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[[ファイル:Q7RTS3.pdb|サムネイル|'''図2. ヒトPTF1A立体構造'''<br>AlphaFold予測（Q7RTS3）]]
{| class="wikitable" style="width:80%"
|+ 内因性オピオイドペプチドとその受容体
|-
! scope="col" | オピオイドペプチド
! scope="col" | [[アミノ酸配列]]
! scope="col" | [[オピオイド受容体]] 標的
! scope="col" | <small>参考文献</small>
|-
! scope="col" colspan="1" | [[エンケファリン]]
! scope="col" colspan="3" |
|-
| [[ロイ-エンケファリン]] || YGGFL || [[δ-オピオイド受容体]]<sup>†</sup>、[[μ-オピオイド受容体]]<sup>†</sup> || <ref name="Endogenous opioid families - 2012 review">{{cite journal | vauthors = Li Y, Lefever MR, Muthu D, Bidlack JM, Bilsky EJ, Polt R | title = Opioid glycopeptide analgesics derived from endogenous enkephalins and endorphins | journal = [[Future Medicinal Chemistry]] | volume = 4 | issue = 2 | pages = 205–226 | date = February 2012 | pmid = 22300099 | pmc = 3306179 | doi = 10.4155/fmc.11.195 | postscript = ,}} in particular [https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3306179/table/T1/ Table 1: Endogenous opioid peptides].</ref><ref name="IUPHAR Opioid receptors - Introduction">{{cite web | title=Opioid receptors: Introduction | url=http://www.guidetopharmacology.org/GRAC/FamilyIntroductionForward?familyId=50 | work= IUPHAR/BPS Guide to PHARMACOLOGY | publisher=International Union of Basic and Clinical Pharmacology | vauthors = Toll L, Caló G, Cox BM, Chavkin C, Christie MJ, Civelli O, Connor M, Devi LA, Evans C, Henderson G, Höllt V, Kieffer B, Kitchen I, Kreek MJ, Liu-Chen LY, Meunier JC, Portoghese PS, Shippenberg TS, Simon EJ, Traynor JR, Ueda H, Wong YH | access-date = 20 October 2017 | date=10 August 2015 }}</ref><ref name="IUPHAR - δ-opioid receptor" />
|-
| [[メチオニン-エンケファリン]] || YGGFM || [[δ-オピオイド受容体]]<sup>†</sup>、[[μ-オピオイド受容体]]<sup>†</sup> || <ref name="Endogenous opioid families - 2012 review" /><ref name="IUPHAR Opioid receptors - Introduction" /><ref name="IUPHAR - δ-opioid receptor" />
|-
| [[メトルファミド]] || YGGFMRRV-NH<sub>2</sub> || [[δ-オピオイド受容体]]、[[μ-オピオイド受容体]] || <ref name="Endogenous opioid families - 2012 review" />
|-
| [[ペプチドE]] || YGGFMRRVGRPEWWMDYQKRYGGFL || [[μ-オピオイド受容体]]、[[κ-オピオイド受容体]] || <ref name="Endogenous opioid families - 2012 review" />
|-
! scope="col" colspan="1" | [[エンドルフィン]]
! scope="col" colspan="3" |
|-
| [[α-エンドルフィン]] || YGGFMTSEKSQTPLVT || [[μ-オピオイド受容体]]、他のオピオイド受容体への親和性は不明 || <ref name="Endogenous opioid families - 2012 review" />
|-
| [[β-エンドルフィン]] || YGGFMTSEKSQTPLVTLFKNAIIKNAYKKGE || [[μ-オピオイド受容体]]<sup>†‡</sup>、[[δ-オピオイド受容体]]<sup>†</sup> || <ref name="Endogenous opioid families - 2012 review" /><ref name="IUPHAR Opioid receptors - Introduction" /><ref name="IUPHAR - δ-opioid receptor">{{cite web | title=δ receptor|url=http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=317 | work= IUPHAR/BPS Guide to PHARMACOLOGY | publisher=International Union of Basic and Clinical Pharmacology | access-date= 28 December 