orphanin FQ

WordNet

1. deprive of parents
2. a young animal without a mother
3. a child who has lost both parents
4. someone or something who lacks support or care or supervision
5. the first line of a paragraph that is set as the last line of a page or column
6. the 6th letter of the Roman alphabet (同)f

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1. 『孤児』 / 孤児の / …‘を'孤児にする

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/07/09 06:10:47」(JST)

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Nociceptin

Names
Other names Orphanin FQ
Identifiers
CAS Number	170713-75-4 Y
ChEBI	CHEBI:80266 N
ChEMBL	ChEMBL396460 Y
ChemSpider	17288154 N
IUPHAR/BPS	1681
Jmol 3D model	Interactive image
MeSH	nociceptin
PubChem	16131448
InChI InChI=1S/C79H129N27O22/c1-41(2)33-54(72(122)95-44(5)66(116)103-56(36-59(84)110)73(123)102-53(77(127)128)27-28-58(83)109)104-70(120)49(23-13-15-29-80)100-69(119)52(26-18-32-90-79(87)88)99-65(115)43(4)96-75(125)57(40-107)105-71(121)50(24-14-16-30-81)101-68(118)51(25-17-31-89-78(85)86)98-64(114)42(3)94-61(112)39-93-76(126)63(45(6)108)106-74(124)55(35-47-21-11-8-12-22-47)97-62(113)38-91-60(111)37-92-67(117)48(82)34-46-19-9-7-10-20-46/h7-12,19-22,41-45,48-57,63,107-108H,13-18,23-40,80-82H2,1-6H3,(H2,83,109)(H2,84,110)(H,91,111)(H,92,117)(H,93,126)(H,94,112)(H,95,122)(H,96,125)(H,97,113)(H,98,114)(H,99,115)(H,100,119)(H,101,118)(H,102,123)(H,103,116)(H,104,120)(H,105,121)(H,106,124)(H,127,128)(H4,85,86,89)(H4,87,88,90)/t42-,43-,44-,45+,48-,49-,50-,51-,52-,53-,54-,55-,56-,57-,63-/m0/s1 N Key: PULGYDLMFSFVBL-SMFNREODSA-N N
SMILES C[C@H]([C@@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CCC(=O)N)C(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@H](Cc2ccccc2)N)O
Properties
Chemical formula	C79H129N27O22
Molar mass	1809.04
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
N verify (what is YN ?)
Infobox references

prepronociceptin
Identifiers
Symbol	PNOC
Entrez	5368
HUGO	9163
OMIM	601459
RefSeq	NM_006228
UniProt	Q13519
Other data
Locus	Chr. 8 p21

Nociceptin/orphanin FQ (N/OFQ), a 17-amino acid neuropeptide, is the endogenous ligand for the nociceptin receptor (NOP, ORL-1), and initiates its function to act on numerous brain activities such as pain sensation and fear learning. It is derived from the prepronociceptin protein, as are a further 2 peptides, nocistatin & NocII, which inhibit the N/OFQ receptor function. Nociceptin itself acts as a potent anti-analgesic, effectively counteracting the effect of pain-relievers. The gene coding for prepronociceptin is located on Ch8p21 in humans. Nociceptin acts at the Nociceptin receptor (NOP receptor) formerly known as ORL1. Nociceptin is the first example of reverse pharmacology; the NOP receptor was discovered before the endogenous ligand which was discovered by two separate groups in 1995.

Roles of Nociceptin

Since its discovery, nociceptin has been of great interest to researchers. Nociceptin is a peptide related to the opioid class of compounds (ex. morphine and codeine), but it does not act at the classic opioid receptors (namely, mu, kappa, and delta opioid receptors) which typically act as pain relievers. Nociceptin is widely distributed in the CNS; it is found in the hypothalamus, brainstem, and forebrain, as well as in the ventral and dorsal horns of the spinal cord. The NOP receptor is also widely distributed throughout areas of the brain, including the cortex, anterior olfactory nucleus, lateral septum, hypothalamus, hippocampus, amygdala, central gray, pontine nuclei, interpeduncular nucleus, substantia nigra, raphe complex, locus coeruleus, and spinal cord.

