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Receptors Flashcards

1
Q

Which opiate receptor has the highest affinity for morphine

A

Mu receptor

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2
Q

What are endorphins and enkephalins

A

Endogenous ligands for opiate receptors

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3
Q

Drug definition

A

A known chemical structure which when administered to a living organism produces a biological effect

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4
Q

Types of drugs

A

Synthetic chemicals, plant chemicals and biopharmaceuticals

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5
Q

What is a biopharmaceutical

A

Something that is made from DNA

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6
Q

Medicine definition

A

A chemical preperation that contains one or more drugs admnistered to produce a therapeutic effect

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7
Q

What other compounds do medicines contain

A

Excipients, stabilizers and solvents

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8
Q

Examples of biopharmaceuticals

A

Proteins (could be endogenous), engineered proteins, antibodies, oligonucleotides, gene therapy and regenerative medicine

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9
Q

What is the first generation of biologics

A

Copies of endogenous proteins produced by recombinant DNA technology

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10
Q

What is the second generation of biologics

A

Engineered proteins to improve antibodies

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11
Q

Benefits of biologics

A

Your body doesn’t accept them but treats them as another human antibody

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12
Q

What can biologics be used for

A

Treating cancer and immune diseases

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13
Q

What does MAB mean at the end of a drug name

A

Monoclonal antibody

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14
Q

What does Humira do

A

Recognises an inflammatory mediator known as TNF alpha

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15
Q

How much does Humira cost

A

14,000 million

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16
Q

What is the basis of the Moderna vaccine to treat COVID

A

Injecting people with mRNA that codes for a protein

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17
Q

What is Pharmacoeconomics

A

Considers the cost benefit of a drug

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18
Q

What kind of proteins do drugs exert their actions on

A

Receptors, enzymes, transporters, ion channels

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19
Q

What macromolecules other than proteins can drugs exert their actions on to

A

Antibiotics and antimicrobials

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20
Q

How are receptors classified

A

Structure, pharmacology, signalling mechanisms

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21
Q

What can increasing the dose of a drug do and why

A

Lead to unwanted side effects because no drug is 100% selective and specific

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22
Q

What can malfunction and loss or receptors lead to

A

Disease

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23
Q

What is an agonist

A

A drug that causes the receptor to switch on and bring about a change within the cell once bound to

