Affinity, Agonist/Antagonists and Potency Flashcards Preview

Pharmacology > Affinity, Agonist/Antagonists and Potency > Flashcards

Flashcards in Affinity, Agonist/Antagonists and Potency Deck (25):
0

What bonds allow for irreversible reactions?

Covalent bonds.

1

What are the three non-covalent bonds?

Ionic bonds, hydrogen bonds and van der waals forces.

2

What % of targets do low affinity drugs target?

25%

3

What % of targets do high affinity drugs target?

50%

4

How can you increase the affinity of a low affinity drug?

By increasing the concentration.

5

Give the three methods of measuring concentration?

Radio ligand binding assay, competition binding and enzymes.

6

Define the term Kd?

The concentration of the drug which is required to occupy 50% of the receptors.

7

What does Bmax stand for?

Maximum binding.

8

Define the term agonist?

A drug which causes a biological response upon binding to its target.

9

Define the term antagonist?

A drug that causes no effect and can be used to block and agonist.

10

In terms of enzymes define an agonists and an antagonist?

Substrate and inhibitor.

11

In the somatic NS what are the agonists and antagonists for a nicotinic receptor?

Acetylcholine and neostigmine

12

In the sympathetic NS what are the receptors used for noradrenaline?

Nicotinic acetylcholine and a and ß receptors

13

What is antagonist that can not be overcome?

An insurmountable antagonist.

14

What can partial agonists act as to full agonists?

Antagonists

15

What % maximum response do full agonists have?

100%

16

What is a competitive surmountable antagonist?

An antagonist which can be overcome with the use of more agonist (reversible).

17

In the parasympathetic NS what receptor is used for acetylcholine and hexamethonum?

Muscat ionic acetylcholine

18

What does EC50 tell you?

About the potency. It is the concentration that produces 50% maximum binding.

19

Does a lower or higher concentration give a lower potency?

Lower

20

Give an examples of an alpha receptor?

Aorta

21

What isoprenaline potency do alpha receptors have?

Low

22

Give an example of ß receptors?

Heart and lungs

23

What are the two ways to measure response?

Signalling assays and isolated tissue.

24

What is IC50?

The concentration of competitor required to remove 50% of the specific binging of the radio ligand.
Lower affinity ligand needs a higher concentration to remove the same amount