Endorphins

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For other uses, see Endorphins (disambiguation).

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Endorphins (contracted from "endogenous morphine"[note 1]) are endogenous opioid neuropeptides
and peptide hormones in humans and other animals. They are produced by the central nervous system
and the pituitary gland. The term "endorphins" implies a pharmacological activity (analogous to the
activity of the corticosteroid category of biochemicals) as opposed to a specific chemical formulation.
It consists of two parts: endo- and -orphin; these are short forms of the words endogenous and
morphine, intended to mean "a morphine-like substance originating from within the body".[3] The
class of endorphins includes three compounds—α-endorphin (alpha endorphins), β-endorphin (beta
endorphins), and γ-endorphin (gamma endorphins)—which preferentially bind to μ-opioid receptors.
[4]
The principal function of endorphins is to inhibit the communication of pain signals; they may also
produce a feeling of euphoria very similar to that produced by other opioids.[5]

Contents
• 1History
• 2Synthesis
• 3Types
• 4Mechanism of action
• 5Properties
• 6Etymology
• 7Notes
• 8References
• 9External links

History[edit]
Opioid neuropeptides were first discovered in 1974 by two independent groups of investigators:

• John Hughes and Hans Kosterlitz of Scotland isolated – from the brain of a pig – what some
called "enkephalins" (from the Greek εγκέφαλος, cerebrum).[6][7]
• Around the same time, in a calf brain, Rabi Simantov and Solomon H. Snyder of the United
States found[8] what Eric Simon (who independently discovered opioid receptors in vertebral
brains) later termed "endorphin" by an abbreviation of "endogenous morphine", meaning
"morphine produced naturally in the body".[3] Studies have demonstrated that human and
 diverse animal tissues are capable of producing morphine, which is not a peptide.[9][10] They
have been continually researched for their pain relieving properties and role in the feeling of
pleasure.

Synthesis[edit]
The three types of endorphins that exist are made through the fragmentation of precursor proteins.
The original protein is called proopiomelanocortin (POMC). This protein is fragmented into many
different smaller proteins including beta-lipotropin (β-LPH). β-LPH, a pituitary hormone with little
opiate activity, is then continually fragmented into different peptides giving rise to α-Endorphin,
β-Endorphin, γ-Endorphin and many other peptides.[11][12][13]

Types[edit]
This section needs expansion. You can help by adding to it. (December 2018)

The class of endorphins includes three endogenous opioid peptides:[4]

• α-Endorphin – The smallest fragment in the family and is composed of 16 amino acids. They
are the same as the first 16 amino acids as the β-endorphin. The sequenced protein has been
shown to be: Tyr-Gly-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-OH.[14][15]
[11]

• β-Endorphin – The longest fragment in the family and is composed of 31 amino acids. The
sequence has been shown to be: Tyr-Gly-Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-
Val-Thr-Leu-Phe-Lys-Asn-Ala-Ile-Ile-Lys-Asn-Ala-Tyr-Lys-Lys-Gly-Glu. .[14][15][11]
• γ-Endorphin – The second longest fragment and is composed of 17 amino acids. It also matches
the first 17 amino Acids of β-endorphin.[14][15][11] The sequence has been shown to be: Tyr-Gly-
Gly-Phe-Met-Thr-Ser-Glu-Lys-Ser-Gln-Thr-Pro-Leu-Val-Thr-Leu-OH.

Mechanism of action[edit]
Endorphins are naturally produced in response to pain. This phenomenon happens in both the Central
Nervous System (CNS) and the Peripheral Nervous System (PNS). In the PNS, endorphins, primarily
β-endorphin, are released from the pituitary gland and bind to μ-receptors. The binding of these two
components inhibits the pain signal of the periphery nerves by blocking the neurotransmitter
substance P. The mechanism in the CNS is similar but works by blocking a different neurotransmitter.
When the endorphin binds to the μ-receptor, it inhibits the release of the neurotransmitter gamma-
aminobutyric acid (GABA) which, in turn, increases the production and release of dopamine, the
neurotransmitter associated with pleasure.[15][16]

Their production can also be triggered by various human activities. Vigorous aerobic exercise can
stimulate the release of β-endorphin which contributes to a phenomenon known as a "runner's
high."[17][18]

