UNIT 7: INTRO TO CNS DRUGS Flashcards
The CNS is composed of the _ and _
brain and spinal cord
These are electrically excitable cells that process and transmit information via an electrochemical process.
Neurons
Inhibits synthesis of serotonin
Parachlorophenylalanine
Inhibits storage of catecholamines
Reserpine
Inhibits release of catecholamines
Amphetamine
Batrachotoxin affects which type of channel?
Sodium Channel
Apamin affects which type of channel?
Potassium Channel
Charybdotoxin affects which type of channel?
Potassium Channel
**Omega-conotoxin **affects which type of channel?
Calcium Channel
Agatoxin affects which type of channel?
Calcium Channel
What are the types of voltage-gated channels? (3)
- Sodium Channel
- Potassium Channel
- Calcium Channel
What are the ligand-gated channels? (4)
- Nicotinic ACh Receptor
- GABAA Receptor
- Glycine Receptor
- AMPA Receptor
Irreversible antagonist for Nicotinic ACh receptor?
a-bungarotoxin
Blocks GABAA receptor?
Picrotoxin
Competitive antagonist for Glycine receptor?
Strychnine
Blocks AMPA receptor?
Philanthotoxin
Blocks channel from the outside
Tetrodotoxin (TTX)
Slows inactivation, shifts activation
Batrachotoxin (BTX)
Blocks small “Ca-activated” K+ channels?
Apamin
Blocks large “Ca-activated” K+ channels?
Charybdotoxin
Blocks **N-type **channel?
Omega-conotoxin (ω-CTX-GVIA)
Blocks **P-type ** channel?
Agatoxin (ω-AGAIVA)
Depletes monoamine synapses of transmitters by interfering with intracellular storage
Reserpine
Causes the release of the peptide substance P from sensory neurons
Capsaicin
Blocks the release of transmitters, leading to symptoms of tetanus
Tetanus Toxin
Blocks the uptake of catecholamines at adrenergic synapses and thus, potentiates the action of these amines
Cocaine
Inactivated by enzymatic degradation
Acetylcholine
Block the degradation of ACh and thereby prolong its action
Anticholinesterases
Can act as neurotransmitter agonist; mimic the action of enkephalin
Opioids
Blocks the receptor for the inhibitory transmitter glycine
Strychnine
Blocks the NMDA subtype of glutamate ionotropic receptors by binding in the ion channel pore
Ketamine (anesthetic)
Can modify neurotransmitter responses mediated through the 2nd messenger cAMP. It blocks cAMP’s metabolism, thereby prolonging its action
Methylxanthines
Enumerate:
Acetylcholine (ACh) Receptor/Agonist
M1: Muscarine
M2: Muscarine, Bethanecol
Nicotinic: Nicotine
Enumerate:
Dopamine (DA) Receptor/Agonist
**D1: **Dihydrexidine
**D2: **Bromocriptine
Enumerate:
Norepinephrine (NE) Receptor/Agonist
**α1: **Phenylephrine
**α2: **Clonidine
**β1: **Isoproterenol, dobutamine
**β2: **Albuterol
Enumerate:
Serotonin
(5-Hydroxytryptamine) Receptor/Agonist
5-HT1A: Eptapirone
5-HT2A: LSD
5-HT3: 2-methyl-5-HT
5-HT4: Cisapride
Identify:
Acetylcholine (ACh) M2 Receptor/Agonist
Inhibitory/Excitatory?
Muscarine, Bethanecol; Inhibitory
Identify:
Acetylcholine (ACh) M1 Receptor/Agonist
Inhibitory/Excitatory?
Muscarine; Excitatory
Identify:
Acetylcholine (ACh) Nicotinic Receptor/Agonist
Inhibitory/Excitatory?
Nicotine; Excitatory
Identify:
Dopamine (DA) D1 Receptor/Agonist
Inhibitory/Excitatory?
Dihydrexidine; Inhibitory
Identify:
Dopamine (DA) D2 Receptor/Agonist
Inhibitory/Excitatory?
Bromocriptine; Inhibitory
Identify:
Norepinephrine (NE) α1 Receptor/Agonist
Inhibitory/Excitatory?
Phenylephrine;Excitatory
Identify:
Norepinephrine (NE) α2 Receptor/Agonist
Inhibitory/Excitatory?
Clonidine; Inhibitory
Identify:
Norepinephrine (NE) β1 Receptor/Agonist
Inhibitory/Excitatory?
Isoproteronol; Excitatory
Identify:
Norepinephrine (NE) β2 Receptor/Agonist
Inhibitory/Excitatory?
Albuterol; Inhibitory
Identify:
Serotonin (5-Hydroxytryptamine) 5-HT1A Receptor/Agonist
Inhibitory/Excitatory?
Eptapirone; Inhibitory
Identify:
Identify: Serotonin (5-Hydroxytryptamine) 5-HT2A Receptor/Agonist
Inhibitory/Excitatory?
LSD; Excitatory
Identify:
Serotonin (5-Hydroxytryptamine) 5-HT3 Receptor/Agonist
Inhibitory/Excitatory?
2-methyl-5-HT; Excitatory
Identify:
Serotonin (5-Hydroxytryptamine) 5-HT4 Receptor/Agonist
Inhibitory/Excitatory?
Cisapride; Excitatory
Enumerate:
Histamine Receptor/Agonist
- H1: 2(m-fluorophenyl)-histamine
- H2: dimaprit
- H3: R-α-methylhistamine
Identify:
Histamine H1 Receptor/Agonist
Inhibitory/Excitatory?