2017 | date=15 May 2017 | quote = Principal endogenous agonists (Human) [are]<br />β-endorphin (POMC, P01189), [Leu]enkephalin (PENK, P01210), [Met]enkephalin (PENK, P01210)}}</ref><ref name="IUPHAR - μ-opioid receptor">{{cite web | title=μ receptor|url=http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=319 | work= IUPHAR/BPS Guide to PHARMACOLOGY | publisher=International Union of Basic and Clinical Pharmacology | access-date= 28 December 2017 | date=15 March 2017 | quote = Comments: β-Endorphin is the highest potency endogenous ligand&nbsp;...<br />Morphine occurs endogenously ([[#Poeaknapo|Poeaknapo et. al. 2004]])&nbsp;...<br />Principal endogenous agonists (Human) [are]<br />β-endorphin (POMC, P01189), [Met]enkephalin (PENK, P01210), [Leu]enkephalin (PENK, P01210)}}, citing:
* {{cite journal | vauthors = Poeaknapo C, Schmidt J, Brandsch M, Dräger B, Zenk MH | year = 2004 | title = Endogenous formation of morphine in human cells | journal = Proc. Natl. Acad. Sci. USA | volume = 101 | issue = 39 | pages = 14091–6 | doi = 10.1073/pnas.0405430101 | doi-access = free | pmc = 521124 | pmid = 15383669 | bibcode = 2004PNAS..10114091P | ref = Poeaknapo}}
</ref>
|-
| [[γ-エンドルフィン]] || YGGFMTSEKSQTPLVTL || [[μ-オピオイド受容体]]、他のオピオイド受容体への親和性は不明 || <ref name="Endogenous opioid families - 2012 review" />
|-
! scope="col" colspan="1" | [[ダイノルフィン]]
! scope="col" colspan="3" |
|-
| [[ダイノルフィンA]] || YGGFLRRIRPKLKWDNQ || [[κ-オピオイド受容体]]<sup>†‡</sup> || <ref name="Endogenous opioid families - 2012 review" /><ref name="IUPHAR Opioid receptors - Introduction" /><ref name="IUPHAR - κ-opioid receptor" />
|-
| [[ダイノルフィンA<sub>1–8</sub>]] || YGGFLRRI || [[κ-オピオイド受容体]]、[[μ-オピオイド受容体]]（[[δ-オピオイド受容体]]に対して部分アゴニスト） || <ref name="HMDB Dynorphin A 1-8">{{cite encyclopedia | title=Dynorphin A 1–8 | url=http://www.hmdb.ca/metabolites/HMDB0012933 | encyclopedia=HMDB Version&nbsp;4.0 | publisher=Human Metabolome Database | access-date=20 October 2017 | date=27 September 2017 | quote = Dynorphin A (1–8) is a fraction of Dynorphin A with only Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile peptide chain.}}</ref><ref name="IUPHAR - Dynorphin A-(1-8) - Biological activity">{{cite web | title=Dynorphin A-(1–8): Biological activity | url=http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?tab=biology&ligandId=1621 | work= IUPHAR/BPS Guide to PHARMACOLOGY | publisher=International Union of Basic and Clinical Pharmacology | access-date= 20 October 2017 }}</ref>
|-
| [[ダイノルフィンB]] || YGGFLRRQFKVVT || [[κ-オピオイド受容体]] || <ref name="Endogenous opioid families - 2012 review" /><ref name="IUPHAR Opioid receptors - Introduction" />
|-
