UNIT 7: INTRO TO CNS DRUGS Flashcards by lab rat

The CNS is composed of the _ and _

brain and spinal cord

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These are electrically excitable cells that process and transmit information via an electrochemical process.

Neurons

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Inhibits synthesis of serotonin

Parachlorophenylalanine

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Inhibits storage of catecholamines

Reserpine

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Inhibits release of catecholamines

Amphetamine

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Batrachotoxin affects which type of channel?

Sodium Channel

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Apamin affects which type of channel?

Potassium Channel

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Charybdotoxin affects which type of channel?

Potassium Channel

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**Omega-conotoxin **affects which type of channel?

Calcium Channel

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Agatoxin affects which type of channel?

Calcium Channel

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What are the types of voltage-gated channels? (3)

Sodium Channel
Potassium Channel
Calcium Channel

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What are the ligand-gated channels? (4)

Nicotinic ACh Receptor
GABAA Receptor
Glycine Receptor
AMPA Receptor

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Irreversible antagonist for Nicotinic ACh receptor?

a-bungarotoxin

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Blocks GABAA receptor?

Picrotoxin

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Competitive antagonist for Glycine receptor?

Strychnine

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Blocks AMPA receptor?

Philanthotoxin

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Blocks channel from the outside

Tetrodotoxin (TTX)

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Slows inactivation, shifts activation

Batrachotoxin (BTX)

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Blocks small “Ca-activated” K+ channels?

Apamin

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Blocks large “Ca-activated” K+ channels?

Charybdotoxin

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Blocks **N-type **channel?

Omega-conotoxin (ω-CTX-GVIA)

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Blocks **P-type ** channel?

Agatoxin (ω-AGAIVA)

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Depletes monoamine synapses of transmitters by interfering with intracellular storage

Reserpine

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Causes the release of the peptide substance P from sensory neurons

Capsaicin

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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

1. Norepinephrine 2. Epinephrine 3. Dopamine 4. Serotonin

# Enumerate: Amino Acid Neurotransmitters

1. GABA 2. Glycine 3. Glutamate 4. 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

UNIT 7: INTRO TO CNS DRUGS Flashcards

(105 cards)