@ meryem or sarim or anyone ----nbme 11 bl 2 qs 20 - docsmily

[ArchivalUser]

Ans is not partial agonist /E for sure because got it wrong in expanded form online.

Can you please explain the best choice ..Thanks

[ArchivalUser]

can u please post the Q.

[ArchivalUser]

Dont know how to copy paste graph here ...If anyone knows please help..Thanks

[ArchivalUser]

Sarim
hi,
You have it just check it out .

[ArchivalUser]

yah can some body tell me how to paste and copy to the forum

[ArchivalUser]

Maryam Can you please post the qs for discussion.Thanks a lot.

[ArchivalUser]

sorry for the late, was at work.
and thank u maryam for sending me the Q


Here is explanation:

D-Noncompetitive Antagonist

This is the case on the concept of "Spare Receptors"

Assume ...100% receptor occupancy required by an Agonist to exert Maximum Effect (Emax) /Optimal effect.

and now consider, if Emax is achieved with result

*Efficacy of Drug X decreases
*5 of the spare receptors are still Unoccupied

Now if we raise the drug "X" dosage.....it will bind to the remaining unoccupied spare receptors and brings it Efficacy back to to the Emax.

there for "No Change in Efficacy" , only "Potency decreases"(as needed higher dose of Drug X)


---------------------------------Graph on the Right--------------------------

But at "High Dose" of of NCA (Drug Y), it will bind to e.g all the 10 spare receptors---->result

*Efficacy(Emax) of Drug X decreases
*there are non of the spare receptors left unoccupied

since there are no extra receptors left, even if we raise the Drug "X" dosage, it won't be able to increase it's Efficacy back to Emax.


Thanks.

[ArchivalUser]

Thank you for the nice explanation

[ArchivalUser]

Complete explanation did not go thru t night

Here is again.



D-Noncompetitive Antagonist

This is the case on the concept of "Spare Receptors"

Assume ...100% receptor occupancy required by an Agonist to exert Maximum Effect (Emax) /Optimal effect.

and now consider, if Emax is achieved with less than 100% receptor occupancy ...means fewer receptors needed to get the Emax.....the remaining
unoccupied receptors are called "Spare Receptors"

How this play role with Noncompetitive Antagonist ?

e.g.
There are
Total # of receptors =20

-------------------------------"First Graph on the Left"------------------------------:

# of receptors Drug "X" occupy to get the Max. effect = 10 receptors
# of receptors left unoccupied(Spare Receptors)........ = 10 receptors



-----------------------------------Middle Graph--------------------------------

Now we add a "Noncompetitive Antagonist"(NCA)...Drug "Y"

At "Low Dose" this NCA (Drug Y) will bind to the e.g 5 spare receptors-----> result

*Efficacy of Drug X decreases
*5 of the spare receptors are still Unoccupied

Now if we raise the drug "X" dosage.....it will bind to the remaining unoccupied spare receptors and brings it Efficacy back to to the Emax.

there for "No Change in Efficacy" , only "Potency decreases"(as needed higher dose of Drug X)


---------------------------------Graph on the Right--------------------------

But at "High Dose" of of NCA (Drug Y), it will bind to e.g all the 10 spare receptors---->result

*Efficacy(Emax) of Drug X decreases
*there are non of the spare receptors left unoccupied

since there are no extra receptors left, even if we raise the Drug "X" dosage, it won't be able to increase it's Efficacy back to Emax.

[ArchivalUser]

I appreciate your effort