How do recepter-antagonist drugs work?

Question

Wouldn't the drug have to bind to the receptor? And if it did bind, wouldn't that actually activate (act as an agonist, in other words) it instead of acting as an antagonist?

Answer 1

It is not the binding alone that activates a receptor. The binding of a molecule to a receptor causes it to change conformation, and the receptor is only activated if it changes into the appropriate conformation.



Also, there are non-competitive receptor antagonists, which do not bind to the receptor at all, but usually bind to the signal, keeping it from binding to the receptor.

Answer 2

antagonist when bind to the receptors they brings up change in the conformation of the receptor and acts as a 1 degree messenger this initiates the 2 degree messenger molecule which in turn follows a specific pathway(signal transduction ) inside the cell . and this can bring upon metabollic or physiological changes in the cell, it may also result in the protein synthesis , secreation or stoping of any previous biological activity of cell.

Answer 3

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