2. History of Caffeine
Caffeine as been around in human culture for thousands of years, legend says that a goat herder
found his goats extremely full of energy after eating coffee shrubs. He decided to try it and
spread it with the other monks, legend has it they stayed up that entire night from the large
amounts of caffeine
History says that coffee beans were heavily used in the middle east, only grown in Africa and
Arabia until 1600. The only way to get it was through trade
The first modern European coffee shop opened in 1616
Caffeine was first extracted from coffee in 1820
90% of American adults consume caffeine daily
Caffeine is the most popular addiction in the world, but why?
3. Caffeine Affects on the Body
Pros
Caffeine prevents drowsiness temporarily
Feeling of alertness and clearness of
thought
Increased memory and comprehension
Sense of feeling good through dopamine
receptors
Cons
Caffeine can cause troubled sleeping patterns
Withdrawal symptoms when positive affects wear off
(dependence)
Diuretic that dehydrates the user
Diarrhea caused by acceleration of digestion
Raises blood pressure
4. Chemical Structure and Binding
Caffeine has a very similar chemical structure to that of
adenosine. Adenosine is the drug that builds up as you
are awake and binds to adenosine receptors (A2A) and
tells your brain to go to sleep.
Adenosine binds to create a drowsy affect and starts to
limit neurological function in and effort to make you
sleep.
What caffeine does since the structure is similar is binds to
the adenosine receptor (A2A) and prevents the adenosine
from binding. However, the caffeine does not limit
neurological function since it is an antagonist
5. How caffeine binds
The caffeine binds to the A2A receptor via a very specific
affinity for the non covalent bonds that are at the binding
sites. Primarily hydrogen bonds to the oxygen and
nitrogen in the rings.
The A2A receptor is a type of GCRP (G-protein coupled
receptor protein) which stimulates adenyl-cyclase which
synthesizes cAMP. This would cause secondary messengers
to tell the brain that it is tired. Since caffeine binds there
are no secondary messages
Normally A2A receptor stimulation would also increase
oxygen to the brain to prepare for sleep, since caffeine
binds the oxygen is restricted and sleep is further
stimulated against.
A2A binding site
6. Dependence on Caffeine
Caffeine has some pretty great benefits with few side affects, the most notable side affect would be
dependence. Caffeine is slightly addictive because it stimulates the dopamine pathways in ones
brain to make them want to use the caffeine again.
People become physically dependent on caffeine over time because your brain realizes that it is
being tricked (in way sense). The brain creates more A2A receptors so that it gets does drowsy, by
creating more, it takes more caffeine to block all those extra receptors then the normal human brain.
Once someone addicted to caffeine stops taking caffeine, they are very tired because the adenosine
receptors (A2A) are all over the place in their brains to make them drowsy. Other side affects of
withdrawal besides tiredness include: migraines, depression, and irritability.
7. How Much is Too Much?
The average adult takes in 200mg of caffeine a day. That is two cups of coffee on average. This
would be enough to experience minor withdrawals without caffeine fro a day since as a mild
headaches, tiredness, and experiencing less energy.
This means that around 80-90% of American adults have some kind of addiction to caffeine
Caffeine can be lethal however, taking more then 150mg per kg of body weight would be enough
to die. That’s over 100 cups of coffee in three hours.