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Intro to Pharmacology > Pharmacodynamics - Part 3 > Flashcards

Pharmacodynamics - Part 3 Flashcards

1
Q

What are two differnt chemical messengers?

A

NTs and hormones

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2
Q

Neurotransmitters

  • ________ released from ______ endings which travel across a nerve _______ to bind with receptors on target cells, such as _____ cells or another _____.
  • response is usually _____-lived and responsible for messages between ________ cells.
A 
chemical
nerve
synapse
muscle
nerve
short
individual
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3
Q

Hormones:
- _______ released from ______ or ______ and which travel some _______ to bind with receptors on target cells _______ the body

A

chemicals
cells or glands
distance
throughout

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4
Q

Both NTs and hormones are ______ metabolites generated by ______ cells.

A

natural

living

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5
Q

Chemical messengers switch ___ receptors _______ undergoing a reaction.

A

on

without

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6
Q

Hormones can be made of what?

A

Lipids or peptides

i.e. precursors are lipid or protein based

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7
Q

NT precursor is what?

A

amino acids

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8
Q

One cell has many different ________.

A

receptors

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9
Q

Why is epinephrine also called adrenaline?

A

Synthesized from the adrenal glands - adrenaline

Generated from the glands atop kidneys - nephron - epinephrine

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10
Q

What are the major receptor classes?

A

Ion-channel receptors
GPCR
Kinase linked receptos
intracellular receptors

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11
Q

Which receptors are membrane bound?

A

Ion-channel
GPCR
kinase linked

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12
Q

Intracellular receptors are of two types, these are?

A

Nuclear receptors or ligand-activated TF

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13
Q

What is the response time of ion-channel receptors?
GPCR?
Kinase linked receptor?

A

msecs
seconds
minutes

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14
Q

What is the signal transduction step of ion-channel receptors?

A

activation of conductance

- change membrane permeability (potential)

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15
Q

What is the signal transduction step of GPCR?

A

genreation of secondary messenger –> activation of cell signaling

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16
Q

What is the signal transduction step of kinase linked receptor?

A

activation of cell signaling

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17
Q

What is the signal transduction step of intracellular receptor?

A

activation of transcriptoin and translation

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18
Q

Ion channel receptors:

  • _____ response –> ___
  • ideal for transmission between ______
  • binding of messenger leads directly to ____ ______ across the cell memrbane
  • secondary effect = ____ _____ (signal transduction)
  • ion concentration within cell ______
  • leads to variation in cell ______
A 
fast - msec
nerves
ion flow
ion flow
alters
chemistry
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19
Q

Ion channel receptors:

  • cationic ion channels - _______
  • anionic ion channels - _______
A

excitatory

inhibitory

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20
Q

Ion channel receptors are _______ in the membrane

A

embedded

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21
Q

How many subunits does an ion channel receptor have?

How many polypeptides?

A

5

5

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22
Q

How does the ion channel open?

A

Ligand binds and induces a conformational change.

Breaks hydrophobic interactions.

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23
Q

Each subunit of an ion channel receptor has how many TM domains?

A

4

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24
Q

The NT binding region is closest to what terminus for the ion channel receptor?

A

N

25
Q

TM1 is closest to what terminus, TM4?

A

N

C

26
Q

Botox works on which receptor type?

A

Ion channel

27
Q

What are the ligands of ion channel receptors?

A 
Serotonin
(nicotinic - not a natural compound)
Ach
GABA
Glycine
28
Q

GPCR - general principles:

  • Receptor binds a messenger leading to an ______ ___
  • Opens a binding site for a signal protein = _-_______
  • G-protein binds, is destabilized, then _____
A

induced fit
G-protein
split

29
Q

The GPCR is how many polypeptides?

A

1

30
Q

What does ligand binding to the GPCR cause?

A

Conformation change to expose G-protein binding area

31
Q

GPCR - general principles:

  • G-protein subunit activates ________ bound ________
  • binsd to _______ binding site
  • induced fit results in _______ of active site
  • intracellualr reaction catalyzed
A

membrane bound enzyme
allosteric
opening

32
Q

A GPCR is a ______ protein with __ TM domains.

A

single

7

33
Q

The _-terminus is outside the cell, the _-terminus is inside for a GPCR

A

N

C

34
Q

G-protein binding site is closest to what terminus?

A

C

35
Q

What are the ligands of GPCR?

A 
monoamines
nucleotides
lipids
hormones
glutamate
Ca2+
36
Q

Ach that binds to ion channel receptor is referred to as _______; when it binds to a GPCR _______

A

nicotinic

muscarinic

37
Q

Draw the map of Receptor type to subtype for GPCR.

A

refer to slide 19

38
Q

GPCR types and subtypes are not _______ distributed amongst tissues.

A

Equally

39
Q

Heart muscle GPCR subtype?

A

B1 adrenergic

40
Q

Fat cell GPCR subtype?

A

B3 adrenergic

41
Q

Bronchial muscle GPCR subtype?

A

a1 and B2

42
Q

Gi-Tract GPCR subtype?

A

A1, a2, B2

43
Q

What residue is generally phosphorylated?

A

Tyrosine

44
Q

A kinase linked receptor plays two roles, what are they?

A

Receptor

enzyme

45
Q

RTKs are how many proteins?

A

1

46
Q

Describe an RTK.

A

Extracellular N-terminus + ligand binding region
intracellular C-terminus and catalytic region
single TM domain

47
Q

Kinase linked receptors - general principles:

  • protein serves dual role - ______ + ________
  • receptor binds messenger leading to an ______ ____
  • protein changes shape and opens ______ site
  • reaction catalyzed _______ cell
  • _________ related to several cancers
A 
receptor and enzyme
induced fit
active
within
overexpression
48
Q

Ligands that bind to kinase linked receptors tend to be ______.

A

large

49
Q

RTKs tend to _______.

A

dimerize

50
Q

What are RTK ligands?

A

peptide hormones - ex: insulin and HGH

51
Q

Describe the mechanism of action of intracellular receptors.

A 
1 - mesesnger crosses memrbane
2 - binds to receptor
3 - receptor dimerization
4 - binds to co-activator
5 - complex binds to DNA
6 - Transcription switched on or off
7 - Protein synthesis activated or inhibited
52
Q

Messengers for intracellular receptors tend to be what?

A

non-polar

53
Q

TF can ______ or _______ transcription

A

induce or inhibit

54
Q

The intracellular receptor has no ____ domain.

A

TM

55
Q

Describe a typical intracellular receptor.

A

C-terminus
Steroid binding region
Zinc finger with DNA binding region
N-terminus

56
Q

Why are there zinc fingers in intracellular receptors?

A

DNA has a negative charged, zinc is positively charged - allows for binding

57
Q

What part of zinc allows it to coordinate?

A

Cystein residues with SH - allows S-Zn interactions

58
Q

What are the ligands for intracellular receptors?

A 
Steroid hormones
Thyroid hormones
Retinoic acid
Vitamin D3
certain FA and phospholipids

Intro to Pharmacology (23 decks)

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