Lecture 10: Neurotransmission and Drugs Flashcards

1
Q

Binding of Neurotransmitter to receptor

A
  • NT binds to receptor
  • Receptor is activated
  • Like a key and lock (usually not 1:1 exclusive either way)
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2
Q

Ligand

A

Molecule that binds to a receptor (key)

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3
Q

Catecholamines

A
  • Adrenaline, noradrenaline, dopamine
  • Similar structures
  • Can be either EPSPs or IPSPs depending on receptor
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4
Q

Epinephrine/Norepinephrine

A
  • Also called adrenaline/noradrenaline
    -General function: mobilize brain and body (fight or flight): increases arousal, respiration, blood flow to muscles, pupil dilation, and release of glucose
  • Acts as both neurotransmitters and hormones based on if they are in the brain or blood
  • Produced in small structures but project broadly
  • Adrenaline is produced in the adrenal glands and medulla
  • Noradrenaline is produced in the brain in the locus coerculeus and outside the brain in the ganglia, skin, and adrenal glands
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5
Q

Locus Coeruleus

A
  • Located in brain stem
  • Responsible for stress, attention, and noradrenaline
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6
Q

Raphe Nuclei

A
  • Located in brain stem
  • Responsible for arousal, pain, and serotonin
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7
Q

Superior Colliculus

A
  • Located in brain stem
  • Responsible for vision
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8
Q

Inferior Colliculus

A
  • Located in brain stem
  • Responsible for hearing
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9
Q

Ventral Tegmental Area (VTA)

A
  • Located in brain stem
  • Responsible for dopamine, motivation, and arousal
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10
Q

Substantia Nigra

A
  • Located in brain stem
  • Responsible for movement and dopamine
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11
Q

Dopamine

A
  • Involved in movement, reward-seeking, and motivation
  • Produced in the substantia nigra and ventral segmental area (VTA)
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12
Q

Dopamine Receptors

A
  • Has D1 and D2 receptors with different roles
  • Two locks opened by the same key
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13
Q

Serotonin (5-HT)

A
  • “Happiness neurotransmitter”
  • Also involved in sleep and appetite
  • Anti-depressant drugs increase serotonin
  • Produced in the raphe nuclei
  • Can be EPSP or IPSP
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14
Q

Opioids

A
  • Endorphins and enkephalins
  • “Natural morphine”
  • Released in happiness, laughter and euphoria
  • Also in pain reduction and reward
  • Mixed EPSP and IPSP
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15
Q

Nitric Oxide

A
  • “Reverse neurotransmitter”
  • Soluble gas (NO) in dendrites
  • Generated by postsynaptic enzyme in response to neurotransmitter
  • Leaks out of dendrite
  • Enters presynaptic neuron
    - Needs no membrane receptor
  • “Retrograde signaling”
  • Influences pre-synaptic mechanisms of neurotransmission
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16
Q

Agonists

A

Turns on neurotransmitter system (EPSP or IPSP)
- Presynaptic: Release neurotransmitter
- Postsynaptic: Activates receptor

17
Q

Antagonists

A

Turns off neurotransmitter system
- Presynaptic: Prevents release
- Postsynaptic: Blocks receptors

18
Q

Inverse Agonists

A
  • Postsynaptic: Binds to receptors but induces opposite effect
19
Q

Presynaptic Agonist: Parkinson’s Disease (L-Dopa)

A
  • Parkinson’s Disease- reduced dopamine levels
    - Medication: L-Dopa (dopamine precursor)
    - Molecule that the brain can use to make more dopamine
    - Can’t provide dopamine directly because it cannot pass the blood-brain barrier
19
Q

Presynaptic Agonist: Cocaine

A
  • Inhibits reuptake of dopamine by blocking dopamine transporter
  • Leaves more dopamine in the synaptic cleft causing it to bind to receptors more frequently than normal
20
Q

Presynaptic Agonist: Amphetamine

A
  • Blocks and reverses dopamine transporter
  • Increases levels of dopamine and norepinephrine
  • Stimulation, euphoria, wakefulness, improved cognitive control
  • Treatment of ADHD, narcolepsy, depression; athletic performance enhancer
  • Adderall: Prescribed combination of amphetamine and dextroamphetamine
21
Q

Presynaptic Agonist: Selective Serotonin Reuptake Inhibitors (SSRIs)

A
  • Blocks reuptake of serotonin
  • Commonly prescribed antidepressant (prozac)
22
Q

Postsynaptic Agonist: Morhpine and Heroin

A
  • Activate post-synaptic opioid receptors
  • Euphoric, pain relief
  • Mimics endorphins and enkephalins
22
Q

Postsynaptic Agonist: Synthetic Opiods; Fentanil and Carfentanil

A
  • Fentinal 100x more potent than morphine
  • Carfentanil is 100x more potent than fentinal
  • Pain relief, tranquilizer darts
  • Overdose inhibits brainstem breathing circuits
23
Q

Postsynaptic Agonist: Benzodiazepines

A
  • Xanax, Valium
  • Sedative, hypnotic, anxiolytic, anti-epileptic, muscle relaxant
  • Binds to GABA receptors and facilitates GABA effects
  • Both it and GABA bind to receptors, and more Cl flows through
24
Q

Postsynaptic Antagonist: Antipsychotics

A
  • Drugs for schizophrenia (pimazide, haloperidol)
  • Blocks D2 dopamine receptors
  • Prevent dopamine from activating
  • Atypical antipsychotics block serotonin as well as dopamine receptors
25
Q

How do drugs reach the synapse?

A
  • The drug goes into the blood stream, then into the brain through the blood-brain barrier
  • Drug gets to the blood stream in a few ways
    - Oral ingestion (digestive system can decompose the drug, but it is easier)
    - Injection
    - Inhalation (short route to brain)
26
Q

Receptor Down-Regulation

A
  • When there is a lot of a neurotransmitter/activator, the neuron reduces the amount of receptors to keep a baseline level of activation
  • You need more of the drug to get the same effect, which closes more receptors and so on
  • For something like chocolate, when you eat too much you may not enjoy it as much for this reason
  • Can cause withdrawal (under-activation)
27
Q

Neural Sensitization

A
  • Hyper-responsive to drug
  • Dopamine sensitization and addiction (wanting vs. liking)
28
Q

Neurotoxicity

A
  • Repeated exposure to a drug (often in large amounts) can kill cells
  • Amphetamine can kill dopamine neurons, but is toxic at 10x the street dose