agonists

Question 1

—- is a chemical that specifically bind to a receptor

Answer 1

Ligand

Question 2

—- a ligand which binds to a receptor and causes biological response

Answer 2

agonists

Question 3

—- binds to a receptor but has no effect and prevents other ligands from binding

Answer 3

antagonist

Question 4

receptors possess — affinity for its endogenous ligand at —– concentration

Answer 4

• high
• physiological

Question 5

true or false:
-receptors are saturable and finite ( limited number of biding sites )
- receptor structure has evolved over time to recognise specific ligands
- often more than one ligand and different ligands can promote different receptor signalling
- once receptor expressed in different titssue can mediate distinct physiological outcomes

Answer 5

true

Question 6

once the endogenous ligand binds to a receptor —- event occurs

Answer 6

biochemical

Question 7

tissue response are generally —- to the — of the receptors occupied with agonist
more occupied receptors = —–
- leads to : —- curve

Answer 7

• directly proportional
• fraction
• bigger signalling response
• dose response ( check slide 8,9)

Question 8

how do we assess how drugs interact w receptors ?
1. —- studies by measuring the response of tissue to drugs
2. — studies by directly measuring the binding of radiolabeled drug to tissue

Answer 8

• functional
• binding

Question 9

necessary assumptions:
1. drugs/agonists bind —- and —- to a receptor
2. biding is —- ( ie. at certain concentration no more biding is possible ) and its —-
3. all receptors are — accessible to ligands
4. receptors are either —- or —- to drugs
5. biding doesnt alter —- or —-

Answer 9

• specifically and reversibly
• saturable and reversible
• equally
• free or bound
• receptor or ligand

Question 10

—- refers to the maximal drug binding to receptor
—- half maximal drug binding to receptor
the equation of the dose response curve is called — which is similar to the michealis constant

Answer 10

• maximum bound ( Max)
• dissociation constant ( Kd)
• Langmuir equation which is normally displayed as log dose/response curves

Question 11

—- allows us to measure drug affinity ( kd) and maximal effect ( E max)

Answer 11

Langmuir equation in the dose response curve

Question 12

—- is the measure of drug activity and its expressed in terms of the amount rewired to produce an —- of a given —-

Answer 12

• potency ( which is related to affinity)
• effect
• intensity
  ( check graph slide 14)

Question 13

some agonist never produce max response which is known as —-
full agonist receptors go from —- to —

Answer 13

• partial agonist ( they can be on without experting max response )
• off to on

Question 14

—- ability to produce a response
- partial agonist exhibit intrinsic activity greater than — but less than —

Answer 14

• intrinsic activity which is also known as: efficacy
• 0
• 1
  ( a=1 : full agonist
  a=0 : antagonist )

Question 15

—- a chemical that binds to a receptor but induces reduced signalling response

Answer 15

partial agonist

Question 16

—– important for pain transmission and neurotransmission
—- are agonist for mu opioid receptors
- full agonist include :
- partial agonist include:

Answer 16

• opoid receptors GPCR
• opoid
• codeine , fentanyl , methadone
• buprenorphine , butrophanol , tramadol

Question 17

nicotine replacement therapy is an example of —-

Answer 17

partial agonism

Question 18

-maximum signalling response often observed without —– of the available receptors
- receptors are — whenever the maximum response at — that full agonist binding

Answer 18

-full occupancy
- spare
- less
( aka spare receptors )
check slide 20 , 21 IMPORTANT