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Jumpy Endorphinaut

Endorphinaut or not?

Opioid neuropeptides were first discovered in 1975 by two independent groups of


investigators.
• John Hughes and Hans Kosterlitz of Scotland isolated — from the brain of a pig
— what they called enkephalins (from the Greek εγκέφαλος, cerebrum).
• Around the same time in the calf brain, Rabi Simantov and Solomon H. Snyder of
the United States found what Eric Simon (who independently discovered opioid receptors
in the brain) later termed "endorphin" by an abbreviation of "endogenous morphine",
which literally means "morphine produced naturally in the body". Importantly, recent
studies have demonstrated that diverse animal and human tissues are in fact capable of
producing morphine itself, which is not a peptide.

Endorphins
The Gift You Give Yourself
By Lorrie Klosterman | Illustration by Annie Dwyer Internicola
"If we could sniff or swallow something that would, for five or six hours each day,
abolish our solitude as individuals, atone us with our fellows in a glowing exaltation of
affection and make life in all its aspects seem not only worth living, but divinely beautiful
and significant...then, it seems to me, all our problems (and not merely the one small
problem of discovering a novel pleasure) would be wholly solved and earth would
become a paradise."
—Aldous Huxley, from "Wanted, a New Pleasure," 1931
As the days shorten and the sun skims a lower arc across the sky, those of us who long for
brilliant overhead sunlight get a little uneasy about the prospects of a long dark winter
ahead. People with SAD (seasonal affective disorder) dust off their full-spectrum lamps
to augment those specific solar wavelengths that cue the brain to keep pumping out
serotonin—one of the brain's "feel good" neurotransmitters. But there are other
neurochemicals, dancing in a complex relationship within the brain, that enhance a sense
of well-being. Among them are endorphins.

The word endorphin is short for "endogenous morphine," referring to self-made


chemicals (endogenous) that have morphine-like effects. In fact, the discovery of
endorphins directly emerged from studies of morphine's influence on the brain. In 1973,
Candace Pert and Sol Snyder published findings that morphine avidly attaches to specific
proteins (receptors) on brain cells, thereby influencing the brain's activity, especially in
regions allied with mood and pain. Those proteins were dubbed opioid receptors because
they bind opiates—morphine and related chemicals from the opium-poppy flower bud
(codeine, heroin, oxycodone).

Researchers then reasoned that opiate receptors ought to have naturally occurring
neurochemicals that attached to them and induced morphine-like responses. The hunt
began, and eventually enkephalins, endorphins, beta-lipoprotein, and other endogenous
opioids were detected in brain tissue—in extremely minute amounts, but exquisitely
powerful. Beta-endorphin is one of the best studied in the endogenous opioid family. It is
a peptide, meaning a short chain of amino acids (30 of them), which is especially
prevalent in the brain but also shows up in the nervous system outside the body and in
immune cells.

Other similar but shorter molecules, like enkephalins and endomorphins, are potent
neurotransmitters as well, and their diverse actions are being elucidated. Together, the
endogenous opioid family of today includes dozens of chemicals that modulate mood,
block perception of pain, influence hunger, regulate reproduction, and perform many
other functions.

Seeking: Endorphins
Endorphins are in the public vernacular in phrases like "That ski run really gave me an
endorphin rush!" or "He/she is so hot my endorphins spiked the moment he/she came in
the room!" It should be noted that many of the things claimed to flood us with endorphins
are not well supported by studies in people. The vast majority of scientific data (and
conclusions) about endorphins are from rats and mice, because studying what's
happening in the brain usually means killing the study subjects. Studies of people
typically measure bloodstream levels of endorphins, not brain levels, with the assumption
that there is a biologically relevant relationship between the two (though endorphins do
not easily travel between brain and blood). Other studies use the drug naloxone to block
opiod action and see what's been altered in human volunteers. This method is a useful, if
not direct, way of probing what endogenous opioids do in people. In addition, PET scans
are now showing activation of the brain's endogenous opioid system more directly, such
as while receiving painful stimuli or exercising.