Laughter may also stimulate endorphin production; a 2011 study showed that attendees at a comedy
club showed increased resistance to pain.[19] Endorphins are also released during various activities
including eating food, sex, orgasm, listening to music and eating chocolate. Research has also
demonstrated meditation by trained individuals to trigger endorphin release. [15][20]

Properties[edit]
Endorphins play a major role in the body's response to inhibiting pain but endorphins have also been
looked at for their role in pleasure. There has been a lot of research in the euphoric state that is
produced after the release of endorphins in cases such as runner's high, orgasms, and eating appetizing
food.[15][20] Endorphins have also been looked into as a way to aid in the treatment of anxiety and
depression through exercising.[21]

On the other hand, endorphins may also be involved in exercise addiction. The release of endorphins a
person gets while exercising will produce a feeling of euphoria. With consistent exercise, the brain
may down-regulate the production of endorphins in periods of rest and a person will need to continue
to exercise more intensely in order to receive the same feeling.[22]

Etymology[edit]
From the words ἔνδον / Greek: éndon meaning "within" (endogenous, ἐνδογενής / Greek: endogenes,
"proceeding from within") and morphine, from Morpheus (Ancient Greek: Μορφεύς,
romanized: Morpheús), the god of dreams in the Greek mythology, thus 'endo(genous) (mo)rphin’
(morphin being the old spelling of morphine).

Notes[edit]
1. ^ In addition to endorphins, chemically authentic morphine is also produced endogenously in
humans and other animals.[1][2]

References[edit]

1. ^ Stefano GB, Ptáček R, Kuželová H, Kream RM (1515). "Endogenous morphine: up-to-date

