Pharmacodynamics - Part 3 Flashcards

(58 cards)

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?

25
TM1 is closest to what terminus, TM4?
N | C
26
Botox works on which receptor type?
Ion channel
27
What are the ligands of ion channel receptors?
``` Serotonin (nicotinic - not a natural compound) Ach GABA Glycine ```
28
GPCR - general principles: - Receptor binds a messenger leading to an ______ ___ - Opens a binding site for a signal protein = _-_______ - G-protein binds, is destabilized, then _____
induced fit G-protein split
29
The GPCR is how many polypeptides?
1
30
What does ligand binding to the GPCR cause?
Conformation change to expose G-protein binding area
31
GPCR - general principles: - G-protein subunit activates ________ bound ________ - binsd to _______ binding site - induced fit results in _______ of active site - intracellualr reaction catalyzed
membrane bound enzyme allosteric opening
32
A GPCR is a ______ protein with __ TM domains.
single | 7
33
The _-terminus is outside the cell, the _-terminus is inside for a GPCR
N | C
34
G-protein binding site is closest to what terminus?
C
35
What are the ligands of GPCR?
``` monoamines nucleotides lipids hormones glutamate Ca2+ ```
36
Ach that binds to ion channel receptor is referred to as _______; when it binds to a GPCR _______
nicotinic | muscarinic
37
Draw the map of Receptor type to subtype for GPCR.
refer to slide 19
38
GPCR types and subtypes are not _______ distributed amongst tissues.
Equally
39
Heart muscle GPCR subtype?
B1 adrenergic
40
Fat cell GPCR subtype?
B3 adrenergic
41
Bronchial muscle GPCR subtype?
a1 and B2
42
Gi-Tract GPCR subtype?
A1, a2, B2
43
What residue is generally phosphorylated?
Tyrosine
44
A kinase linked receptor plays two roles, what are they?
Receptor | enzyme
45
RTKs are how many proteins?
1
46
Describe an RTK.
Extracellular N-terminus + ligand binding region intracellular C-terminus and catalytic region single TM domain
47
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
``` receptor and enzyme induced fit active within overexpression ```
48
Ligands that bind to kinase linked receptors tend to be ______.
large
49
RTKs tend to _______.
dimerize
50
What are RTK ligands?
peptide hormones - ex: insulin and HGH
51
Describe the mechanism of action of intracellular receptors.
``` 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
Messengers for intracellular receptors tend to be what?
non-polar
53
TF can ______ or _______ transcription
induce or inhibit
54
The intracellular receptor has no ____ domain.
TM
55
Describe a typical intracellular receptor.
C-terminus Steroid binding region Zinc finger with DNA binding region N-terminus
56
Why are there zinc fingers in intracellular receptors?
DNA has a negative charged, zinc is positively charged - allows for binding
57
What part of zinc allows it to coordinate?
Cystein residues with SH - allows S-Zn interactions
58
What are the ligands for intracellular receptors?
``` Steroid hormones Thyroid hormones Retinoic acid Vitamin D3 certain FA and phospholipids ```