Hurts So Good
One of the best-supported activators of endorphins is pain. Like morphine, endorphins are
analgesic, replacing pain with a relaxed, calm, and sometimes "euphoric" feeling. They
dampen the perception of pain signals that reach the brain, and may also tame the
frequency of signals sent to the brain by injured tissues. Note that things not inherently
delightful to some people but which trigger a tolerable level of physical pain, may be
sought by others who experience a euphoric response. Presumably endorphins (or other
opioids) encourage such pain-seeking activities, but the body's other stress-induced
neurochemicals, like norepinephrine (adrenalin), may be involved.

But endorphins are released within the brain by more than overt injury. Vigorous
exercise, childbirth, bodywork, and acupuncture also tweak brain endorphins. For some,
like childbirth, the physical stress is obvious. But even something as simple as eating hot
chili peppers has been shown (in rats, by direct application of a chemical extracted from
peppers to nerve cells) to trigger brain endorphins, and is assumed to do the same for
chili-pepper lovers who crave the afterglow.

Exercise
Vigorous exercise is a stressor on the body. Endorphins are clearly released under certain
conditions to produce that famous "runner's high," a biochemically measurable
phenomenon to which athletes attest.

"It feels so peaceful," says Dorothy Hamburg, an exercise physiologist and certified
exercise trainer who owns Personal Strength and Training in Rhinebeck. "The runner's
high, being in the zone, is real. I've been in races where I find myself struggling, then all
of a sudden it just becomes easy, fun. Instead of 'oh, no, I've got to run another hour,' it
becomes effortless. There is no struggle."

Hamburg, who has enjoyed endurance athletics and marathons for years, explains that
endorphins are released when exercise level is moderate to high, "at the point when you
are going from aerobic to anaerobic exercise." A clue as to when that's happening is
"when you wouldn't be able to have a comfortable conversation while exercising." Short
bursts of activity like weight-lifting or sprinting, don't trigger endorphins enough to be
measured in the bloodstream, but might boost brain levels, and they help condition the
body for more exertional activities. Also, studies do show that an hour or more of even
modest exercise can elevate endorphins.

Most of Hamburg's personal training clients are women wanting to get exercise back into
their lives as their bodies change in middle life. The endorphins are not a goal, but a perk,
and the exercise can be just plain enjoyable for many reasons. "The most important thing
is to find what you like doing. If you don't like it, you won't do it." It could include a
combination of things, like gardening, walking, and yoga, for a total of half an hour a
day. "Start with gentle effort. Learn the movement patterns, see how you feel, then
increase in duration, intensity, and frequency."

Hamburg also suggests a one-on-one consultation with a trainer or coach. "Look for
someone with education in the health fitness industry, a sports medicine background, or
who is certified by the National Strength Conditioning Association [NSCA], American
Council of Exercise [ACE], or the American College of Sports Medicine [ACSM]."

There are many other beneficial physiological changes induced by exercise, such as
deeper breathing, revved-up blood circulation, better lymphatic drainage, and increased
cellular metabolism, each of which have complex interrelations with brain chemistry and
influence mood, alertness, physical sensations, and overall health.

Bodywork And Acupuncture


Physical treatments that stimulate nerves directly or indirectly (through muscle
manipulation) also release endorphins, says Dr. David Ness, certified sports chiropractor
in New Paltz. "Very simply, whether it's acupuncture, chiropractic, or bodywork, in
addition to the therapeutic value, you get both the emotional and endorphin effects."

Chiropractic releases endorphins through its impact on the nervous system, he explains,
adding that all bodywork releases endorphins. "Yoga, Pilates, Tai Chi, Qi Gong, any of
those modalities improve overall health—physical, spiritual, and mental. They are part of
the wellness revolution," meaning the shift away from medicalized treatment of ailments
to maintaining wellness and taking responsibility for one's own health and well-being.
That once-a-week class isn't going to be much help, though. "If you are going to use it for
an exercise, it needs to be done more than once a week," Ness encourages.

