Neurotransmitters Flashcards

(43 cards)

1
Q

What are examples of monoamines?

A
  • epinephrine
  • norepinephrine
  • dopamine
  • serotonin
  • histamine
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2
Q

Where do you find norepinephrine?

A

•locus ceruleus
•other pontine/
medullary areas

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3
Q

Where do you find epinephrine?

A

medulla

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4
Q

Describe the synthesis of neurotransmitters from tyrosine.

A

• Tyrosine -> dopamine -> norepi -> epi
•Tyrosine hydroxylase conversion of tyrosine to DOPA is ratelimiting
step.
•Then moved into vesicles
•NE created
•Neurons that have Phenolethanolamine-N-methyl transferase
(PNMT) convert NE to epi after NE leaves the vesicles
•Epinephrine moved back into vesicles

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5
Q

What type of receptors do norepinephrine and epinephrine bind to?

A

alpha-adrenergic

beta-adrenergic

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6
Q

Which receptors do dopamine bind to, and what are their basic functions?

A

D1 and D5: Gs, increase cAMP

D2: Gi, decrease cAMP and increase K

D3 and D4: Gi, decrease cAMP

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7
Q

Where do you find Dopamine (DA)?

A
  • Basal ganglia (motor control)
  • hypothalamus & limbic system (mood)
  • cortex
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8
Q

Where do you find serotonin (5HT)?

A
  • Brainstem Raphe nuclei (modification of motor activity)
  • hypothalamus & limbic system (mood)
  • cerebellum (modification of motor activity)
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9
Q

What is the precursor for serotonin?

A

Tryptophan, via tryptophan hydroxylase

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10
Q

Which receptors do serotonin bind to?

A

• One ionotropic receptor: 5HT3 (Na influx)
•5HT2c: knock-out mice are obese & seizure
prone
**•5HT3: area postrema (vomiting)
**
•5HT6: anti-depressant effect
•5HT7: limbic system

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11
Q

Where do you find histamine?

A

Tuberomammillary nucleus of Hypothalamus

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12
Q

What is the precursor for histamine?

A

Histidine, via histidine decarboxylase

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13
Q

Which receptors do histamine bind to?

A
  • Serpentine receptors
  • H1: PLC activation
  • H2:  cAMP (associated with gastric acid release)
  • H3: presynaptic, decrease histamine release
  • More H1 and H3 in brain than H2
  • H1 involved in wakefulness
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14
Q

Where is acetylcholine made?

A
  • Striatum of basal ganglia (control of voluntary motion)

- Midbrain and Pons (Baseline excitation to cortex, and REM sleep)

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15
Q

Which receptors do Ach bind to?

A

Nicotinic and Muscarinic
**• M1 (neuronal): increase IP3/DAG, Ca++
• M2 (cardiac): increase cAMP
• M3 (smooth m. of bronchi, vasculature; endothelial cells of vasculature (NO): increase IP3/DAG, Ca++
**
•M4 (presynaptic autoreceptor; striatum of basal ganglia): decrease cAMP (Gi)
***• M5 (cerebrovasculature; dopaminergic neurons of basal ganglia): increase IP3/DAG

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16
Q

What are the two major inhibitory neurotransmitters?

A

-GABA and Glycine

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17
Q

How is GABA synthesized?

A

From Glutamate via Glutamate decarboxylase

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18
Q

How is GABA removed from the synapse?

A
  • GAT1 – on the presynaptic terminal

* GAT2 – on glial cells surrounding the synapse

19
Q

What are features of GABAa Receptors?

A
Believed to be site of many general anesthetics.
• Ionotropic (Cl conductance)
• Activation produces ipsp in
adult neurons.
• Multiple binding sites
modulate:
• Benzodiazepine site
• Ethanol
• Certain steroids
• These all potentiate.
20
Q

What are features of GABAb Receptors?

A
  • Metabotropic
  • Gi/Go protein coupled.
    • Activate a K+ channel (GIRK)
    • Close down (inhibit) a Ca++ channel
  • Located pre- and post-synaptically
    • Presynaptic: regulate NT release
    • Postsynaptic: inhibition of post-synaptic cell
21
Q

Where is Glycine mainly found?

A
  • Spinal Cord (major)
  • Brainstem (medulla)
  • Much less in higher areas of CNS
22
Q

What are some features of the Glycine receptor?

A
• Ionotropic (Chloride)
• Influx of chloride leads to ipsp.
• Ethanol & general anesthetics
bind to it and potentiate.
• Stychnine binds to it and blocks
it.
23
Q

What are some features of the P1 purine receptor?

