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74 Cards in this Set

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