Introduction to Pharmacology of CNS Drugs Flashcards
Anandamide is a receptor agonist of?
Endocannabinoids
Which has a Kainate receptor subtype?
A. Acetylcholine
B. Dopamine
C. Glutamate
D. Norepinephrine
C. Glutamate
Which can modify neurotransmitter responses mediated through cAMP?
A. Methylxanthines
B. Strychnine
C. Opioids
D. Endocannabinoids
C. Opioids
Type of voltage-gated ion channel receptor of Agatoxin
Calcium channel
Which is an irreversible nicotinic acetylcholine receptor antagonist?
A. Batrachotoxin
B. alpha-Bungarotoxin
C. Picrotoxin
D. Omega conotoxin
B. alpha-Bungarotoxin
Include all the pathways directly involved in sensory perception and motor control
Hierarchical Neuronal System
Neuronal System of serotonergic pathways
Non-specific or Diffuse Neuronal System
Can modulate voltage-gated channels via a membrane-delimited pathway
Metabotropic receptors
Also known as ionotropic receptors
Ligand-gated ion channels
Glutamate
A. Inhibitory
B. Excitatory
C. Both
D. Neither
B. Excitatory
Acetylcholine
A. Inhibitory
B. Excitatory
C. Both
D. Neither
C. Both
EPSP or IPSP: Opening of postsynaptic calcium channels
EPSP
EPSP or IPSP: Hyperpolarizing
IPSP
GABA
A. Amino Acid
B. Neuropeptides
C. Monoamine
D. None
A. Amino Acid
Histamine
A. Amino Acid
B. Neuropeptides
C. Monoamine
D. None
C. Monoamine
T/F: Nearly all drugs with CNS effects act on a specific receptors that modulates transmission.
TRUE
T/F: CNS drugs are among the most important tools for studying all aspects of CNS physiology
TRUE
Unraveling the actions of drugs with known clinical efficacy led to the hypotheses regarding the mechanism of diseases, such as?
Alzheimer’s disease, Parkinson’s disease, Addiction
The excesses or deficiencies of chemicals in the brain would result to?
Diseases
Holds on the blood vessels to prevent excessive sodium, and will not allows drugs to readily affect the nervous cells
Astrocyte
Oligodendrocytes in the peripheral NS?
Schwann cells
Schwann cells in the central NS?
Oligodendrocytes
T/F: Synapses with another neuron comes into contact with one another
FALSE, they do NOT come in contact
T/F: Most drugs that act on the CNS do so by changing ion flow through transmembrane channels of nerve cells
TRUE
T/F: All channel types can be affected reversibly, competitively, and inhibited by several chemicals except for Potassium and Calcium channels
FALSE
What are the 2 toxins that characterize sodium channels?
Tetrodotoxin (TTX)
Batrachotoxin (BTX)
What are the 2 toxins that characterize potassium channels?
Apamin
Charybdotoxin
What are the 2 toxins that characterize calcium channels?
Omega-conotoxin (ω-CTX-GVIA)
Agatoxin (ω-AGAIVA)
Sodium, potassium, and calcium channels are what type of channels?
Voltage-gated channels
What is the toxin that characterize the nicotinic ACh receptor?
ɑ-Bungarotoxin
What is the toxin that characterize GABA A receptor?
Picrotoxin
What is the toxin that characterize glycine receptor?
Strychnine
What is the toxin that characterize AMPA receptor?
Philanthotoxin
What are the 4 different receptors in Ligand-gated channel?
Nicotinic ACh receptor, GABA A receptor, Glycine receptor, AMPA receptor
What are the two types of gated channels?
Voltage Gated Channels
Ligand Gated Channels
Nerve cells contain two types of channels defined on the basis of the mechanism controlling the?
Gates (opening and closing)
Respond to changes in membrane potential
Voltage-Gated Ion Channels
Voltage-Gated Ion Channels are concentrated on the?
Axon hillock/ initial segment of the axons
T/F: Voltage-gated ion channels are responsible for slow action potentials
FALSE, they are responsible for FAST action potentials
2 Classes of Neurotransmitter Receptors
Ligand-gated ion channels (ionotropic receptors)
Metabotropic receptors
Chemically-gated
Ligand-gated ion channels
Respond the chemical neurotransmitters that binds to receptor subunits of the channel
Ligand-gated ion channels
G-protein coupled
Metabotropic receptors
T/F: Binding to a metabotropic receptor results in direct gating of a channel?
FALSE, it is indirect
Binding to a metabotropic receptor engages the G-protein that results into the production of?
Second messengers
Modulates the voltage gated channels intracellularly
Second messengers
Drug mimics what chemical?
Endogenous chemicals
What are the 2 membrane delimited pathways?
Potassium and Calcium channels
3 examples of second messengers?
Cyclic adenosine monophosphate (cAMP)
Inositol triphosphate (IP3)
Diacyclglycerol (DAG)
Are EPSPs hyperpolarizing or depolarizing?
Depolarizing, it is excitatory
Are IPSPs hyperpolarizing or depolarizing?
Hyperpolarizing, it is inhibitory
Depolarizing potential change
EPSPs
EPSPs can be generated by opening what channels?
Sodium and Calcium channels
EPSPs can be generated by closing what channels?
Potassium channels
T/F: In EPSPs, closing a potassium channel would make the membrane negative.
FALSE, it would make the membrane more positive
Hyperpolarizing potential change
IPSPs
IPSPs can be generated by opening what channels?
