Question

If a substance lowers the EC50 for a receptor, what does it mean?

Answer 1

are we talking about \(\sf EC_{50}\) as concentration measurement?

Answer 2

Yes, lol.

Answer 3

first off, what do you know? is this also a biochem pharmacology class?

Answer 4

I took a version of this class, just curious :D

Answer 5

@jthec

Answer 6

have you learned about kinetics of the drugs? anything? hello.....

Answer 7

It does not matter whether he took drug kinetics. The concept can be explicated without that detail.

Answer 8

This graph pretty much should answer your question. If you don't mind, what does this graph infer?

http://a.static.trunity.net/files/113901_114000/113975/300px-Dose-response-fig-6.gif

Answer 9

@nincompoop

The concept philosophical views are different, but the same meaning.

Answer 10

There is a key distinction.

Answer 11

@jthec

Reply back when you're online.

Answer 12

yes, yes - the graph can reveal something, but only to the learned in that subject matter.

Answer 13

Hello! Sorry for the late reply

Answer 14

Oh hi.

so what are you not "understanding"?

Answer 15

It is from an article I'm trying to decipher: "Augmentation of glycine receptor alpha3 currents suggests amechanism for glucose-mediated analgesia" It states, in presence of sugars, EC50 values of glycine were reduced up to 4.5- fold.

Answer 16

Well doesn't that mean that if the receptor is lowered, that the binding of that molecule can also be lowered. In other words the drug can bind greater, does that makes sense?

Answer 17

Yes, sort of, thanks.

Answer 18

haha, I'm not giving up on you yet lol.

Ec50 ---> half maximal effective concentration

Answer 19

look at the graph I posted, Ec50 refers to the halfway mark.

Agreed?

Answer 20

@jthec

Answer 21

@jthec


since you went offline, this reading will answer your question. Also, the graph helps a lot to visualize the concept.

The EC50 of a graded dose response curve therefore represents the concentration of a compound where 50% of its maximal effect is observed.[2] The EC50 of a quantal dose response curve represents the concentration of a compound where 50% of the population exhibit a response,[3] after a specified exposure duration.

It is also related to IC50 which is a measure of a compound's inhibition (50% inhibition). For competition binding assays and functional antagonist assays IC50 is the most common summary measure of the dose-response curve. For agonist/stimulator assays the most common summary measure is the EC50.[4] Sometimes it is also expressed as pEC50 = - LOG(EC50) (with EC50 in M/l).

A small change in ligand concentration typically result in rapid changes in response in the biological system, following a sigmoidal function.The inflection point at which the increase in response with increasing ligand concentration begins to slow is the EC50. Which can be mathematically determined by derivation of the best-fit line. While relying on a graph for estimation is more convenient, this typical method yields less accurate results and less precise.[5]

Answer 22

@alphadxg, don't copy and paste other peoples answers from elsewhere on the web and present it as your own work. Just don't.

Answer 23

@hectoroftroy

I never claimed it was my own work.

Hence, "since you went offline, this reading will answer your question. "

Answer 24

Thanks for the help @alphadxg, just reading this now