| [[ビッグダイノルフィン]] || YGGFLRRIRPKLKWDNQKRYGGFLRRQFKVVT || [[κ-オピオイド受容体]]<sup>†‡</sup> || <ref name="IUPHAR - κ-opioid receptor">{{cite web | title=κ receptor|url=http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=318 | work= IUPHAR/BPS Guide to PHARMACOLOGY | publisher=International Union of Basic and Clinical Pharmacology | access-date= 28 December 2017 | date=21 February 2017 | quote = Comments: Dynorphin A and big dynorphin are the highest potency endogenous ligands&nbsp;...<br />Principal endogenous agonists (Human) [are]<br />big dynorphin (PDYN, P01213), dynorphin A (PDYN, P01213)}}</ref><ref name="IUPHAR - Big dynorphin - Biological activity">{{cite web | title=Big dynorphin: Biological activity|url=http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?tab=biology&ligandId=3669 | work= IUPHAR/BPS Guide to PHARMACOLOGY | publisher=International Union of Basic and Clinical Pharmacology | access-date= 20 October 2017 | quote = Principal endogenous agonists at κ receptor}}.</ref><ref name="IUPHAR - Big dynorphin - Structure">{{cite web | title=Big dynorphin: Structure&nbsp;– Peptide Sequence | url=http://www.guidetopharmacology.org/GRAC/LigandDisplayForward?tab=structure&ligandId=3669 | work= IUPHAR/BPS Guide to PHARMACOLOGY | publisher=International Union of Basic and Clinical Pharmacology | access-date= 20 October 2017 | quote = Peptide sequence<br />YGGFLRRIRPKLKWDNQKRYGGFLRRQFKVVT}}</ref>
|-
| [[リューモルフィン]] || YGGFLRRQFKVVTRSQEDPNAYYEELFDV || [[κ-オピオイド受容体]] || <ref name="Dynorphins 2009 review">{{cite journal | vauthors = Schwarzer C | title = 30 years of dynorphins—new insights on their functions in neuropsychiatric diseases | journal = Pharmacology & Therapeutics | volume = 123 | issue = 3 | pages = 353–370 | date = September 2009 | pmid = 19481570 | pmc = 2872771 | doi = 10.1016/j.pharmthera.2009.05.006 }}</ref><ref name="PubChem - Leumorphin">{{cite encyclopedia | title=Dynorphin B (1-29) | url = https://pubchem.ncbi.nlm.nih.gov/compound/16131065 | encyclopedia=PubChem Compound | publisher=United States National Library of Medicine&nbsp;– National Center for Biotechnology Information | access-date=28 December 2017 | date=23 December 2017}}</ref><ref name="Leumorphin primary 1">{{cite journal | vauthors = Suda M, Nakao K, Yoshimasa T, Sakamoto M, Morii N, Ikeda Y, Yanaihara C, Yanaihara N, Numa S, Imura H | title = Human leumorphin is a potent, kappa opioid receptor agonist | journal = Neuroscience Letters | volume = 50 | issue = 1–3 | pages = 49–52 | date = September 1984 | pmid = 6149506 | doi = 10.1016/0304-3940(84)90460-9 | s2cid = 42419724 }}</ref><ref name="Leumorphin primary 2">{{cite journal | vauthors = Inenaga K, Nagatomo T, Nakao K, Yanaihara N, Yamashita H | title = Kappa-selective agonists decrease postsynaptic potentials and calcium components of action potentials in the supraoptic nucleus of rat hypothalamus in vitro | journal = Neuroscience | volume = 58 | issue = 2 | pages = 331–340 | date = January 1994 | pmid = 7908725 | doi = 10.1016/0306-4522(94)90039-6| s2cid = 24631286 }}</ref>
|-
