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74 Cards in this Set
- Front
- Back
Molecule that can bind a receptor
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Ligand
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Ligand that binds to and acivates a receptor
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Agonist
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Lignad that binds to and prevents activation of a receptor
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Antagonist (may or may not be competitive)
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What are the three families of ligand-gated receptors?
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1) ATP 2) ACh, GABA & Glycine 3) Glutamate
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What are the two classes of neurotransmitter action?
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1) Ligand Gated pore 2) 2nd Messenger System
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What are the three families of Glutamate Receptors?
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1) NMDA 2) Kainate 3) AMPA
These are three classical ionotropic glutamate receptors |
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Neither Kainate or AMPA receptors allow ____ to flow whereas NMDA receptor does under certain circumstances/
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Ca2+
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CNQX drugs block which receptors?
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Only Kainate and AMPA- not NMDA
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AAPV drugs block which receptors?
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NMDA - not Kainate or AMPA receptors
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PCD and MK801 block which receptors to produce the effects that resemble hallucination assoc. with schizophrenia?
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Block NMDA receptors
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Antipsychotic drugs enhance the current flow through the _____ receptor channels.
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NMDA receptor channels.
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___ ____ plug the NMDA receptor ionophore at membrane potentals close to rest.
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Mg2+
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What causes the Mg2+ ion plug to be ejected from the NMDA receptor?
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The depolarization of the cell though the entry of Na+ through the AMPA receptor induced by the binding of Glutamate.
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The gutamate receptors can also be activated by what?
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Aspartate (thought to act as a transmitter by some neurons).
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Excitatory amino acids are ________ while inhibotory amino acids are _________.
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Dicarboxylic and Monocarboxylic.
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What are the two inter-related pools of gultamate?
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Metabolic and Transmitter
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Which pool of glutamate is present in all cells?
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Metabolic
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Which pool of glutamate is located in the vesicles of presynaptic neurons?
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Transmitter
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The presence of what near the synaptic junction is critical to help maintain the proper balance in the glutamate system?
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Glia
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Which receptors are involved in Long Term Potentiation?
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NMDA
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Long term potentiation can be prevented by what?
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NMDA agonists: APV or MK-
801 |
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______ _______ produces a lasting change that enables the terminal to release a greater amount of glutamate when subsequently activated.
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Retrograde Signal (results from increased Ca2+ in the cytosol)
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______ removes the Mg2+ block from ________ which, with glutamate, allows Ca2+ to enter the post-synaptic cell.
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Depolarization, NMDA receptor channel
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_____ functions as the key excitatory transmitter in the CNS.
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Glutamate
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NName the two ionotropic receptors that are present throughout the CNS and have channels selective for Cl- ions.
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Glycine and GABA (both have a reversal potential of -70)
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Most common inhibitory transmitter in the CNS
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GABA
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How is Glutamate Acid Decarboxylase (GAD) used?
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As a marker for GABA neurons because GABA is synthesized by this enzyme.
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______ have Cl- ionopore and is responsible for the classical post-synaptic IPSP
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GABA A receptor
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_______ are located pre-synaptically, are metabotropic and impt for presynaptic inhibition.
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GABA B receptors
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____ is taken up by neurons and Glia and recycled via Krebs Cycle and Glutamate.
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GABA
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_______ and ________ both acti via the GABA system by enhancing the binding of GABA to its receptors and potentiating its actions.
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Benzodiazepines and Barbituates
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A drug that acts as a very effcient GABA agonist.
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Baclofen
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What two things synthesize ACh?
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Acetyl CoA and enzyme ChAT.
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_______ is used as a marker for cholinergic receptors in the CNS
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ChAT
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Which toxin acts by binding presynaptically to high-affinity recognition sites on the cholinergic nerve terminals? What effect does this have?
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Botulinum toxin. This decreases the release of ACh and causes a neuromuscular blocking effect.
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Which three toxins bind and inhibit nicotine ACh receptor activity?
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Bungarotoxin, Curare, and Hexamethonium.
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Which toxin blocks re-uptake of choline by high affinity transporter ChT?
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Hemicholinium.
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Which toxin is a reversible inhibitor of Ach esterase?
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Physostigmine (eserine)
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Which toxin is a competetive antagonist for muscarinic ACh receptors (mAChRs)?
