7 - Antipsychotics Flashcards

1
Q

Which subtypes of the 5-HT receptor are most pharmacotherapeutically important? What types of receptors are they?

A
  • Subtypes 1, 2, 3, and 7

- All are GPCRs, except 5-HT3 is a ligand-gated ion channel

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2
Q

5-HT receptors (subtypes 1, 2, and 4-7) have ____ transmembrane domains

A

7

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3
Q

Where are 5-HT (subtype 1) receptor located? What are their functions?

A
  • Located in CNS, CV, skin, and ileum

- Functions = behavioural, vasoconstriction, and vasodilation

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4
Q

Where are 5-HT (subtype 2) receptor located? What are their functions?

A
  • Located in CNS, CV, respiratory, urogenital, and blood platelets
  • Functions = behavioural, muscle contraction, and platelet aggregation
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5
Q

Where are 5-HT (subtype 3) receptor located? What are their functions?

A
  • Located in CNS and PNS

- Functions = neuronal excitation, anxiety, and emesis

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6
Q

Majority of 5-HT receptors are _____, except ____ which is _____

A

Majority are post-synaptic, except 5-HT1 which is pre- and post-synaptic

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7
Q

Where is serotonin stored? When is it released into blood?

A
  • Stored in platelets

- Released into blood when platelet activating factor concentration is less than 1 nM (too much vasodilation)

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8
Q

What are the most commonly prescribed migraine tx?

A

“Triptans”, potent agonists of 5-HT1B and 5-HT1D receptors

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9
Q

Why does agonism of 5-HT1B and 5-HT1D receptors cause migraine relief?

A

Causes constriction of cranial blood vessels and inhibition of pro-inflammatory mediators

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10
Q

What is buspirone?

A

Long-chain arylpiperazine, which is a non-selective 5-HT1A receptor agonist

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11
Q

What is chlorpromazine?

A

Typical antipsychotic

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12
Q

What are common structural features of typical antipsychotics?

A
  • Either tricyclic or bicyclic w/ EW groups

- Tethered to chain w/ terminal amine

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13
Q

What are some side effects of second gen antipsychotics?

A
  • Weight gain
  • Movement effects (tremor, stiffness, agitation)
  • Sedation
  • Decreased sex drive and function
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14
Q

What is “modelling the pharmacophore”?

A

Using the receptor and seeing which ligands fit into it, and looking at what is important to each molecule for agonist activity

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15
Q

What are the 4 spheres for 5-HT3 receptor pharmacophores?

A

1) Hydrophobic group
2) Aromatic ring 1
3) Aromatic ring 2
4) Basic center (amine)

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16
Q

What are the 3 components that a selective 5-HT reuptake inhibitor must have?

A

1) 2 aromatic rings that are almost perpendicular to each other
2) Basic center (amine) which is 6.6A and 4.1A distance form aromatic rings 1 and 2
3) Hydrophobic group as a substituent for 1 aromatic ring

17
Q

What are the 4 spheres for 5-HT transporter pharmacophores?

A

1) H bond acceptor
2) Aromatic ring
3) Basic center (amine)
4) Hydrophobic group