| [[α-ネオエンドルフィン]] || YGGFLRKYPK || [[κ-オピオイド受容体]] || <ref name="Endogenous opioid families - 2012 review" /><ref name="IUPHAR Opioid receptors - Introduction" />
|-
| [[β-ネオエンドルフィン]] || YGGFLRKYP || [[κ-オピオイド受容体]] || <ref name="Endogenous opioid families - 2012 review" />
|-
! scope="col" colspan="1" | [[ノシセプチン]]
! scope="col" colspan="3" |
|-
| [[ノシセプチン]] || FGGFTGARKSARKLANQ || [[ノシセプチン受容体]]<sup>†‡</sup> || <ref name="Endogenous opioid families - 2012 review" /><ref name="IUPHAR Opioid receptors - Introduction" /><ref name="IUPHAR - nociceptin receptor">{{cite web | title=NOP receptor|url=http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=320 | work= IUPHAR/BPS Guide to PHARMACOLOGY | publisher=International Union of Basic and Clinical Pharmacology | access-date= 28 December 2017 | date=18 August 2017 | quote = Natural/Endogenous Ligands<br />nociceptin/orphanin FQ}}</ref>
|-
! scope="col" colspan="1" | [[エンドモルフィン]]
! scope="col" colspan="3" |
|-
| [[エンドモルフィン-1]] || YPWF-NH<sub>2</sub> || [[μ-オピオイド受容体]] || <ref name="Endogenous opioid families - 2012 review" /><ref name="IUPHAR Opioid receptors - Introduction" />
|-
| [[エンドモルフィン-2]] || YPFF-NH<sub>2</sub> || [[μ-オピオイド受容体]] || <ref name="Endogenous opioid families - 2012 review" /><ref name="IUPHAR Opioid receptors - Introduction" />
|-
! scope="col" colspan="4" style="text-align:left" | <sup>†</sup> この記号は、そのペプチドがヒトにおいて当該受容体の主要な内因性アゴニストであることを示す。<br /><sup>‡</sup> この記号は、そのペプチドがヒトにおいて当該受容体に対して最も高い既知の[[効力 (薬理学)|効力]]を持つ内因性リガンドであることを示す。
|}

2025年8月14日 (木) 16:23時点における版

内因性オピオイドペプチドとその受容体
オピオイドペプチド アミノ酸配列 オピオイド受容体 標的 参考文献
エンケファリン
ロイ-エンケファリン YGGFL δ-オピオイド受容体†、μ-オピオイド受容体† [1][2][3]
メチオニン-エンケファリン YGGFM δ-オピオイド受容体†、μ-オピオイド受容体† [1][2][3]
メトルファミド YGGFMRRV-NH2 δ-オピオイド受容体、μ-オピオイド受容体 [1]
ペプチドE YGGFMRRVGRPEWWMDYQKRYGGFL μ-オピオイド受容体、κ-オピオイド受容体 [1]
エンドルフィン
α-エンドルフィン YGGFMTSEKSQTPLVT μ-オピオイド受容体、他のオピオイド受容体への親和性は不明 [1]
β-エンドルフィン YGGFMTSEKSQTPLVTLFKNAIIKNAYKKGE μ-オピオイド受容体†‡、δ-オピオイド受容体† [1][2][3][4]
γ-エンドルフィン YGGFMTSEKSQTPLVTL μ-オピオイド受容体、他のオピオイド受容体への親和性は不明 [1]
ダイノルフィン
ダイノルフィンA YGGFLRRIRPKLKWDNQ κ-オピオイド受容体†‡ [1][2][5]
[[ダイノルフィンA1–8]] YGGFLRRI κ-オピオイド受容体、μ-オピオイド受容体（δ-オピオイド受容体に対して部分アゴニスト） [6][7]
ダイノルフィンB YGGFLRRQFKVVT κ-オピオイド受容体 [1][2]
ビッグダイノルフィン YGGFLRRIRPKLKWDNQKRYGGFLRRQFKVVT κ-オピオイド受容体†‡ [5][8][9]
リューモルフィン YGGFLRRQFKVVTRSQEDPNAYYEELFDV κ-オピオイド受容体 [10][11][12][13]
α-ネオエンドルフィン YGGFLRKYPK κ-オピオイド受容体 [1][2]
β-ネオエンドルフィン YGGFLRKYP κ-オピオイド受容体 [1]
ノシセプチン
ノシセプチン FGGFTGARKSARKLANQ ノシセプチン受容体†‡ [1][2][14]
エンドモルフィン
エンドモルフィン-1 YPWF-NH2 μ-オピオイド受容体 [1][2]
エンドモルフィン-2 YPFF-NH2 μ-オピオイド受容体 [1][2]
† この記号は、そのペプチドがヒトにおいて当該受容体の主要な内因性アゴニストであることを示す。
‡ この記号は、そのペプチドがヒトにおいて当該受容体に対して最も高い既知の効力を持つ内因性リガンドであることを示す。
  1. ↑ 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 1.11 1.12 1.13 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): 205–226. doi:10.4155/fmc.11.195. PMC 3306179. PMID 22300099, in particular Table 1: Endogenous opioid peptides.