Pain

The N/OFQ-NOP system is found in central and peripheral nervous tissue, where it is well placed to modulate nociception, or the body's sensation of pain. Unlike morphine and other opioids that are used to alleviate pain, nociceptin's role in nociception is not straightforward. Administration of N/OFQ in the brain causes increased sensations of pain (hyperalgesia). This makes it unique from classic opioid peptides, which typically act as analgesics (pain relievers), as it means that nociceptin can even counteract analgesia, thus acting as an antiopioid. Additionally, blocking the nociceptin receptor can lead to an increased pain threshold and a decreased tolerance development to analgesic opioids. As such, nociceptin has a lower risk of addiction than many pain relievers that are currently used. Recent studies have proposed that this anti-analgesic function of nociceptin stems from the inhibition of the periaqueductal grey, which controls pain modulation from the central nervous system. This effect of nociceptin may lead to its future use as a method to reduce morphine dosage and decrease the development of tolerance and dependence. When administered to the spinal cord, nociceptin produces similar analgesic effects to classical opioids.

Mood Disorders

There are various studies on animals that suggest that the N/OFQ-NOP system has a part to play in both anxiety and depression. It appears that nociceptin is an anxiolytic (anxiety inhibitor) but also seems to perpetuate depression, since preventing N/OFQ from binding to NOP seems to improve depression.

Drug Abuse Medications

The NOP receptor has shown potential as a target for medications designed to alleviate the effects of substance abuse disorders. Areas in the hypothalamus and amygdala that correlate to the reward process of drug abuse have been found to contain NOP receptors. Nociceptin has also been found to inhibit dopamine production related to the reward process. Specifically, nociceptin acts to inhibit neural rewards induced by drugs such as amphetamines, morphine, cocaine, and especially alcohol in animal models, though the exact mechanism of this has not yet been proven. Additionally, nociceptin may have lower tolerance development than drugs such as morphine. This was shown when nociceptin compounds were used as a pain medication substitution for morphine. Nociceptin also has therapeutic capabilities for addictions to multiple drugs, potentially playing a role in compounds that have decreased withdrawal tendencies (such as muscle aches, anxiety, and restlessness).

Learning and Memory

In animal studies, the N/OFQ-NOP receptor pathway has also been found to play both positive and negative roles in both learning and memory. For example, malfunctions in this pathway are linked to altered fear learning in brain disorders such as post-traumatic stress disorder (PTSD). As such, the receptor pathway maintains homeostatic responses to fear and stressful situations. Nociceptin could also play an inhibitory role in memory function, as some studies show that it impairs spatial learning in vivo, while inhibiting long term potentiation and synaptic transmission in vitro.

Cardiovascular System

The N/OFQ-NOP system has also been implicated in control of the cardiovascular system, as nociceptin administration has led to high blood pressure and bradycardia. Nociceptin has significant effects on cardiovascular parameters such as blood pressure and heart rate that vary by species, as it is excitatory for rodents yet inhibitory for sheep.

Renal System

In the renal system, nociceptin plays a role in water balance, electrolyte balance, and arterial blood pressure regulation. It has also shown potential as a diuretic treatment for alleviating water-retaining diseases.

Immune System

Additional research suggests that nociceptin may be involved in the immune system and sepsis. A study at the University of Leicester looked at patients who were critically ill with sepsis and found that blood N/OFQ levels were significantly higher in patients who died within thirty days in comparison to survivors.

Digestive System

In the gut, nociceptin has been found to have varying effects on stomach and intestinal contractility while also stimulating the increased consumption of food. Additional studies have shown that nociceptin may have an effect as an anti-epileptic drug component.

