Human body●●●●●Difficulty 3 of 5

How does a drug find the right cells in a whole body?

Your cells carry locks, and a drug is a key that happens to fit one of them.

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A drug finds the right cells because those cells carry the right receptors. A receptor is a protein, usually on the surface of a cell, that receives a chemical message and turns it into a response, for example a change in the cell's electrical activity. The molecule that binds to it is called a ligand, and the ligand can be a hormone, a neurotransmitter, a toxin, or a pharmaceutical drug. Each receptor binds only ligands of a particular shape, which people compare to locks that accept only specifically shaped keys.

This is how a drug can act on some cells and not others: the body already uses the lock. The drug is a key that happens to fit, or a copy of one. The nicotinic acetylcholine receptor is a good example: the body's own key is acetylcholine, nicotine can also turn it, and curare can block it.

Fitting is only half of the story. Scientists separate how tightly a ligand binds, called affinity, from how well it switches the receptor on once bound, called efficacy. Some ligands bind and activate, and are called agonists. Others bind and do nothing, and by occupying the lock they stop other keys from working. Those are antagonists.

Same lock, different keys

Agonist

  • Binds the receptor
  • Switches it on
  • Imitates the body's own message

Antagonist

  • Binds the receptor
  • Does not switch it on
  • Blocks other keys from working

So a medicine can work in two opposite ways: by imitating a message, or by blocking one. In both cases the shape of the molecule decides what it can do, and that is why chemists spend so much effort adjusting shapes.

Quiz me

0/3

  1. 1.What separates an agonist from an antagonist?
  2. 2.Why does a partial agonist give a weaker response than a full agonist even when it occupies every receptor?
  3. 3.Why were rimonabant and taranabant withdrawn?

Recap

A drug binds a receptor, and whether it switches it on or blocks it depends on its efficacy.

💡 A trick to remember it · A drug is a key that either turns the lock or just jams it.

Surprising fact · Some drugs trigger a full response while occupying under 1% of the receptors.

Sources (1)

No source, no claim. Every fact in this lesson (14 claims) cites at least one of these.

  1. [1]Receptor (biochemistry) · Wikipedia
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