Opioidergic

Structural correlation between met-enkephalin, an opioid peptide, *(left)* and morphine, an opiate drug, *(right)*

An opioidergic agent (or drug) is a chemical which directly or indirectly modulate the function of opioid receptors. Opioidergics comprise opioids, as well as allosteric modulators and enzyme affecting agents like enkephalinase inhibitors.

Allosteric modulators

BMS-986121: μ-PAM^[1]
BMS-986122: μ-PAM^[1]
BPRMU191: confers agonistic properties to small-molecule morphinan antagonists^[2]
Ignavine^[3]
Oxytocin: μ-PAM^[4]
δ-PAM (see reference)^[5]
Cannabidiol^[6]
Tetrahydrocannabinol^[6]
Sodium (Na⁺) ^[7]

References

^ ^a ^b Burford NT, Clark MJ, Wehrman TS, et al. (June 2013). "Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor". Proc. Natl. Acad. Sci. U.S.A. 110 (26): 10830–5. Bibcode:2013PNAS..11010830B. doi:10.1073/pnas.1300393110. PMC 3696790. PMID 23754417.
^ Huang YH, Lin SY, Ou LC, et al. (2024). "Discovery of a mu-opioid receptor modulator that in combination with morphinan antagonists induces analgesia". Cell Chem Biol. 31 (11): 1885–1898.e10. doi:10.1016/j.chembiol.2024.06.013. PMID 39025070.
^ Ohbuchi K, Miyagi C, Suzuki Y, Mizuhara Y, Mizuno K, Omiya Y, Yamamoto M, Warabi E, Sudo Y, Yokoyama A, Miyano K, Hirokawa T, Uezono Y (August 2016). "Ignavine: a novel allosteric modulator of the μ opioid receptor". Sci Rep. 6: 31748. Bibcode:2016NatSR...631748O. doi:10.1038/srep31748. PMC 4987652. PMID 27530869.
^ Meguro Y, Miyano K, Hirayama S, et al. (May 2018). "Neuropeptide oxytocin enhances μ opioid receptor signaling as a positive allosteric modulator". J. Pharmacol. Sci. 137 (1): 67–75. doi:10.1016/j.jphs.2018.04.002. PMID 29716811.
^ Burford NT, Livingston KE, Canals M, Ryan MR, Budenholzer LM, Han Y, Shang Y, Herbst JJ, O'Connell J, Banks M, Zhang L, Filizola M, Bassoni DL, Wehrman TS, Christopoulos A, Traynor JR, Gerritz SW, Alt A (2015). "Discovery, Synthesis, and Molecular Pharmacology of Selective Positive Allosteric Modulators of the δ-Opioid Receptor". J. Med. Chem. 58 (10): 4220–9. doi:10.1021/acs.jmedchem.5b00007. PMC 4703104. PMID 25901762.
^ ^a ^b Kathmann M, Flau K, Redmer A, Tränkle C, Schlicker E (February 2006). "Cannabidiol is an allosteric modulator at mu- and delta-opioid receptors". Naunyn-Schmiedeberg's Arch. Pharmacol. 372 (5): 354–61. doi:10.1007/s00210-006-0033-x. PMID 16489449. S2CID 4877869.
^ Shang Y, LeRouzic V, Schneider S, Bisignano P, Pasternak GW, Filizola M (2014). "Mechanistic insights into the allosteric modulation of opioid receptors by sodium ions". Biochemistry. 53 (31): 5140–9. doi:10.1021/bi5006915. PMC 4131901. PMID 25073009.

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[pmid23754417-1] Burford NT, Clark MJ, Wehrman TS, et al. (June 2013). "Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor". Proc. Natl. Acad. Sci. U.S.A. 110 (26): 10830–5. Bibcode:2013PNAS..11010830B. doi:10.1073/pnas.1300393110. PMC 3696790. PMID 23754417.

[pmid39025070-2] Huang YH, Lin SY, Ou LC, et al. (2024). "Discovery of a mu-opioid receptor modulator that in combination with morphinan antagonists induces analgesia". Cell Chem Biol. 31 (11): 1885–1898.e10. doi:10.1016/j.chembiol.2024.06.013. PMID 39025070.

[pmid27530869-3] Ohbuchi K, Miyagi C, Suzuki Y, Mizuhara Y, Mizuno K, Omiya Y, Yamamoto M, Warabi E, Sudo Y, Yokoyama A, Miyano K, Hirokawa T, Uezono Y (August 2016). "Ignavine: a novel allosteric modulator of the μ opioid receptor". Sci Rep. 6: 31748. Bibcode:2016NatSR...631748O. doi:10.1038/srep31748. PMC 4987652. PMID 27530869.

[pmid29716811-4] Meguro Y, Miyano K, Hirayama S, et al. (May 2018). "Neuropeptide oxytocin enhances μ opioid receptor signaling as a positive allosteric modulator". J. Pharmacol. Sci. 137 (1): 67–75. doi:10.1016/j.jphs.2018.04.002. PMID 29716811.

[pmid25901762-5] Burford NT, Livingston KE, Canals M, Ryan MR, Budenholzer LM, Han Y, Shang Y, Herbst JJ, O'Connell J, Banks M, Zhang L, Filizola M, Bassoni DL, Wehrman TS, Christopoulos A, Traynor JR, Gerritz SW, Alt A (2015). "Discovery, Synthesis, and Molecular Pharmacology of Selective Positive Allosteric Modulators of the δ-Opioid Receptor". J. Med. Chem. 58 (10): 4220–9. doi:10.1021/acs.jmedchem.5b00007. PMC 4703104. PMID 25901762.

[PMID16489449-6] Kathmann M, Flau K, Redmer A, Tränkle C, Schlicker E (February 2006). "Cannabidiol is an allosteric modulator at mu- and delta-opioid receptors". Naunyn-Schmiedeberg's Arch. Pharmacol. 372 (5): 354–61. doi:10.1007/s00210-006-0033-x. PMID 16489449. S2CID 4877869.

[pmid25073009-7] Shang Y, LeRouzic V, Schneider S, Bisignano P, Pasternak GW, Filizola M (2014). "Mechanistic insights into the allosteric modulation of opioid receptors by sodium ions". Biochemistry. 53 (31): 5140–9. doi:10.1021/bi5006915. PMC 4131901. PMID 25073009.

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[2]

[3]

[4]

[5]

[6]

[7]

Allosteric modulators

See also

References