Potassium and Chloride channels (postsynaptic)
T/F: IPSPs can be generated by opening potassium channels in the presynaptic.
FALSE, it should be postsynaptic
IPSPs can be generated by closing what channels?
Calcium channels (presynaptic)
T/F: EPSPs may not readily reach the threshold
TRUE
Several excitatory potential coming from different communicating neurons which causes higher depolarization, reaching the threshold causing an action potential to be generated
Spatial summation
Subsequent EPs
Temporal summation
__PSPs are important in preventing seizure/ epilepsy
IPSPs
Some drugs exert their effect through __________ interactions with molecular components of ion channels on axons
Direct
Drugs that exert their effect through direct interactions on axons
Carbamazepine, Phenytoin, Local anesthetics, General anesthesia
Most drugs exert their effect mainly at the _____________
Synapses
Drugs may act presynaptically to alter?
Synthesis, Storage, Release, Reuptake, Metabolism
T/F: You cannot prevent the action potential propagation by blocking ion channels?
FALSE, sa axon palang, you can prevent it na
Myasthenia gravis can be attributed to the problem of?
Presynaptic storage
T/F: Neurotransmitters need to be stored so that when an action potential comes in, it will be able to release it.
TRUE
Ionic conductance can be accomplished through __________-______________ ________________ receptors
Membrane-delimited metabotropic receptors
This sends signal to inhibit release because the postsynaptic neuron is overly stimulated
Retrograde signaling
Reuptake is processed in the?
Glial cells
Inhibits synthesis of serotonin
Parachlorophenylalanine
Inhibits synthesis of cathecolamines
Reserpine
Inhibits release of catecholamines
Amphetamine
Inhibits degradation of Acetylcholine
Anticholinesterase
T/F: Amphetamine is used for Myasthenia gravis.
FALSE, Anticholinesterase is used
Contain large myelinated, rapidly conducting fibers
Hierarchical System
Control major sensory and motor functions
Hierarchical System
Type of neuronal system responsible for excitability of the CNS
Hierarchical System
Hierarchical system is modulated by _________ to be able to control how much muscle contraction will occur
Interneurons
Major excitatory transmitters of hierarchical system
Aspartate, Glutamate
Small inhibitory interneurons transmitter of hierarchical system
Gamma amino butyric acid (GABA), Glycine
Broadly distributed, with single cells frequently sending processes to many different parts of the brain-tangential
Diffused or Non-specific Neuronal System
T/F: In neuropsychiatry, it is hard to determine unless the neurotransmitter is the one that is primarily affected
TRUE
Substantia nigra is associated with?
Dopamine
Locus coeruleus is associated with?
Norepinephrine
Raphe nuclei is associated with?
Serotonin
Nucleus Basalis of Meynert and Cholinergic nuclei 5-8 is associated with
Acetylcholine
Periodic enlargements that contain transmitter vesicles
Varicosities
Varicosities are located in the?
Axons
Transmitters for Diffused/ Non-specific neuronal system
Noradrenegic Amines (Norephinerine, Dopamine, Serotonin)
Peptides (act on metabotropic receptors)
T/F: Transmitters for hierarchical neuronal system are found primarily in a compact cell group called caeruleus in the caudal pontine central gray matter.
FALSE, Diffused/ non-specific neuronal system
Marked effects of Diffused/ non-specific neuronal function on CNS functions
Attention, Appetite, Emotional states
Criteria for Transmitter Status
- High concentration in synaptic area (localized)
- Released by electrical or chemical stimulation by calcium-dependent mechanism
- Synaptic mimicry
Produce the same sort of postsynaptic response that is seen with physiologic activation of the synapse
Synaptic mimicry
How many percent of neurons have transmitters for ACh?
5%
G protein-coupled muscarinic M1 receptors
Acetylcholine (ACh)
Is ACh fast or slow? Excitation or inhibitory?
Slow excitation
ACh ___________ permeability to potassium
Decrease
Dopamine ____________ actions at synapses in specific neuronal systems
Inhibitory
G protein-coupled activation of potassium channels
Dopamine
Main dopamine subtype
D2 receptor
Dopamine increases?
cAMP
Norepinephrine excitatory effects
Activation of ɑ1 and β1 receptors
Decrease potassium conductance
Norepinephrine inhibitory effects
Activation of ɑ2 and β2 receptors
Increase potassium conductance
Serotonin has multiple _________________ receptor subtypes
5 hydroxytryptamine (5-HT)
Serotonin is ___________ at many sites
Inhibitory
Serotonin is _____________ depending on the receptor subtype activated
Excitatory
T/F: Serotonin is metabotropic.
TRUE
Glutamic acid for most neurons is?
Excitatory
Receptor for glutamic acid
N-methyl-D-aspartate (NMDA)
NMDA is responsible for?
Learning and memory
Glutamic acid inhibits?
Adenyl cyclase
mGluR in glutamate has _________ reaction
Slower
AMPAR and NMDAR in glutamate have ____________ response
Quicker
Enzyme converting Glutamine to Glutamate
Glutaminase
Primary NTA mediating IPSPs
GABA
GABA A receptor activation
Opens chloride conductance
GABA B receptor activation
Opens potassium channels
Closes calcium channel
Glycine is more numerous in the?
Spinal cord
Glycine causes?
Chloride conductance
GABA and Glycine causes?
Postsynaptic inhibition (hyperpolarization)
Beta-endorphins, Dynorphins
Opioid Peptides
Opioid presynaptic inhibitory
Decrease calcium conductance
Opioid postsynaptic inhibitory
Increase potassium conductance