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24
Q

What is an inverse agonist

A

When bound to a receptor, they reduce signalling to that receptor

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25
What are antagonists
When bound to receptor, they do nothing and blocks the receptor from carrying out its action
26
What is morphine an agonist for
Mu receptor
27
What are Mu receptors
They are g-coupled receptors in the location of the brain that processes pain and reward pathways
28
What are blockers (drugs) and example
They enter the pore of the channel and prevent ions from moving through them. For example, Lidocaine
29
What are modulators (drugs) and example
They modify the way the channel behaves, can open more or less. For example, Valium
30
What does Lidocaine target
sodium channels that send information to the brain when you have a painful incident
31
What do enzyme inhibitors do and example
The normal reaction is inhibited. For example, aspirin
32
What do enzyme false substrates do
The molecule enters into the enzyme to produce something that is inactive/ abnormal metabolite is produced
33
What do prodrug enzymes do
Active drug is produced
34
Examples of transporter drugs
Prozac and digoxin
35
What does Colchicine do
Disrupts the cytoskeleton and inhibits the invasion of immune cells into the inflamed joint
36
What does Paclitaxel do
Targets and prevents the diasembly of microtubules
37
What does Paclitaxel do
Targets and prevents the disassembly of microtubules to stop cell division
38
Main side effects of opiate
Chronic constipation and respiratory issues
39
Why is knowing where the receptor is in the body important
Helps us predict drug affects
40
Examples of agonists for the MU-receptor
Morphine, heroin, methadone, codeine, fentanyl, beta-endorphins
41
What is a ligand
Any molecule that binds to the receptor
42
Examples of antagonists for the MU- receptor and what does it do
Naloxone, stops heroin activation
43
What are the 4 types of receptor
Ligand- gated ion channels, g- coupled protein receptors, kinase linked receptors, nuclear receptors
44
What is the largest class of receptor
G- coupled
45
What is kinase
Any protein which has enzymatic activity that adds phosphate to another protein
46
What are the fastest receptors
Ligand gated
47
Slowest receptors
Nuclear (take a couple of hours
48
What is the basic mechanism for ligand gated ion channels to open
Ions flow through aqueous pore which is opened when neurotransmitter/ agonist binds. Flow of ions leads to changes in membrane potential causing action potentials to fire
49
Examples of ligand gated ion channels and the number of transmembrane domains
Nicotinic, 4 Glutamate, 3 P2XR, 2
50
What happens when agonist binds to g-coupled receptors
They signal the change by activation of a g protein
51
What are the g protein subunits in g coupled receptors
Alpha, beta and gamma
52
What is the alpha subunit less attractive to (what happens next)
GDP so has a greater affinity to GTP. When GDP comes off GTP comes on
53
What happens to the alpha subunit over time
It becomes a nuclear kinase
54
What does activation of kinase receptors lead to
Changes in transcription
55
What are cytokine receptors useful for
Regulate within the nucleus
56
What is an important feature of nuclear receptors
They bind directly to DNA to regulate the transcription of genes
57
What percentage of the mammalian genome is regulated by nuclear receptors
1%
58
What is an autoimmune disease
Makes an antibody to itself and the target can be a receptor
59
What is Myasthenia Gravis
Antibodies to nicotine acetylcholine receptors involving muscle contractions
60
What is Gravis disease
Where a thyroid receptor is targeted leading to high metabolic rate, increased skin temperature
61
What can epilepsy be caused by
A mutation leading to increased stimulus to a receptor
62
What do mutations in the beta- 2 adreno receptors lead to
Means that inhalers don't work
63
What is affinity
A chemical property that defines how likely they are to come together
64
What is the constant for the forward and backward reaction
K+1 and K-1
65
What is how good a molecule is at fixing a receptor governed by
efficacy
66
What is the number of receptors that are occupied by a drug in one point of time determined by
affinity
67
what is KD
A constant that defines the affinity of a drug for that receptor
68
What is the forward rate of a reaction defined by
The forward rate constant multiplied by the concentration of the agonist and concentration of receptors
69
What is the order of reaction for the forward rate and why
Second order because it depends on the concentration of two types of molecules
70
What is the reverse rate of reaction equation
k-1[AR]
71
What is the dissociation constant equal to
The reverse reaction divided by the forward reaction
72
What is KD a direct measurement of
affinity
73
What is occupancy governed by
Affinity
74
Equation for occupancy
number of receptors occupied/ total number of receptors
75
What does occupancy vary between
0 (no drug present) and 1 (all receptors occupied)
76
How do we measure affinity
Radioligand binding assay
77
What are the steps for measuring receptor affinity
Mix these two together, incubate them and filter the sample so only thing left is the receptors bound radioligand, then analyse the data
78
what are some considerations for measuring receptor affinity
Controlling the temperature so proteins aren't digested Adding antioxidants in case the molecules released from the cells are oxidisable Free radical scavenger to stop degradation Avoiding light
79
What must the radioligand be in measuring receptor affinity
Must be biologically active and pure chemically
80
Advantages of using hydrogen in measuring receptor affinity
Won't cause issues to the structure, affinity will be maintained Powerful radioactive substance Long half life
81
Disadvantages of using hydrogen in measuring receptor affinity
Specialised labs required, labelling is expensive and difficult
82
Advantages of using iodine in measuring receptor affinity
Similar size of aromatic amino acids Chemistry involved is straight forward
83
Disadvantages of using iodine in measuring receptor affinity
Easily degradable, more radical change in structure of the molecule
84
How do you separate the bound from the free in measuring receptor affinity
Wash away the none bound drug
85
What is non-specific binding
The ligand will bind to other things in addition to the receptors e.g. plastic test tube
86
How to stop non-specific binding
Setting up two test tubes in parallel, add a known concentration of radioactive drug to one and a huge excess of non-radioactive drug to the other Non-radioactive drug will outcompete radioactive drug Subtract non-specific binding from the total to get the specific binding
87
What does affinity give us an indication of
What levels, of drug are needed in the body to have a therapeutic effect and a way of identifying and defining the type of receptor
88
What kind of relationship do we get between the concentration and the amount of binding
Sigmoidal
89
What happens to the values in a sigmoidal relationship
They plateau, shows 100% occupancy
90
What does 100% occupancy mean
100% of the receptors in that tissue are occupied by that drug
91
What is the Langmuir equation
Bound= bmaxXa/ (Xa + KD)
92
The concentration that occupies 50% of the total number of receptors present gives us a direct measure of what
KD
93
What does a low KD show
High affinity
94
What can the drug Pirenzepine distinguish
Distinguishes between the subtypes of muscarinic receptora

Biology (9 decks)

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