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D2: 609 Pharm and Pain Control > 01: Dose Response Relationship > Flashcards

01: Dose Response Relationship Flashcards

1
Q

What are the 4 general classes of receptors

A

Ion Channel
G Protein
Tyrosine Kinase Receptors
Binding/Transportation to Nucleus (Chemotherapeutics)

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2
Q

What is the process that occurs after a drug binds a receptor and leads to a drug response?

A

Transduction

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3
Q

What type of receptor is a ligand-gated ion channel?

A

Ionotropic

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4
Q

What type of receptor links a drug to internal cell mechanisms through a G-Protein

A

Metabotropic

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5
Q

Which receptor type will make use of 2nd messengers like cAMP, AC, etc? (Ionotropic or Metabotropic)

A

Metabotropic

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6
Q

What is the general structure of an Ion channel receptor?

A

Protein pores in the plasma membrane

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7
Q

When a drug binds to an ion channel receptor it causes a conformational change, but what actually triggers a cellular response?

A

The change in ion concentration resulting from the ion channel opening (or closing)

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8
Q

What is the difference between an IPSP and an EPSP ion channel receptor?

A

IPSP = Inhibitory drug ligand

EPSP = Excitatory drug ligand

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9
Q

What type of sodium channels are cholenergic receptors?

A

Ligand-gated

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10
Q

What stimulus opens a voltage gated sodium receptor? (Hyperpolarization or Depolarization)

A

Membrane DEPOLARIZATION

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11
Q

What stimulates the opening of a cholenergic sodium channel receptor?

A

Acetylcholine (Ach)

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12
Q

What ligand is associated with Nicotinic ligand-gated channels?

A

Ach

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13
Q

What are the two types of Metabotropic receptors?

A
  1. activated alpha subunit (of G protein) binds and opens ion channel directly
  2. activated alpha subunit binds to a membrane enzyme, which activates a 2nd messenger to open ion channel.
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14
Q

What are 2 classic examples of the membrane enzyme that is activated by the alpha subunit in Metabotropic receptors?

A 
Adenylyl Cyclase (AC)
Phospholipase C
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15
Q

What is the second messenger that is activated by Adenylyl Cyclase in the Metabotropic transduction pathway?

A

cAMP

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16
Q

After cAMP is activated by AC, what is the next molecular messenger in the Metabotropic transduction pathway?

A

Protein Kinase A (PKA)

17
Q

In the Phospholipase C transduction pathway what is the second messenger that PLC activates?

A

IP3

18
Q

After IP3 is activated it travels to its target Calcium ion channel which is located on the membrane of which organelle?

A

ER

19
Q

If cAMP and IP3 are second messengers, what are the first messengers?

A

The original signal molecules that bind to the G protein receptor (e.g. Epinephrine, Norepinephrine, etc.)

20
Q

What is the polypeptide structure of a G Protein Receptor?

A

It is a single polypeptide in an alpha-helix configuration

21
Q

How many times does each G Protein Receptor Polypeptide transverse the cell membrane

A

7

22
Q

Which end of the GPCR polypeptide is on the cytosolic side of the membrane (NH3+ or COO-)?

A

COO-

23
Q

G proteins are trimeric. What are the names of their 3 subunits?

A

Alpha

Beta/Gamma

24
Q

When a G protein is in its rest state, what molecule is it bound to?

A

GDP

25
Q

When a ligand activates a GPCR what happens to the GDP on the g protein?

A

It leaves and is replaced with GTP. The Alpha subunit dissociates from the Beta/Gamma

26
Q

What must happen in order for the G protein to return to its resting state (bound to GDP)?

A

The extracellular ligand must dissociate from the GPCR

27
Q

What molecule actually converts GTP to GDP when the G protein is returning to its resting state?

A

The G protein hydrolyzes its own GTP through the use of intrinsic hydrolytic functionality

28
Q

What are the two sub-types of G protein that we will be dealing with in this course?

A

Gs (stimulatory)

Gi (inhibitory)

29
Q

What G protein subtype is used in muscarinic GPCR’s

A

Gi

30
Q

Why is the Gi protein considered inhibitory?

A

Because when Gi’s alpha subunit effects AC, it inhibits it.

31
Q

What are RGS protein?

A

They are the proteins that “Reset” the G protein to its basal state

32
Q

What is the effect of the alpha subunit of a Gs protein?

A

Increased activation of AC and increased cAMP

33
Q

What is the effect of the alpha subunit of a Gi protein?

A

Inhibition of AC and decreased cAMP

34
Q

What is the importance of Gi vs. Gs and their respective effects of intracellular cAMP levels?

A

Because that is the pharmaceutical effect (Mechanism of Action) of the GPCR related drugs that we will be studying in this course

35
Q

What is the GPCR related consequence of Opiods?

A

Opiods activate Gi/ALPHAi thereby inhibiting cAMP production eventually leading to an analgesic effect.

36
Q

The third most important subtype of G proteins is the Gq subtype….what is its effect?

A

Increased activation of PLC and increased levels of intracellular Ca++

37
Q

A less common G protein subtype is Go, how does it work?

A

In a very similar fashion to Gi

38
Q

What type of G protein would be associated with these pathway molecules:

PIP2, PLC, DAG, IP3, PKC

A

Gq

D2: 609 Pharm and Pain Control (16 decks)

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