Bruce Pomeranz, PhD, at the University of Toronto, was the first to propose that
acupuncture, commonly undertaken to relieve pain, does so through endorphins. After
attending a 1975 conference at which the discovery of endorphins was announced, he
theorized that acupuncture needles inserted at key locations in the body (which
correspond to points on the meridian) stimulate nerves that trigger endorphin release
within the brain (d'ai chi, meaning twisting the needles, is key to the effect, he says).
There, the endorphins block the brain from registering the sensation of pain.

He then spent 20 years collecting data to disprove that (as proper science is meant to
proceed). But diverse studies of his and other researchers indeed support this
"westernized" medical explanation of why acupuncture is analgesic (versus that of
traditional Chinese medicine, which explains it in terms of chi energy flowing through
meridians). Bottom line: Acupuncture works and endorphins help make it happen.

Mind Over Body


Endorphins may also be behind the placebo effect, which is a measurable improvement in
a person's condition, like pain, without any specific treatment being given. The placebo
effect often is explained as the power of the mind to create physiological changes in the
body, but some researchers argue that a placebo effect can be explained by study design
instead; an example is the likelihood that, in any study of illness or a health condition,
some people would be getting better on their own anyway.

But researchers at the University of Michigan implicated endorphins as a player in the


placebo effect in a study earlier this year. They used PET brain scans of volunteers to
record changes in activity of the brain's opioid system while the volunteers received a
painful injection. The scans showed markedly increased activity of the endorphin/opioid
system after the volunteers were told they were being given something that might ease
the pain (though they weren't). The volunteers reported feeling less pain as well. This
suggests that the idea of relief triggered the brain's natural pain-reliever (endorphins),
which lowered the sensation of pain. "The mind-body connection is quite clear," the
study's authors concluded.

Weak Evidence, But Who Cares?


Does having sex increase endorphins? The belief that it does is much more prevalent than
any real data. A search of the Library of Medicine's database of thousands of biomedical
journals produced a glaring paucity of studies relating endorphins and sexual activity in
people (the more abundant data for rats offers mixed conclusions). There is reasonable
evidence implicating the endogenous opiod system somehow in sexual behavior,
however, and in reproduction, but in complex ways that include the two neurochemicals
more reliably linked to sexual behavior: dopamine and serotonin. Similarly, there is
almost no data to support the notion that laughter's emotional high is mediated through
endorphins.

But who cares what's behind the warm and fuzzy aftermath of sex or out-of-control belly
laughs? Something's definitely going on in that cranium. Plus, both have whole-body
health benefits as cardiovascular exercises that increase blood and oxygen delivery and
give muscles a workout, including those that other forms of exercise don't seem to get to.

The preceding brief review of endorphins suggests there surely is much more to them
than we currently know. An annual review of endogenous opioids, published in the
scientific journal Peptides in 2004, included sections on their relation to pain, stress,
learning and memory, eating and drinking, drug abuse, sexual activity, development,
mental illness, mood, neurological disorders, digestion, kidney and liver function, the
cardiovascular system, respiration, thermoregulation, immunity, and more (though, again,
most information is from studies in lab animals).

Just Do It
Mark Wilson of Woodstock is founder and president of the Hudson Valley Triathlon Club
and a triathlon coach. "It doesn't take much to enjoy the benefits of endorphins via
exercise," he says. "Literally 10 to 20 minutes of activity can release the natural drugs
into your system, which creates a sense of well-being and joy that cannot be felt by
sedentary folks. Brief, quick efforts up stairways or down the block can trigger the
release of endorphins and possibly keep you from buying that cup of joe on the way to
work, not to mention the doughnut! Bottom line, keep moving your body; it likes that!"

Are there any endorphin downsides? Some things that trigger them might become
harmful, like overindulgence in highly sweet or fatty foods or a body-wracking exercise
schedule, and they are implicated in addictive and obsessive behaviors like eating
disorders and alcoholism. For example, alcohol triggers endorphin release; drugs that
block endorphin attachment to receptors can decrease cravings. Interestingly, there appear
to be inherited differences in brain endorphin levels, which are associated with
susceptibility to alcoholism (naturally higher levels induce alcohol cravings).

