Caffeine: the world’s favorite molecule

ByHeather

Caffeine (1,3,7-trimethylxanthine) is a naturally occurring central nervous system stimulant belonging to the methylxanthine class.  Methylxanthine is a group of chemical compounds containing one or more methyl (CH3) groups on a xanthine molecule or a purine base.

It is naturally occurring in approximately 60 plants including coffee beans, many types of tea, and cacao beans.  It can also be an additive in foods and liquids. 
First isolated in 1819 by Fredlieb Ferdinand Runge, it is considered the most utilized psychoactive stimulant worldwide.

The FDA has approved the use of caffeine for the treatment of apnea of prematurity.  Apnea of prematurity is a condition where a preterm infant stops breathing either for a prolonged time or in conjunction with slow heartbeat or signs of cyanosis.  Off-label uses include the treatment of migraines.  There are on-going studies of the use of caffeine in the treatment of depression and diseases with neurocognitive decline such as Alzheimer’s and Parkinson.

How does it work?

Caffeine is both fat and water soluble and easily crosses the blood-brain barrier.  It is an adenosine receptor antagonist that can bind to all 4 adenosine receptor subtypes, blocking the binding of adenosine.  Antagonism of the A2a receptor is primarily responsible for the effects of mental stimulation.  Around the body, interaction with the A1 receptor in cardiac muscles can affect both the speed and strength of contractions.  Additionally, caffeine can increase renal blood flow, glomerular filtration, and sodium excretion as well as gastric acid secretion and gastrointestinal motility.  This is why you usually have to use the restroom after you drink your coffee.

Caffeine through history

https://drinkgetroastedcoffee.com/blogs/get-roasted-coffee-blog/a-history-of-coffee-in-a-nutshell

The first historical record of caffeine usage is coffee consumption in Ethiopia in the 6th century, although legend has it that in the 3rd century AD, a shepherd noticed his goats becoming very frisky and agitated after eating coffee berries (beans).  According to the legend, the shepherd took the beans to a nearby monastery where the monks discovered that taking the beans and brewing them in hot water helped them stay awake during evening prayers.  From there, coffee makes its way across northern Africa and the Middle East where it becomes very popular. By 1000 AD, coffee became a popular social ritual among Muslims.   Around this time, there are recorded uses of tea during Tang Dynasty of China (618-907 AD) where it is believed to prolong life.  In the Americas, the Olmecs of Mexico made a caffeinated drink from cacao potentially as early as 1200 BC.  From there, the drink was passed onto the Izapa and the Mayans. 

It is difficult to know how the Europeans were introduced to caffeine, but it was likely due to colonization either in the Middle East, the Americas, or the Far East.  By the 17th century, caffeine was widely consumed in Europe, typically in the form of either coffee or tea.  Caffeine was made famous in America with the Boston Tea Party in 1773.  By the 18th century, coffee and tea plantations were established across southeast Asia, Africa, and the West Indies.  In 1890, the first patent for soluble or instant coffee was filed by David Strang in New Zealand, although earlier versions were available in Great Britain at the end of the 16th century and in North America during the Civil War.   In 1901, Japanese chemist Satori Kato developed a more stable version or instant coffee, and George Constant Louis Washing developed a commercial process for the mass production of instant coffee.    Instant coffee increased its popularity during and after World War I.  Today, caffeine is consumed worldwide.

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