Measuring Responce Flashcards

1
Q

What is Kd used for?

A

Measuring the affinity of a drug for a receptor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is efficacy?

A

Affinity and intrinsic activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What is efficacy?

A

A measurement of response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

How are concentration-response relationships plotted?

A

Log[agonist] vs response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What information can be gained from a concentration-response curve?

A

Potency and Intrinsic activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What is potency?

A

A measure of the concentration of a drug needed to elicit a given effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What is EC50?

A

The concentration which gives a maximal response - EC stands for effective concentration

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What is isoprenaline?

A

Modified from adrenaline, additional 2 methyls on the N

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What is a full agonist?

A

Elicits a maximum response even when only a portion of the receptors are occupied

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What is a partial agonist?

A

Cannot induce a maximal response when when all receptors are occupied

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What is intrinsic activity?

A

Ability of the drug-receptor complex to evoke a response.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is a surmountable antagonist?

A

Increasing the concentration of agonist will overcome the block

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What is thrombin?

A

A proteinase-activated receptor - the N-terminal becomes an agonist and binds to the receptor, switching it off

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is pA2?

A

log(Kb) The concentration of antagonist that requires a 2-fold increase in agonist to regain the original response level.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What is the Schild plot?

A

A pharmacological method of receptor classification - also called pA2 analysis.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

What is a non-competitive antagonist?

A

One in which a conformational change is induced by binding to an allosteric site

17
Q

What is physiological antagonism?

A

Functional antagonism - two drugs acting on different sites and eliciting opposing effects

18
Q

What do serine proteinases do?

A

Enzymes involved in degradation and signalling of proteinase-activated receptors.

19
Q

What happens to serine proteinases once activated?

A

They are permanently switched on so have to be internalised and degraded

20
Q

What does vorpaxar/Zontivity do?

A

Acts as a ligand to PAR-1. Prevents thrombin-induced platelet aggregation.

21
Q

What pathway do Gs linked GPCRs stimulate and what can be monitored as a sign of this?

A

Adenylyl cyclase - cAMP

22
Q

What pathway do Gi linked GPCRs inhibit and what can be monitored as a sign of this?

A

Adenylyl cyclase - cAMP

23
Q

What pathway do Gq linked GPCRs activate and what can be monitored as a sign of this?

A

PLC pathway - IP or Ca2+