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Opioid peptides or opiate peptides are
peptide Peptides are short chains of amino acids linked by peptide bonds. A polypeptide is a longer, continuous, unbranched peptide chain. Polypeptides that have a molecular mass of 10,000 Da or more are called proteins. Chains of fewer than twenty am ...
s that bind to
opioid receptor Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostati ...
s in the brain;
opiate An opiate is an alkaloid substance derived from opium (or poppy straw). It differs from the similar term ''opioid'' in that the latter is used to designate all substances, both natural and synthetic, that bind to opioid receptors in the brain ( ...
s and
opioid Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ...
s mimic the effect of these peptides. Such peptides may be produced by the body itself, for example
endorphins Endorphins (contracted from endogenous morphine) are peptides produced in the brain that block the perception of pain and increase feelings of wellbeing. They are produced and stored in the pituitary gland of the brain. Endorphins are endogeno ...
. The effects of these peptides vary, but they all resemble those of opiates. Brain opioid peptide systems are known to play an important role in
motivation Motivation is an mental state, internal state that propels individuals to engage in goal-directed behavior. It is often understood as a force that explains why people or animals initiate, continue, or terminate a certain behavior at a particul ...
,
emotion Emotions are physical and mental states brought on by neurophysiology, neurophysiological changes, variously associated with thoughts, feelings, behavior, behavioral responses, and a degree of pleasure or suffering, displeasure. There is ...
, attachment behaviour, the response to stress and
pain Pain is a distressing feeling often caused by intense or damaging Stimulus (physiology), stimuli. The International Association for the Study of Pain defines pain as "an unpleasant sense, sensory and emotional experience associated with, or res ...
, control of food intake, and the rewarding effects of
alcohol Alcohol may refer to: Common uses * Alcohol (chemistry), a class of compounds * Ethanol, one of several alcohols, commonly known as alcohol in everyday life ** Alcohol (drug), intoxicant found in alcoholic beverages ** Alcoholic beverage, an alco ...
and
nicotine Nicotine is a natural product, naturally produced alkaloid in the nightshade family of plants (most predominantly in tobacco and ''Duboisia hopwoodii'') and is widely used recreational drug use, recreationally as a stimulant and anxiolytic. As ...
. Opioid-like peptides may also be absorbed from partially digested
food Food is any substance consumed by an organism for Nutrient, nutritional support. Food is usually of plant, animal, or Fungus, fungal origin and contains essential nutrients such as carbohydrates, fats, protein (nutrient), proteins, vitamins, ...
(
casomorphin Casomorphin is an opioid peptide (protein fragment) derived from the digestion of the milk protein casein. Health Digestive enzymes can break casein down into peptides that have some biological activity in cells and in laboratory animals though ...
s, exorphins, and rubiscolins). Opioid peptides from food typically have lengths between 4–8
amino acid Amino acids are organic compounds that contain both amino and carboxylic acid functional groups. Although over 500 amino acids exist in nature, by far the most important are the 22 α-amino acids incorporated into proteins. Only these 22 a ...
s. Endogenous opioids are generally much longer. Opioid peptides are released by post-translational proteolytic cleavage of precursor proteins. The precursors consist of the following components: a signal sequence that precedes a conserved region of about 50 residues; a variable-length region; and the sequence of the
neuropeptides Neuropeptides are chemical messengers made up of small chains of amino acids that are synthesized and released by neurons. Neuropeptides typically bind to G protein-coupled receptors (GPCRs) to modulate neural activity and other tissues like the ...
themselves.
Sequence In mathematics, a sequence is an enumerated collection of objects in which repetitions are allowed and order matters. Like a set, it contains members (also called ''elements'', or ''terms''). The number of elements (possibly infinite) is cal ...
analysis reveals that the conserved
N-terminal The N-terminus (also known as the amino-terminus, NH2-terminus, N-terminal end or amine-terminus) is the start of a protein or polypeptide, referring to the free amine group (-NH2) located at the end of a polypeptide. Within a peptide, the amin ...
region of the precursors contains 6
cysteine Cysteine (; symbol Cys or C) is a semiessential proteinogenic amino acid with the chemical formula, formula . The thiol side chain in cysteine enables the formation of Disulfide, disulfide bonds, and often participates in enzymatic reactions as ...
s, which are probably involved in
disulfide bond In chemistry, a disulfide (or disulphide in British English) is a compound containing a functional group or the anion. The linkage is also called an SS-bond or sometimes a disulfide bridge and usually derived from two thiol groups. In inor ...
formation. It is speculated that this region might be important for neuropeptide processing.


