Part 2 Pharma

Question 1

Specific binding

Answer 1

Binding to receptor of interest

Question 2

Non-specific binding

Answer 2

Binding to other sites

Question 3

Radioligand

Answer 3

Radioactive ligand

Question 4

Goal of saturation binding sites

Answer 4

To determine the KD and Bmax

Question 5

Define IC50

Answer 5

The concentration of the competing ligand which causes a 50 % inhibition of radioligand binding
The lower the IC50 the higher the affinity of the inhibitor for the receptor

Question 6

Define Ki

Answer 6

Equilibrium dissociation constant of inhibitor

Question 7

Into which metabolites is codeine transformed into

Answer 7

Morphine and morphine-6-glucuronide

Question 8

Binding curve

Answer 8

*uses the Bmax equation
*occupation is governed by affinity

Question 9

Effect curve

Answer 9

• uses Emax equation
• Activation is hovered by efficacy

Question 10

Two distinct steps important for generation of receptor-mediated response by an agonist

Answer 10

Ligand binding
Receptor activation

Question 11

What is more efficiently coupled with occupancy-response

Answer 11

Full agonists cause they have high affinity and efficacy

Question 12

Examples of pharmacological responses

Answer 12

Contraction or relaxation of a strip of smooth muscle in organ bath

Question 13

C50 (EC50)

Answer 13

Concentration of the drug needed to cause 50% of maximal response

Question 14

What pharmacological tool is used to study concentration effect curves

Answer 14

Organ /tissue bath