References

External links

• nociceptin at the US National Library of Medicine Medical Subject Headings (MeSH)
• prepronociceptin at the US National Library of Medicine Medical Subject Headings (MeSH)

UpToDate Contents

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• 1. 成人における放射線障害の治療 treatment of radiation injury in the adult
• 2. 腸チフスの治療および予防 treatment and prevention of typhoid fever

English Journal

• Nociceptin and the nociceptin receptor in learning and memory.

• Andero R1.
• Progress in neuro-psychopharmacology & biological psychiatry.Prog Neuropsychopharmacol Biol Psychiatry.2015 Oct 1;62:45-50. doi: 10.1016/j.pnpbp.2015.02.007. Epub 2015 Feb 24.
• There are many processes in which the neuropeptide nociceptin/orphanin FQ (N/OFQ or nociceptin) is involved in the brain. The role of nociceptin in learning and memory holds promise in modulating these processes in health and disease in the human brain. This review summarizes the body of research fo
• PMID 25724763

• Novel Synthesis and Pharmacological Characterization of NOP Receptor Agonist 8-(1S,3αS)-(2,3,3a,4,5,6-Hexahydro-1H-phenalin-1-yl)-1-phenyl-1,3,8-triazaspiro[4,5]decan-4-one (Ro 64-6198).

• Chang SD, Brieaddy LE, Harvey JD, Lewin AH, Mascarella SW, Seltzman HH, Reddy PA, Decker AM, McElhinny CJ, Zhong D, Peterson EE, Navarro HA, Bruchas MR, Carroll FI.
• ACS chemical neuroscience.ACS Chem Neurosci.2015 Sep 14. [Epub ahead of print]
• The nociceptin/orphanin FQ opioid peptide (NOP) receptor is a widely expressed GPCR involved in the modulation of pain, anxiety, and motor behaviors. Dissecting the functional properties of this receptor is limited by the lack of systemically active ligands that are brain permeant. The small molecul
• PMID 26367173

Japanese Journal

• The effect of serotonergic system on nociceptin/orphanin FQ induced food intake in chicken

• Zendehdel Morteza,Mokhtarpouriani Kasra,Babapour Vahab [他],BAGHBANZADEH Ali,POURRAHIMI Maryam,HASSANPOUR Shahin
• The journal of physiological sciences : JPS 63(4), 271-277, 2013-07-01
• NAID 10031184280

• Antihyperalgesic Effect of Buprenorphine Involves Nociceptin/Orphanin FQ Peptide-Receptor Activation in Rats With Spinal Nerve Injury-Induced Neuropathy

• Takahashi Tomoko,Okubo Kazumasa,Kojima Shota [他],NISHIKAWA Hiroyuki,TAKEMURA Motohide,TSUBOTA MATSUNAMI Maho,SEKIGUCHI Fumiko,KAWABATA Atsufumi
• Journal of pharmacological sciences 122(1), 51-54, 2013-05-20
• … We evaluated the effect of buprenorphine, a mixed agonist for μ-opioid receptors and nociceptin/orphanin FQ peptide (NOP) receptors, in neuropathic rats, using the paw pressure test. …
• NAID 10031177880

Related Links

• Nociceptin/Orphanin FQ （ノシセプチン）/（オルファニンFQ ...

遺伝子技術を駆使して見つかった新しいペプチド ... ホーム 新製品・新技術情報 Nociceptin/Orphanin FQ （ノシセプチン）/（オルファニンFQ） Nociceptin/Orphanin FQ （ノシセプチン）/（オルファニンFQ）

• Structure of the nociceptin/orphanin FQ receptor in complex ...

Members of the opioid receptor family of G-protein-coupled receptors (GPCRs) are found throughout the peripheral and central nervous system, where they have key roles in nociception and analgesia. Unlike the /`classical/' opioid ...

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• 孤児、オーファン

関

orphaned child

　 　 　 　 　 　

「F」

　　[★] フェニルアラニン phenylalanine