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Atropine
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What is the most abundant family of receptors in the CNS?
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Glutamate
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What are the primary inhibitory receptors in the CNS?
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Glycine and GABA
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______ _______ leads to an increase in the amount of glutamate stored in the presynaptic vessicles.
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Retrograde Signal
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Glutamate Toxixity or Excitotoxicity occurs as a result of what?
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Occurs when glutamate (specifically NMDA) receptors are activated excessively and the Ca2+ that enters the cell exceeds its ability to sequester or remove it from the extracellular space.
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The receptors for GABA and Glycine are both ionotropic and selective for which ion?
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Cl-
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GABA-A and Glycine receptors are most commonly found where?
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Postsynaptically
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Which inhibitory neurotransmitter is taken up by glial cells in the region of the synapse and becomes part of the krebs cycle for that cell?
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GABA
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Where are many of the small molecule transmitters synthesized and/or recycled?
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At the nerve terminal
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Which neurotransmitters must be synthesized at the cell body?
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Peptide neurotransmitters
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Peptides that affect neuronal activity and are thought to have modulatory roles in the CNS.
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Neuroactive peptides
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3 types of catecholamines
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Dopamine, Norepinephrine, and Epinephrine
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Type of small molecule transmitters known as indolamines
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Serotonin
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What is the rate limiting enzyme of the pathway creating catecholamine neurotransmitters?
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Tyrosine Hydroxylase.
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What is the immediate precursor to dopamine? How can it be used?
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L-Dopa, it allows by-passing of the rate limiting step in the creation of the catecholamines.
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When dopamine is released from the nerve terminal as a transmitter, how is it removed from the synaptic cleft?
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It is either taken up by the nerve terminal and recycled or broken down by MAO.
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Where is the largest concentration of dopaminergic neurons?
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In the substantia nigra (located in the midbrain)
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Where is the largest concentration of noradrenergic (norepinephrinergic) neurons?
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In the pontine nucleus Locus Coeruleus.
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What is the Locus Ceruleus thought to be involved in?
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Attention, arousal and sleep.
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Where is the largest concentration of of serotonergic neurons?
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In the Nucleus Raphe in the medulla.
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Serotonin that remains in the extracellular space is degraded by what?
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MAO
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Which two neuropeptides are involved in the response to painful stimuli?
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Enkephalins and Substance P
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Which neurotransmitter participates in both the peripheral response to pain and the central response to pain?
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Substance P
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Which neurotransmitter it co-packaged and co-released with almost all other neurotransmitters?
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ATP
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Describe the co-transmission of ATP and adenosine.
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At some synapses in the CNS they are packaged together in the same synaptic vesicle and released together in the neuronal terminals.
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________ is a modulator of the ACh receptor, acting to increase the force of a resulting muscle contraction by mobilizing the 2nd messenger adenylyl cyclase.
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CGRP (calitonin gene-related peptide)
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Term used to describe 2nd messenger mediated events that accounts for the long-lasting effects of some neurotransmission.
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Cascades
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Describe the two modes of action of 2nd messenger systems.
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1. They alter the membrane potential by altering the activity of gated channels
2. They induce metabolic pathways in the cell leading to long-term changes in protein synthesis and function |
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Group of transmembrane proteins that can move about the cell membrane making contact with other transmembrane and cytosolic proteins. Common to all second messenger systems
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G-Proteins
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Processes dependent on G proteins coming into contact with other mobile proteins.
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Collision Coupled Mechanisms
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Enzyme that gives rise to the second messenger cAMP
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Adenylyl Cyclase
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Enzyme that gives to the second messengers inositol polyphosphate (IP3) and Diacyl Glycerol (DAG)
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Phospholipase C
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Enzyme that gives rise to the second messenger arachidonic acid
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phosphlipase A2
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What are the effects of the adnylyl cyclase system giving rise to the release of cAMP?
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Activation of cAMP dependent protein kinases that have short and long term effects on channel function and up-regulate protein synthesis.
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What is the end result of the phospholipase release of IP3-DAG?
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The mobilization of intracellular calcium from the SER which can lead to opening of Ca2+ dependent K+ channels (short-run) and increased protein synthesis (long-run)
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What are the effects of the production of arachidonic acid?
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The production of prostaglandins, leukotrienes and other molecules involved in inflammation.
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