2-histamine; Excitatory
Identify:
Histamine H2 Receptor/Agonist
Inhibitory/Excitatory?
Dimaprit; Excitatory
Identify:
Histamine H3 Receptor/Agonist
Inhibitory/Excitatory?
R-α-methylhistamine; Inhibitory
Enumerate:
GABA Receptor/Agonist
GABA A: Muscimol
GABA B: Baclofen
Identify:
GABAA Receptor/Agonist
Inhibitory/Excitatory?
Muscimol; Inhibitory
Identify:
GABAB Receptor/Agonist
Inhibitory/Excitatory?
Baclofen; Inhibitory
Enumerate:
Glutamate Receptor/Agonist
- NMDA: NMDA
- AMPA: AMPA
- Kainate: Kainic Acid, Domoic Acid
- Metabotropic: ACPD, quisqualate
Identify:
Glutamate Metabotropic Receptor/Agonist
Inhibitory/Excitatory?
ACPD, quisqualate; Inhibitory
Identify:
Glycine Receptor/Inhibitor
Inhibitory/Excitatory?
Taurine, β-alanine; Inhibitory
Inhibitory/Excitatory/Both:
Acetylcholine
Both
Inhibitory/Excitatory/Both:
Dopamine
Inhibitory
Inhibitory/Excitatory/Both:
Serotonin
Both
Inhibitory/Excitatory/Both:
Histamine
Both
Inhibitory/Excitatory/Both:
GABA
Inhibitory
Inhibitory/Excitatory/Both:
Glycine
Inhibitory
Inhibitory/Excitatory/Both:
Glutamate
Both
Inhibitory/Excitatory/Both:
Opioid Peptides
Inhibitory
Inhibitory/Excitatory/Both:
Orexins
Excitatory
Inhibitory/Excitatory/Both:
Tachykinins
Excitatory
Inhibitory/Excitatory/Both:
Endocannabinoids
Inhibitory
Enumerate:
Monoamine Neurotransmitters
- Norepinephrine
- Epinephrine
- Dopamine
- Serotonin
Enumerate:
Amino Acid Neurotransmitters
- GABA
- Glycine
- Glutamate
- Aspartate
Binding of the neurotransmitter ligand directly opens the channel
Ligand-gated Channels or Ionotropic Receptors
These channels are insensitive or only weakly sensitive to membrane potential.
Ligand-gated Channels or Ionotropic Receptors
Activation of these channels typically results in a brief (a few milliseconds to tens of milliseconds) opening of the channel.
Ligand-gated Channels or Ionotropic Receptors
These channels are responsible for fast synaptic transmission typical of hierarchical pathways in the CNS.
Ligand-gated Channels or Ionotropic Receptors
These are seven transmembrane G protein coupled receptors (GPCRs).
Metabotropic Receptors
Binding to this type of receptor engages a G protein, which results in the production of second messengers that mediate intracellular signaling cascades
Metabotropic Receptors
Respond to changes in the** membrane potential **of the cell.
Voltage-gated Channels
These channels are highly concentrated on the initial segment or axon hillock of the axon
Voltage-gated Channels
EPSPs/IPSPs:
Opening of sodium or calcium channels
EPSPs
EPSPs/IPSPs:
Closing of potassium channels in some synapses
EPSPs
EPSPs/IPSPs:
↑Na+, ↑Ca+2, ↓K+
EPSPs
EPSPs/IPSPs:
Depolarizing potential change
EPSPs
EPSPs/IPSPs:
Opening of potassium channels
IPSPs
EPSPs/IPSPs:
Opening of chloride channels
IPSPs
EPSPs/IPSPs:
Increases K+, Increases Cl-, Decreases Ca+2 (presynaptic)
IPSPs
Hierarchical/Diffused:
Contain large myelinated, rapidly conducting fibers
Hierarchical
Hierarchical/Diffused:
Control major sensory and motor functions
Hierarchical
Hierarchical/Diffused:
These pathways are generally clearly delineated
Hierarchical
Hierarchical/Diffused:
The information is typically phasic and occurs in bursts of action potentials.
Hierarchical
Hierarchical/Diffused:
Major excitatory transmitters: Aspartate, Glutamate
Hierarchical
Hierarchical/Diffused:
Small, inhibitory interneurons transmitters: Gamma amino butyric acid (GABA), Glycine
Hierarchical
Hierarchical/Diffused:
These neurotransmitters are produced by only a limited number of neurons
Diffused (Nonspecific)
Hierarchical/Diffused:
Noradrenergic Amines (NE, dopamine and serotonin)
Diffused
Hierarchical/Diffused:
Broadly distributed, with single cells frequently sending processes to many different parts of the brain tangential
Diffused
Hierarchical/Diffused:
Affects sleeping and waking, attention, appetite, and emotional states.
Diffused
Hierarchical/Diffused:
Because the axons from these diffusely projecting neurons are fine and unmyelinated, they conduct very slowly, at about 0.5 m/s.
Diffused
Acetylcholine Receptor Subtypes
Muscarinic M1
Muscarinic M2
Nicotinic
Dopamine Receptor Subtypes
D1
D2
GABA Receptor Subtypes
GABA-A
GABA-B
Glutamate Receptor Subtypes
NMDA
AMPA
Kainate
Metabotropic
Serotonin Receptor Subtypes
5-HT1a
5-HT2a
5-HT3
5-HT4
Norepinephrine Receptor Subtypes
a1
a2
b1
b2
Histamine Receptor Subtypes
H1
H2
H3