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47 Cards in this Set
- Front
- Back
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what is the time scale for fast and slow synaptic transission, neuromodulation, and neurotrophic effects?
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fast - msec
slow - 100s of msec to sec neuromodulation - minutes to hours trophic effects - hours to days |
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neuromodulators are usually ___
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neuropeptides
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metabotropic receptors are involved in ___ synaptic transmission
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slow
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the effects of ____ receptors are indirect
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metabotropic / GCPR
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neurotrophic factors act through ___ receptors
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metabotrophic
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structural differences between ionotropic and metabotropic receptors?
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ionotropic
5 subunits each with 4 TMD's 4 subunits each with 3 TMD's (glutamate) these form a pore metabotropic one serpentine GPCR (7 TMD) |
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what NT has just ionotropic receptors?
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glycine
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which NT's have just metabotropic receptors?
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dopamine, norepinephrine, and all neuropeptides
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sensory receptors are in the category of ____ receptors
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metabotropic
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what is densensitization?
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the decrease of the response to an agonist event though the agonist is still present (bound??)
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when would the relative amounts of the agonist and antagonist matter in determining effect?
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with a competitive antagonist
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glutamate ionotropic receptors structure
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4 subunits with 3 TMD's and a pore loop
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all other ionotropic receptor structure
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5 subunits with 4 TMD's
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how is the diversity of ionotropic receptors with regards to desentization, regulation, agonists and antagonists, and selectivity achieved?
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with different combinations of subunits
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2 receptors for glutamate differ in their amount of desentization. how is this accomplished?
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by different combinations of subunits
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GABA and glycine are ____ NT's and their receptors are permeable to ____
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inhibitory; Cl
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Glutamate, Ach, and serotonin are ____ NT's and their receptors are permeable to ____
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excitatory; Na, K, sometimes Ca
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how are muscle Ach receptors different from those in the brain?
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muscle 2a,b,g,d
brain -just a and b. some are homopentamers of alpha |
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which subunits of AchR bind Ach
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alpha
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all ionotropic glutamate receptors are permeable to __ and ___, and some are also permeable to ___
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Na, K; Ca
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3 types of ionotropic glutamate receptors
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NMDA, AMPA, Kainate
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difference b/t NMDA and AMPA glutamate receptors?
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NMDA is blocked by a Mg ion at RMP. with depolarization AND glutamate, it can open. NMDA is permeable to calcium. its dual requirement for opening makes it important in learning and memory.
AMPA is not blocked at RMP and is not Ca permeable |
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picrotoxin and biculline are antagonists of ___ receptor
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GABA (GABAa receptor)
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___ is the predominant GABA receptor in the brain. ___ is only in the retina
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GABAa; GABAc
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why are allosteric binding sites on the GABAa receptor important?
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they allow affects from drugs like barbituates, benzodiazepines, steroids, convulsants (biculline), and ethanol to modulate inhibitory current in the brain and spinal cord
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benzodiezapines - effect and mech?
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potentiate GABA binding at GABA receptors, have anti-anxiety and muscle relaxing properties
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strychnine
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blocks glycine receptors. (major inhibitory NT of the spinal cord) causes muscle spasms
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co-agonist for NMDA receptor?
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glycine
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cholera toxin
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prevents GalphaS from hydrolyzing GTP. this keeps it in active form.
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pertussis toxin
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prevents Galphabetagamma bound to GDP from releasing GDP. this keeps the G protein from becoming activated again.
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how can a GPCR modulate the release of NT?
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there is autoregulation at presynaptic nerve terminals. there are alpha-2 adrenergic receptors (GPCR) that inactivate calcium channels preventing further release of NT.
presynaptic autoreceptors |
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how can metabotropic NT receptors produce the longest effects?
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by modulating gene expression
e.g. modulating enzymes, etc, and changing the synthesis of NT's |
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what implication does a variety of metabotropic receptor subtypes have for drug design?
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the same NT can have different affects in different cells. a drug may have side effects because of this
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Alzheimer's is associated with which NT?
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acetylcholine
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glycine receptors are blocked by ___
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strychnine
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what is slow channel syndrome?
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a mutation in muscle AchR causes the channel to stay open too long. these people have prolonged AP's which results in muscle problems
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what is startle disease / stiff baby syndrome?
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mutation in glycine receptor causes exaggerated startle reflex
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benzodiazepines and barbituates act at __ receptor
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GABA. they are agonists and increase inhibition
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Enhancement of ___ is a highly effective method for treating some types of anxiety and epilepsy.
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GABA
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the ____ receptor is implicated in excitotoxicity and stroke
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NMDA
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how can glutamate play a role in stroke?
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ischemic neurons release glutamate
glutamate binds to NMDA receptors on other neurons and causes them to fire, taking in large amounts of Na and Ca. these neurons die (excitotoxicity) and they then release glutamate toxic cascade |
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cocaine blocks reuptake of ___ which plays a role in the ____ system of the brain
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dopamine
reward |
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amphetamine causes the _____ to run in reverse resulting in ____ release
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dopamine transporter
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ritalin blocks ____
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dopamine and norepinephrine transporters, keeping them in the synapse longer for greater affect
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MAO inhibitors function as ___ and block degredation of ___
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antidepressants
serotonin, norepinephrine, and dopamine |
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what is serotonin syndrome?
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a side effect of too much serotonin. SSRI or drugs (ecstasy) can cause this happy drunk feeling, lots of other shit, and then death
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MDMA acts causes release of ___ and inhibits reuptake
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dopamine
MDMA=ecstasy |