A
  • ligand = adenosine
  • Post-synaptic locations
    • Sleep induction
    • General inhibition of neural function
  • Pre-synaptic locations
    • Inhibition of neurotransmitter release
24
Q

What are some features of the P2 purine receptors?

A
  • P2X receptors
    • Ionotropic
    • Ligand: ATP
  • P2Y
    • Metabotropic
    • Ligand: ATP, ADP, UTP, UDP
    • Gi/Gq coupled
  • Functions
    • Learning & memory (co-release with EAA)
    • Modification of locomotor pathways
25
Opioids are a family of peptides which include:
- Endorphins - Enkephalins - Dynorphin - Nociceptin
26
What are some features of the Mu opioid receptor?
``` -Leads to an increase in potassium efflux and hyperpolarization. • Analgesia • Respiratory depression • Euphoria • Constipation • Sedation ```
27
What are some features of the Kappa opioid receptor?
``` -Decrease calcium influx. • Analgesia • Dysphoria • Diuresis • Miosis ```
28
What are some features of the Delta opioid receptor?
-Decrease calcium influx. • Produces analgesia when activated.
29
What are functions of endocannabinoids in various parts of the CNS?
* Basal ganglia * Mood * Motor performance * Spinal cord * Modulation of nociception * Cortex * Neuroprotection * Hippocampus * Memory formation * Hypothalamus * Control of body energy/hunger
30
What is a precursor for endocannabinoids?
Membrane arachadonic acid
31
How is the synthesis of the two common endogenous cannabinoids different?
* Anandamide: Derived from N-arachidonoylphosphatidylethanol (NAPE) * 2-AG: Derived from arachidonoyl-containing phosphatidylinositol bis-phosphate (PIP2)
32
What is 2-AG a precursor for in the brain?
major source for Arachidonic acid in certain tissues, especially brain. • Consequence: Pharmacologic manipulation of 2-AG production has wide reaching effects beyond those of the endocannabinoid system.
33
What are some features of the CB1 endocannabinoid receptor?
* Found on pre-synaptic terminals of EAA and GABA releasing synapses * Reduces EAA and GABA release. * Via a Gi coupled protein * Anandamide and 2-AG are equally effective.
34
What are some features of the CB2 endocannabinoid receptor?
-found on microglia • Highly inducible in response to injury or inflammation. • Binds 2-AG better than AEA.
35
What are the Exitatory Amino Acids?
Glutamate and Aspartate
36
What are some features of the NMDA type EAA receptor?
* When activated, the channel allows influx of calcium. * GLYCINE regulatory binding site * is a required co-agonist, but it alone cannot open the channel * Both EAA and glycine must be present for the channel to open. * Magnesium (Mg++) binding site * Within the channel itself * Blocks the channel at resting membrane potential * PCP binding site * Horse tranquilizer * Blocks channel
37
What are some features of the non-NMDA type EAA receptors?
-AMPA • Exogenous agent AMPA activated (really long chemical name, just know AMPA) • Glutamate/Aspartate are the endogenous ligands • Sodium influx when open • Benzodiazepines bind to a site on the extracellular face of the protein • Reduce the amount of sodium that enters. -Kainate similar function
38
How does the response to activation of NMDA and non-NMDA receptors differ?
NMDA type receptors cause an elongated EPSP onset and duration, whereas the non-NMDA type receptors cause a short onset and duration EPSP.
39
How is the function of NMDA and non-NMDA type EAA receptors related?
• EAA released • Binds to both types of receptors • Both non-NMDA and NMDA channels open - • Na+ flows in via the non-NMDA channels • Ca++ cannot enter the NMDA channel because of the Mg++ • The non-NMDA receptor activation produces the typical epsp. • The epsp can provide sufficient depolarization to cause the Mg++ to leave the NMDA channel. • Ca++ now enters the NMDA channel, producing the longer lasting epsp.
40
What are common functions of non-NMDA type EAA receptors?
* Primary sensory afferents | * Upper motor neurons
41
What are common functions of NMDA type EAA receptors?
* Critical in short- and long-term memory formation | * Synaptic plasticity in many forms
42
What are some features of metabotropic EAA receptors?
Divided into three groups (families) • Group 1: Gq coupled • Groups 2 & 3: Gi coupled
43
What are some of the neural functions of NO?
* Memory * Long-term potentiation * In hippocampus & cerebellum * Cardiovascular and respiratory control * Pons and medulla