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pharmacology class > Neuro-Drug Targets > Flashcards

Neuro-Drug Targets Flashcards

1
Q

What are the major five classes of drug targets

A

1) Membrane receptors
2) Nuclear receptors
3) Ion Channels
4) Transport Proteins
5) Enzymes

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2
Q

What is the very basic order of membrane receptors signal transduction

A

1) Ligand binds
2) Membrane receptors are bound
3) Intracellular signaling intermediates
4) Cellular response

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3
Q

What is the most common membrane protein drug target

A

GCPR

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4
Q

What is the target of dobutamine

A

B1 agonist

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5
Q

What is the process of down-regulation in GCPRs

A

When a true triggers activity in the G protein, it will illicit the result, however over time, as the drug remains, the effect will become desensitized

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6
Q

What the result of a patient on Beta blockers over time that suddenly stops

A

The presence of a beta bloacker will lead to the up regulation of the B2 receptor, but the beta blocker will keep from ever seeing a result. If the patient suddenly stops, they become very sensitive to NE with devastating responses

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7
Q

What must all transcription factors contain

A

DNA binding segment

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8
Q

Where do transcription factors usually bind

A

Promoters or enhancing regions that are adjacent to the coding region of the regulated gene

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9
Q

What is the specific region that a transcription factor will bind to

A

Response elements

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10
Q

What usually occurs at the N-terminal of the GCPR

A

Glycosylated

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11
Q

Where is the N terminal located in the GCPR

A

Extracellular portion

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12
Q

Where is the C terminal of the GCPR located

A

Cytosol

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13
Q

What usually occurs at the C terminal of GCPR

A

Phosphorylated at serine/threonine sites)

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14
Q

What portion of the GCPR contains the G protein binding sites

A

Cytoplasmic loops

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15
Q

Which region of the GCPR usually interacts with cytoplasmic regions upon ligand binding

A

Third cytoplasmic loop connecting regions 5 and 6

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16
Q

What is the event with GCPR that can lead to receptor endocytosis

A

Phosphorylation of the terminal serine and threonine hydroxyl sites

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17
Q

What is the process of ligand binding causing the activation of the GCPR

A

1) Ligand binds and activates the heterotrimeric G protein by the receptor
2) GDP is released and GTP is able to bind
3) GTP bound state is able to activated enzymes/channel
4) GTP is cleaved to GDP in order to deactivate the GCPR

18
Q

The Gs family of GCPR activates which enzymes

A

All adenyl Cyclase and Src Tyrosine kinases

19
Q

What group of enzymes are affected by the Gi family of GCPR

A

Inhibition of adenylyl cyclase, but will activate Src tyrosine kinase

20
Q

What enzymes are affected by the Gq family of GCPR

A

Phospholipase Cbeta

21
Q

Activation of phosphodiesterase results in what effect

A

Breakdown of cAMP and reduction of downstream results

22
Q

What is the result of increase in catalytic subunits

A

Phosphorylation and activation of response elements

23
Q

What is the result of an increase in phophatase activity

A

Removal of phosphates and decrease actions of response elements

24
Q

What is the result of an increase in PLC activity

A

Increase production of IP3 and DAG from PIP2 leading to more activation

25
Q

What is the result of increased activity of PKC

A

Increased phosphorylation of substrates leading to more of a response

26
Q

What are the characteristics of lipophilic drugs with regards to onset and elimination

A

Onset is delayed, but the effects can persist after the drug has been eliminated

27
Q

What is the mechanism of action of steroid drugs

A

1) DNA binding region of receptor is bound by HSP90
2) Drug binds to the ligand binding site, removing HSP90
3) Receptor becomes activated and can affect transcription

28
Q

What type of NT is acetylcholine

A

Excitatory

29
Q

What type of NT is glutamate

A

Excitatory

30
Q

What type of NT is GABA

A

Inhibitory

31
Q

What type of NT is Glycine

A

Inhibatory

32
Q

How doe excitatory NTs work

A

Open cation channels that cause deoplarization

33
Q

How do inhibitory NTs work

A

Open anion channels and move away from threshold, hyper-polarize the cells

34
Q

Binding and activation of nAchR leads to influx of which ion

A

Sodium

35
Q

Binding and activation of GABA receptors allows the flow of which ion

A

Calcium influx and hyperpolarization

36
Q

GABA receptors are the targets for which drugs

A
  • General anesthetics
  • Hypnotic and anti anxiety
  • ethanol
37
Q

What does the SH2 domain bind to

A

Phosphotyrosines

38
Q

What does the SH3 domain bind to

A

Phosphoprolines

39
Q

What is the process of activation of a tyrosine kinase leading to downstream

A

1) TK dimerizes leading to phosphorylated tyrosine
2) P-tyrosines bind to SH2 on Grb2
3) SH3 on Grb2 binds to SOS (a GEF)
4) SOS moved from RAS-GDP to RAS-GTP

40
Q

What is the effect on the level of ENaC and Na/K ATPase with the administration of spironolactone

A

Decreased expression

pharmacology class (7 decks)

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