  2. ↑ 2.0 2.1 2.2 2.3 2.4 2.5 2.6 2.7 2.8 Toll L, Caló G, Cox BM, Chavkin C, Christie MJ, Civelli O, Connor M, Devi LA, Evans C, Henderson G, Höllt V, Kieffer B, Kitchen I, Kreek MJ, Liu-Chen LY, Meunier JC, Portoghese PS, Shippenberg TS, Simon EJ, Traynor JR, Ueda H, Wong YH (10 August 2015). "Opioid receptors: Introduction". IUPHAR/BPS Guide to PHARMACOLOGY. International Union of Basic and Clinical Pharmacology. Retrieved 20 October 2017.
  3. ↑ 3.0 3.1 3.2 "δ receptor". IUPHAR/BPS Guide to PHARMACOLOGY. International Union of Basic and Clinical Pharmacology. 15 May 2017. Retrieved 28 December 2017. Principal endogenous agonists (Human) [are]
    β-endorphin (POMC, P01189), [Leu]enkephalin (PENK, P01210), [Met]enkephalin (PENK, P01210)
  4. ↑ "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 (Poeaknapo et. al. 2004) ...
    Principal endogenous agonists (Human) [are]
    β-endorphin (POMC, P01189), [Met]enkephalin (PENK, P01210), [Leu]enkephalin (PENK, P01210)    , citing:
  5. ↑ 5.0 5.1 "κ receptor". IUPHAR/BPS Guide to PHARMACOLOGY. International Union of Basic and Clinical Pharmacology. 21 February 2017. Retrieved 28 December 2017. Comments: Dynorphin A and big dynorphin are the highest potency endogenous ligands ...
    Principal endogenous agonists (Human) [are]
    big dynorphin (PDYN, P01213), dynorphin A (PDYN, P01213)
  6. ↑ "Dynorphin A 1–8". HMDB Version 4.0. Human Metabolome Database. 27 September 2017. Retrieved 20 October 2017. Dynorphin A (1–8) is a fraction of Dynorphin A with only Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile peptide chain.
  7. ↑ "Dynorphin A-(1–8): Biological activity". IUPHAR/BPS Guide to PHARMACOLOGY. International Union of Basic and Clinical Pharmacology. Retrieved 20 October 2017.
  8. ↑ "Big dynorphin: Biological activity". IUPHAR/BPS Guide to PHARMACOLOGY. International Union of Basic and Clinical Pharmacology. Retrieved 20 October 2017. Principal endogenous agonists at κ receptor.
  9. ↑ "Big dynorphin: Structure – Peptide Sequence". IUPHAR/BPS Guide to PHARMACOLOGY. International Union of Basic and Clinical Pharmacology. Retrieved 20 October 2017. Peptide sequence
    YGGFLRRIRPKLKWDNQKRYGGFLRRQFKVVT
  10. ↑ Schwarzer C (September 2009). "30 years of dynorphins—new insights on their functions in neuropsychiatric diseases". Pharmacology & Therapeutics. 123 (3): 353–370. doi:10.1016/j.pharmthera.2009.05.006. PMC 2872771. PMID 19481570.
  11. ↑ "Dynorphin B (1-29)". PubChem Compound. United States National Library of Medicine – National Center for Biotechnology Information. 23 December 2017. Retrieved 28 December 2017.
  12. ↑ Suda M, Nakao K, Yoshimasa T, Sakamoto M, Morii N, Ikeda Y, Yanaihara C, Yanaihara N, Numa S, Imura H (September 1984). "Human leumorphin is a potent, kappa opioid receptor agonist". Neuroscience Letters. 50 (1–3): 49–52. doi:10.1016/0304-3940(84)90460-9. PMID 6149506. S2CID 42419724.
  13. ↑ Inenaga K, Nagatomo T, Nakao K, Yanaihara N, Yamashita H (January 1994). "Kappa-selective agonists decrease postsynaptic potentials and calcium components of action potentials in the supraoptic nucleus of rat hypothalamus in vitro". Neuroscience. 58 (2): 331–340. doi:10.1016/0306-4522(94)90039-6. PMID 7908725. S2CID 24631286.
  14. ↑ "NOP receptor". IUPHAR/BPS Guide to PHARMACOLOGY. International Union of Basic and Clinical Pharmacology. 18 August 2017. Retrieved 28 December 2017. Natural/Endogenous Ligands
    nociceptin/orphanin FQ
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