Endogenous

The human
genome A genome is all the genetic information of an organism. It consists of nucleotide sequences of DNA (or RNA in RNA viruses). The nuclear genome includes protein-coding genes and non-coding genes, other functional regions of the genome such as ...
contains several homologous
gene In biology, the word gene has two meanings. The Mendelian gene is a basic unit of heredity. The molecular gene is a sequence of nucleotides in DNA that is transcribed to produce a functional RNA. There are two types of molecular genes: protei ...
s that are known to
code In communications and information processing, code is a system of rules to convert information—such as a letter, word, sound, image, or gesture—into another form, sometimes shortened or secret, for communication through a communicati ...
for endogenous opioid peptides. * The nucleotide sequence of the human gene for
proopiomelanocortin Pro-opiomelanocortin (POMC) is a precursor polypeptide with 241 amino acid residues. POMC is Protein biosynthesis, synthesized in Corticotropic cell, corticotrophs of the anterior pituitary from the 267-amino-acid-long Precursor polypeptide, pol ...
(POMC) was characterized in 1980. The POMC gene codes for endogenous opioids such as β-endorphin and γ-endorphin. * The human gene for the
enkephalin An enkephalin is a pentapeptide involved in regulating nociception (pain sensation) in the body. The enkephalins are termed endogenous ligands, as they are internally derived (and therefore endogenous) and bind as ligands to the body's opioid ...
s was isolated and its sequence described in 1982. * The human gene for dynorphins (originally called the "Enkephalin B" gene because of sequence similarity to the enkephalin gene) was isolated and its sequence described in 1983. * The PNOC gene encoding prepronociceptin, which is cleaved into nociceptin and potentially two additional neuropeptides. * Adrenorphin, amidorphin, and leumorphin were discovered in the 1980s. * The endomorphins were discovered in the 1990s. * Opiorphin and spinorphin,
enkephalinase inhibitor An enkephalinase inhibitor is a type of enzyme inhibitor which inhibits one or more members of the enkephalinase class of enzymes that break down the endogenous enkephalin opioid peptides. Examples include racecadotril, ubenimex (bestatin), RB-1 ...
s (i.e., prevent the metabolism of enkephalins). * Hemorphins,
hemoglobin Hemoglobin (haemoglobin, Hb or Hgb) is a protein containing iron that facilitates the transportation of oxygen in red blood cells. Almost all vertebrates contain hemoglobin, with the sole exception of the fish family Channichthyidae. Hemoglobin ...
-derived opioid peptides, including hemorphin-4, valorphin, and spinorphin, among others. While not peptides,
codeine Codeine is an opiate and prodrug of morphine mainly used to treat pain, coughing, and diarrhea. It is also commonly used as a recreational drug. It is found naturally in the sap of the opium poppy, ''Papaver somniferum''. It is typically use ...
and
morphine Morphine, formerly also called morphia, is an opiate that is found naturally in opium, a dark brown resin produced by drying the latex of opium poppies (''Papaver somniferum''). It is mainly used as an analgesic (pain medication). There are ...
are also produced in the human body.


Exogenous

Exogenous opioid substances are called exorphins, as opposed to
endorphins Endorphins (contracted from endogenous morphine) are peptides produced in the brain that block the perception of pain and increase feelings of wellbeing. They are produced and stored in the pituitary gland of the brain. Endorphins are endogeno ...
. Exorphins include
opioid food peptides Opioid food peptides include: * Casomorphin (from milk) * Gluten exorphin (from gluten) * Gliadorphin, Gliadorphin/gluteomorphin (from gluten) * Rubiscolin (from spinach) * Soymorphin-5 (from soy) * Oryzatensin (from rice) Peptides Opioids {{i ...
, such as gluten exorphin and
opioid food peptides Opioid food peptides include: * Casomorphin (from milk) * Gluten exorphin (from gluten) * Gliadorphin, Gliadorphin/gluteomorphin (from gluten) * Rubiscolin (from spinach) * Soymorphin-5 (from soy) * Oryzatensin (from rice) Peptides Opioids {{i ...
, and are often contained in cereals and animal milk. Exorphins mimic the actions of endorphins by binding to and activating
opioid receptor Opioid receptors are a group of inhibitory G protein-coupled receptors with opioids as ligands. The endogenous opioids are dynorphins, enkephalins, endorphins, endomorphins and nociceptin. The opioid receptors are ~40% identical to somatostati ...
s in the brain. Common exorphins include: *
Casomorphin Casomorphin is an opioid peptide (protein fragment) derived from the digestion of the milk protein casein. Health Digestive enzymes can break casein down into peptides that have some biological activity in cells and in laboratory animals though ...
(from
casein Casein ( , from Latin ''caseus'' "cheese") is a family of related phosphoproteins (CSN1S1, αS1, aS2, CSN2, β, K-casein, κ) that are commonly found in mammalian milk, comprising about 80% of the proteins in cow's milk and between 20% and 60% of ...
found in milk of mammals, including cows and humans) * Gluten exorphin (from
gluten Gluten is a structural protein naturally found in certain Cereal, cereal grains. The term ''gluten'' usually refers to the elastic network of a wheat grain's proteins, gliadin and glutenin primarily, that forms readily with the addition of water ...
found in
cereal A cereal is a grass cultivated for its edible grain. Cereals are the world's largest crops, and are therefore staple foods. They include rice, wheat, rye, oats, barley, millet, and maize ( Corn). Edible grains from other plant families, ...
s wheat, rye, barley), including: ** Gliadorphin/gluteomorphin * Soymorphin-5 (from
soybean The soybean, soy bean, or soya bean (''Glycine max'') is a species of legume native to East Asia, widely grown for its edible bean. Soy is a staple crop, the world's most grown legume, and an important animal feed. Soy is a key source o ...
) * Rubiscolin (from
spinach Spinach (''Spinacia oleracea'') is a leafy green flowering plant native to Central Asia, Central and Western Asia. It is of the order Caryophyllales, family Amaranthaceae, subfamily Chenopodioideae. Its leaves are a common vegetable consumed eit ...
)


Amphibian

* Deltorphin * Deltorphin I * Deltorphin II * Dermorphin


Synthetic

* Zyklophin – semisynthetic KOR antagonist derived from dynorphin A


References


External links

* {{Authority control Protein families