropharm test 2 last lec
how does nicotinic receptors or nAChR alpha 7 receptors affext the expression and glucose utilization?
low-level of expression in non-smokers. nonsmokers show high levels of glucose utilization. utilization of glucose goes down the more they smoke _ possible calming effect
Neuropharm test 2 last lec
what is th effect of nAChR of Na?
nAChR mediate the Na+ current
Neuropharm test 2 last lec
what is the nAChRhill coefficient?
most of these receptors have Hill coefficient of 2 (1 is not sufficient
Neuropharm test 2 last lec
what are the uses of nAChR ligands clinically?
o Treatment of: 1-Motor dysfunctions. 2-Cognitive impairments, ADD. 3-Memory impairments. 2-Tobacco addiction. 3- Autonomic functions 4- Surgical paralysis
Neuropharm test 2 last lec
what are the non-clinical use of nAChR ligands?
o Recreational Smoking, chewing, snuff, Insecticides, neurotoxins, Paralytic, assassination poisons
Neuropharm test 2 last lec
what are some of the Short and long-acting analogs of Ach?
1-ACh (endogenous ligand): Broken down extremely rapidly after release from pre-synaptic terminals
2-Shortest acting analog: Carbachol _ lasts much longer than ACh in the synapse
Neuropharm test 2 last lec
where are the 3 region of the body where we look for nAchR?
CNS, autonmic ganglia, NMJ
Neuropharm test 2 last lec
what kind of subunit of n-AchR is only in mostly in brain or CNS?
Alpha-7
Neuropharm test 2 last lec
what are the competitive agonist that works on CNS, autonomic ganglia and NMJ?
Ach, Carbachol, Nicotine
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which one of the competitive agonist does not work on autonomic ganglia but it does on all other area?
Anatoxin
Neuropharm test 2 last lec
which kind of agonist is specific to autonomic ganglia?
DMPP
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which kind of agonist is specific to NMJ?
Suxamethonium
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which kind of agonist is specific to CNS only?
Labeline, Anabasine
Neuropharm test 2 last lec
what is the endogenous agonist that works on all regions?
Ach
Neuropharm test 2 last lec
for the non-alpha7 CNS name an competitive antagonist?
Coronaridine
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for the alpha-7 CNS which name a competitive antagonist?
Alpha-bungarotoxin _ competitive antagonist
Neuropharm test 2 last lec
which none-competitive antagonist block alpha-7 CNS?
Buproprion (wellbutrin) _ noncompetitive antagonist
Neuropharm test 2 last lec
what is an competitve antagonist of autonomic ganglia?
Hexamethonium, kappa-bungarotoxin
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which antagonist keeps the membane of the Autonomic ganglia depolarized?
Trimethaphan (technically very, very strong agonists)
Neuropharm test 2 last lec
what are some of the competitive antagonist for NMJ nAChR?
Decamethonium, curare, tubocurarine (active compound)
Neuropharm test 2 last lec
what is the name of the depolarizing agonist for NMJ nAChR ?
Succinylcholine _ depolarizing blocker (keeps membrane depolarized
Neuropharm test 2 last lec
what are some of the non-competitive antagonist of CNS, CNS alpha 7, autonomic ganglia, NMJ?
PCP, TEA
Neuropharm test 2 last lec
name a suicide antagonist for CNS, CNS alpha 7, AG, NMJ?
bromoACh
Neuropharm test 2 last lec
what are some of the hexamethonium and it family?
o 6 hydro carbons, fairly specific for ganglionic receptors, shorter the drugs are, the more specific they are for the ganglionic
the longer version is more specific for Ach receptor
Neuropharm test 2 last lec
how can neuro-transmission be altered?
_ Nerve AP
_ Biosynthesis
_ Vesicular release
_ Receptors
_ Degradation
_ Ion channels
_ Spread of muscle excitation
_ Muscle contration