Still, some of the best things in life are endorphin-friendly (or suspected of being so) and
generate many health and social benefits. Even if scientific studies don't prove everything
yet, how these activities make us feel is a good bottom line. No one really can tell what's
going on inside our heads as well as we can. Plus, as a drug of choice, endorphins are
very safe, and you'll never run out.

'Sexercise' yourself into shape

Forget about jogging round the block, the NHS says


The NHS has some new advice for people struggling to schedule a fitness routine into
their daily lives - a workout between the sheets.

According to the NHS Direct website, "sexercise" can lower the risk of heart attacks and
helps people live longer.

Endorphins released during orgasm stimulate immune system cells, which also helps
target illnesses like cancer, as well as wrinkles, it states.

Sexual health experts said such claims could not be scientifically proven.

"It's good to see the NHS are promoting sexual wellbeing," Dr Melissa Sayer told the
Guardian newspaper.

"Yes, there is evidence that sex has benefits for mental wellbeing, but to say there is a
link with reduced risk of heart disease and cancer is taking the argument too far."

NHS Direct, however, told the paper the content was "backed by science and clinical
evidence" and "isn't just a bit of fun".

'Regular romps'

The advice, published under the headline "Get more than zeds in bed", is one of several
sexual health-related articles to be found on the NHS Direct website.

Sex with a little energy and imagination provides a workout worthy of an athlete, the
article says.

If you're worried about wrinkles - orgasms even help prevent frown lines from
deepening

NHS Direct

"Forget about jogging round the block or struggling with sit-ups.

"Sex uses every muscle group, gets the heart and lungs working hard, and burns about
300 calories an hour."

The advice suggests "regular romps this winter" could lead to a better body and a younger
look.

Increased production of endorphins "will make your hair shine and your skin smooth," it
adds.

"If you're worried about wrinkles - orgasms even help prevent frown lines from
deepening."
The article goes on to say that orgasms release "painkillers" into the bloodstream, which
helping keep mild illnesses like colds and aches and pains at bay.

The production of extra oestrogen and testosterone hormones "will keep your bones and
muscles healthy, leaving you feeling fabulous inside and out"

Role of endorphins discovered


1975

In the 1960s, nuerochemist Choh Hao Li at the University of California in San Francisco
was investigating the pituitary gland for substances that aided in the metabolism of fat. It
was hard to get enough of this substance, though, so he acquired about 500 dried camel
pituitaries. But the camels had none of this fat-metaboliser. Li isolated another amino
acid substance from the camel pituitary, beta-endorphin, but it didn't play into the
questions he was asking and he put it in storage.

In 1973, research teams in Sweden, Baltimore, and New York independently found that
the brain has special receptors that interact with opiates such as morphine. Strong opiates
tended to bind better to these sites than weak ones. This seemed odd. Why would human
brains around the world have a receptor for morphine, the product of flowers that
originated in the Middle East?

In 1975, John Hughes and Hans Kosterlitz published their discovery of a small amino-
acid molecule in the brains of pigs. They called this molecule "enkephalin"(meaning "in
the head"). It had some of the qualities of morphine, which helped answer the question of
why the brain had receptors for morphine. Hughes thought they might be able to use
enkephalin in painkillers that were not as addictive as morphine. They tried this idea out
in the lab and were disheartened to find that the reverse was true: The painkilling power
was weak, but it was extremely addictive.

Back in San Francisco, Li realized that the beta-endorphin he had isolated contained
enkephalin. Now he had a question to ask about it: Did it have something to do with pain
perception? When Li injected the substance into the brain, he found it was 48 times more
powerful than morphine; injected in the vein it was 3 times as powerful. And also
addictive.

This research allowed neuroscientists to conclude that the brain has receptors for
painkillers which the pituitary releases under great stress. If an artificial painkiller such as
morphine is given, it occupies more of the pain receptors in the brain; however, less
natural painkiller is released. Then, when the artificial source is taken away, there are
more empty pain receptors, causing the craving for narcotics and a withdrawal response.

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