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45 Cards in this Set
- Front
- Back
What are the percentage breakdowns of targets of psychotropic meds?
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30% Transporters
30% G-Protein-Linked receptors 20% Ligand-gated Ion channels 20% Voltage-sensitive Ion channels 10% Enzymes |
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Transporters are the _______. They are _______that binds to a NT and transport them across the membrane.
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Wheels
Receptors |
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There is a superfamily of ___transmembrane region proteins. Name 5 of the transporters.
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12
DAT NET SERT VMAT VAChT |
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List 3 types of transporters. (PIN)
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Plasma Membrane Transporters
Intracellular synaptic ves Tranporters NT transporters |
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What do Plasma membrane transporters do?
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brings things in from "outside" the presyn neuron.
There are 2 kinds based on gene families: SLC6 (5HT, NE, DA, GABA, Glycine) and SLC1 (Glu) |
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In SLC6 energy for transport is provided by_____pumps.
___is constantly pumped out. ___ and ___ are also involved. |
Na+
Na+ K+ and Cl- |
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_____are MA transporters.
____ binding is needed for MA binding to occur. |
VMAT
Na+ |
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What is allosteric binding?
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it means "other space" or sites and the binding that occurs in MA binding. IE SSRIs bind allosterically because once used by neuron it has a free ride into the cell.
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The more ___at binding, the ____ the side effects, typically.
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Selective
Fewer |
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GABA is an ____NT and its reuptake is inhibited GAT1.
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inhibitory
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What happens when you inhibit the reuptake of an inhibitory NT?
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You inhibit the reuptake of the GABA and it is kept in the synaptic cleft longer and build up leading to greater inhibitory effects. This is true in anti psychotics, anxiolytics, anticonvulsants, etc.,
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Glu is an _____NT
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excitatory
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What would happen is you inhibited transport of Glu?
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There would be more glumamate for excitation which would cause increased excitation.
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In ______transport, VMATS are provided energy by ______ and the VMATS ____ the material via ______transport, not allosteric.
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Vesicular Transport
Proton Pumps repackage Direct |
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______target DATs and NETs (presyn) as well as VMATs. They compete at binding sites and ____vesicular DA. Releaing DA into synapse. DA builds up.
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Amphetamines
displace |
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G protein-linked receptor targets (postsyn) are part of a superfamily of ____ _____ regions. They are defined by different _________ and triggered by ______
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7 transmembrane
Agonists/antagonists Enzymes |
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List the types of action on receptors according to the Agonist spectrum.
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None - no change, baseline
Agonist - Max activity caused by natural NT Partial Agonist -stabilizer, "Goldilocks solution" Antagonist - blocks action of agonists. Direct vs Indirect. Inverse Agonist |
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Inverse agonist?
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An IA is the opposite of an agonist. It causes total inactivation and reduces activity below baseline.
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What are the 2 types of Ion Channels?
What 4 ions are targetted? |
Ligand-gated (opened by NTS)
Voltage Sensitive (charge) Na+, Ca+, K+, Cl- |
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________ion channels are opened and closed by actions of____. _____of psychotropic meds wrk on these.
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Ligand-gated
NT 20% |
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Immediate change of ions in ____= almost immediate effects
Vs. G-Protein-Linked changes __________. |
Ligand-gated ion channels
that take longer |
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Explain what makes an ion channel pentameric.
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pentameric when assembled from five protein subunits, each with receptor binding sites both inside and outside the channel.
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Explain tetrameric ion channel.
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Belong to ionotropic Glu receptors. 4 protein subunits each w 3 transmembrane regions and a reentrant loop.
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GABA-A is ______cholinergic.
Nicotine desensitizes & inactivates nicotinic cholinergic receptors. Deactivates because it_____ |
Nicotinic
competes at the same sites as Ach - not broken down by enzymes liek Ach |
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a Partial agonist= _______ in presence of full agonist
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net antagonist
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antagonist=______net agonist in presence of _____
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net agonist
inverse agonist |
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PAM=?
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Positive Allosteric Modulation - this boosts NT effect, opens more and more often than Full Agonist alone but only in presence of NT
IE Benzos |
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NAM=?
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Negative Allosteric Modulation - blocks or reduces NT effects, closes more and more often than NT alone
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What is desensitization?
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prolonged exposure to Agonist
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What is inactivation?
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receptor stabilized/closed after Inverse Agonist
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VSSC is ______
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Voltage Sensitive Sodium Channel
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2 types of Voltage Sensitive Ion Channels.
Neuron is ___charged at rest. ___, ____and then K+ all pumped in when neuron fires. |
VSSC and VSCC
(-) Na+, Ca+ |
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VSCC is _________
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Voltage Sensitive Calcium Channel
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Describe the structure of VSCCs and VSSCs
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4 subunits, each with 6 transmembrane regions (#4 is voltage sensitive) and an extracellular loop (ionic filter) form the alpha subunit
May have other regulatory proteins. |
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3 possible states of VSSCs
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1. Open
2. Inactived 3. Closed and inactivated |
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What is excitation secretion coupling?
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Chemical pairing. It is the way in which Sodium and calcium channels work together cooperatively
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Enzymes are the targets. Meds usually work as ______.
___ and ____ are only 2 known targets currently |
enzyme inhibitors
MAO and AChE |
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enzymes have binding sites for _____.
_____ block these from binding. |
Substrates
Inhibitors |
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Descrieb the new model of pscyhiatric genetics
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Genes produce subtle, molecular abnormalities that create bias (or increase risk)
•Environment still important/influential for development of Sx and Dx •Not really a “debate” anymore between nature and nurture Mental Illnesses are symptom mixtures described by characteristic syndromes |
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Define genotype
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What is coded in the DNA
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Define phenotype
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what is expressed as a result of genotype
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Define endophenotypes
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Endophenotypes are the intermediary phenotypes on the pathway between the molecular abnormality encoded by a gene which contributes to risk for mental illness and the mental illness itself. The two types are biological endophenotypes and symptom endophenotypes.
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Explain what VMAT does.
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VMATs are vesicular transporters for monoamines. Each monoamine has its own unique presynaptic transporter but all monoamines utilize the same transporter know as VMAT
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the processes involved in increasing intracellular DA as a result of amphetamine use.
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When DA is recaptured normally into the presynaptic neuron the neurotransmitter molecules are released and then can be taken back up into the neuron by the DAT. Once the DA is back inside the cell, it can be reused again in subsequent neurotransmissions. This process is significantly altered by the presence of amphetamines. Amphetamines inhibit DA at the VMAT and DAT. This causes the displacement of DAT from the synaptic vesicles, which means that massive amounts of intracellular DA are made available.
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List the 5 types of neutrophins. What do they do?
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BNDF
NGF NT3 NT4 NT5 Promote survival of neurons |