review 2011" (PDF). Folia Biologica. 58 (2): 49–56. PMID 22578954. "Positive evolutionary
pressure has apparently preserved the ability to synthesize chemically authentic morphine,
albeit in homeopathic concentrations, throughout animal phyla. ... The apparently serendipitous
finding of an opiate alkaloid-sensitive, opioid peptide-insensitive, µ3 opiate receptor subtype
expressed by invertebrate immunocytes, human blood monocytes, macrophage cell lines, and
human blood granulocytes provided compelling validating evidence for an autonomous role of
endogenous morphine as a biologically important cellular signalling molecule (Stefano et al.,
1993; Cruciani et al., 1994; Stefano and Scharrer, 1994; Makman et al., 1995). ... Human white
blood cells have the ability to make and release morphine"
2. ^ "μ receptor". IUPHAR/BPS Guide to PHARMACOLOGY. International Union of Basic and
Clinical Pharmacology. 15 March 2017. Retrieved 28 December 2017. "Comments:
β-Endorphin is the highest potency endogenous ligand ... Morphine occurs endogenously
[117]."
 3. ^ a b Goldstein A, Lowery PJ (September 1975). "Effect of the opiate antagonist naloxone on
body temperature in rats". Life Sciences. 17 (6): 927–31. doi:10.1016/0024-3205(75)90445-2.
PMID 1195988.
4. ^ a b Li Y, Lefever MR, Muthu D, Bidlack JM, Bilsky EJ, Polt R (February 2012). "Opioid
glycopeptide analgesics derived from endogenous enkephalins and endorphins". Future
Medicinal Chemistry. 4 (2): 205–26. doi:10.4155/fmc.11.195. PMC 3306179. PMID 22300099.
"Table 1: Endogenous opioid peptides"
5. ^ "Is there a link between exercise and happiness?". 22 June 2009. Retrieved 18 September
2014.
6. ^ "Role of endorphins discovered". PBS Online: A Science Odyssey: People and Discoveries.
Public Broadcasting System. 1 January 1998. Retrieved 15 October 2008.
7. ^ Hughes J, Smith TW, Kosterlitz HW, Fothergill LA, Morgan BA, Morris HR (December
1975). "Identification of two related pentapeptides from the brain with potent opiate agonist
activity". Nature. 258 (5536): 577–80. Bibcode:1975Natur.258..577H. doi:10.1038/258577a0.
PMID 1207728.
8. ^ Simantov R, Snyder SH (July 1976). "Morphine-like peptides in mammalian brain: isolation,
structure elucidation, and interactions with the opiate receptor". Proceedings of the National
Academy of Sciences of the United States of America. 73 (7): 2515–9.
Bibcode:1976PNAS...73.2515S. doi:10.1073/pnas.73.7.2515. PMC 430630. PMID 1065904.
9. ^ Poeaknapo C, Schmidt J, Brandsch M, Dräger B, Zenk MH (September 2004). "Endogenous
formation of morphine in human cells". Proceedings of the National Academy of Sciences of the
United States of America. 101 (39): 14091–6. Bibcode:2004PNAS..10114091P.
doi:10.1073/pnas.0405430101. PMC 521124. PMID 15383669.
10. ^ Kream RM, Stefano GB (October 2006). "De novo biosynthesis of morphine in animal cells:
an evidence-based model". Medical Science Monitor. 12 (10): RA207–19. PMID 17006413.
11. ^ a b c d Ambinder RF, Schuster MM (November 1979). "Endorphins: new gut peptides with a
familiar face". Gastroenterology. 77 (5): 1132–40. PMID 226450.
12. ^ Crine P, Gianoulakis C, Seidah NG, Gossard F, Pezalla PD, Lis M, Chrétien M (October
1978). "Biosynthesis of beta-endorphin from beta-lipotropin and a larger molecular weight
precursor in rat pars intermedia". Proceedings of the National Academy of Sciences of the
United States of America. 75 (10): 4719–23. doi:10.1073/pnas.75.10.4719. PMC 336191.
PMID 216997.
13. ^ Goldstein A (September 1976). "Opioid peptides endorphins in pituitary and brain". Science.
193 (4258): 1081–6. Bibcode:1976Sci...193.1081G. doi:10.1126/science.959823.
PMID 959823.
14. ^ a b c Ling N, Burgus R, Guillemin R (November 1976). "Isolation, primary structure, and
synthesis of alpha-endorphin and gamma-endorphin, two peptides of hypothalamic-hypophysial
origin with morphinomimetic activity". Proceedings of the National Academy of Sciences of the
United States of America. 73 (11): 3942–6. doi:10.1073/pnas.73.11.3942. PMC 431275.
PMID 1069261.
15. ^ a b c d e f Chaudhry SR, Bhimji SS (2018). Biochemistry, Endorphin. StatPearls. StatPearls
Publishing. PMID 29262177. Retrieved 20 February 2019.
16. ^ Sprouse-Blum AS, Smith G, Sugai D, Parsa FD (March 2010). "Understanding endorphins
and their importance in pain management". Hawaii Medical Journal. 69 (3): 70–1.
PMC 3104618. PMID 20397507.
17. ^ Boecker H, Sprenger T, Spilker ME, Henriksen G, Koppenhoefer M, Wagner KJ, Valet M,
Berthele A, Tolle TR (November 2008). "The runner's high: opioidergic mechanisms in the
 human brain" (PDF). Cerebral Cortex. 18 (11): 2523–31. doi:10.1093/cercor/bhn013.
PMID 18296435.[permanent dead link]
18. ^ Kolata G (27 March 2008). "Yes, Running Can Make You High". The New York Times.
ISSN 0362-4331. Retrieved 26 May 2016.
19. ^ Dunbar RI, Baron R, Frangou A, Pearce E, van Leeuwen EJ, Stow J, Partridge G, MacDonald
I, Barra V, van Vugt M (March 2012). "Social laughter is correlated with an elevated pain
threshold". Proceedings. Biological Sciences. 279 (1731): 1161–7. doi:10.1098/rspb.2011.1373.
PMC 3267132. PMID 21920973.
20. ^ a b Dfarhud D, Malmir M, Khanahmadi M (November 2014). "Happiness & Health: The
Biological Factors- Systematic Review Article". Iranian Journal of Public Health. 43 (11):
1468–77. PMC 4449495. PMID 26060713.
21. ^ Anderson E, Shivakumar G (23 April 2013). "Effects of exercise and physical activity on
anxiety". Frontiers in Psychiatry. 4: 27. doi:10.3389/fpsyt.2013.00027. PMC 3632802.
PMID 23630504.
22. ^ Freimuth M, Moniz S, Kim SR (October 2011). "Clarifying exercise addiction: differential
diagnosis, co-occurring disorders, and phases of addiction". International Journal of
Environmental Research and Public Health. 8 (10): 4069–81. doi:10.3390/ijerph8104069.
PMC 3210598. PMID 22073029.

External links[edit]
• Endorphins at the US National Library of Medicine Medical Subject Headings (MeSH)
• Wine Benefits for health Increase our endorphins

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Opioid receptor modulators

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