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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][5]
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][6]
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） [7][8]
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†‡ [6][9][10]
リューモルフィン YGGFLRRQFKVVTRSQEDPNAYYEELFDV κ-オピオイド受容体 [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, M.R., Muthu, D., Bidlack, J.M., Bilsky, E.J., & Polt, R. (2012).
    Opioid glycopeptide analgesics derived from endogenous enkephalins and endorphins. Future medicinal chemistry, 4(2), 205-26. [PubMed:22300099] [PMC] [WorldCat] [DOI]
  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)
  5. ↑ Poeaknapo, C., Schmidt, J., Brandsch, M., Dräger, B., & Zenk, M.H. (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. [PubMed:15383669] [PMC] [WorldCat] [DOI]
  6. ↑ 6.0 6.1 "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)
  7. ↑ "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.
  8. ↑ "Dynorphin A-(1–8): Biological activity". IUPHAR/BPS Guide to PHARMACOLOGY. International Union of Basic and Clinical Pharmacology. Retrieved 20 October 2017.
  9. ↑ "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.
  10. ↑ "Big dynorphin: Structure – Peptide Sequence". IUPHAR/BPS Guide to PHARMACOLOGY. International Union of Basic and Clinical Pharmacology. Retrieved 20 October 2017. Peptide sequence
    YGGFLRRIRPKLKWDNQKRYGGFLRRQFKVVT
  11. ↑ Schwarzer, C. (2009).
    30 years of dynorphins--new insights on their functions in neuropsychiatric diseases. Pharmacology & therapeutics, 123(3), 353-70. [PubMed:19481570] [PMC] [WorldCat] [DOI]
  12. ↑ Suda, M., Nakao, K., Yoshimasa, T., Sakamoto, M., Morii, N., Ikeda, Y., ..., & Imura, H. (1984).
    Human leumorphin is a potent, kappa opioid receptor agonist. Neuroscience letters, 50(1-3), 49-52. [PubMed:6149506] [WorldCat] [DOI]
  13. ↑ Inenaga, K., Nagatomo, T., Nakao, K., Yanaihara, N., & Yamashita, H. (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), 331-40. [PubMed:7908725] [WorldCat] [DOI]
  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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