Opioidergic Explained

See main article: article. An opioidergic agent (or drug) is a chemical which functions to directly modulate the opioid neuropeptide systems (i.e., endorphin, enkephalin, dynorphin, nociceptin) in the body or brain. Examples include opioid analgesics such as morphine and opioid antagonists such as naloxone. Opioidergics also comprise allosteric modulators and enzyme affecting agents like enkephalinase inhibitors.

Allosteric modulators

• BMS-986121: μ-PAM^[1]
• BMS-986122: μ-PAM^[1]
• Ignavine^[2]
• Oxytocin: μ-PAM^[3]
• δ-PAM (see reference)^[4]
• Cannabidiol^[5]
• Tetrahydrocannabinol^[5]
• Sodium (Na⁺) ^[6]

See also

• List of opioids
• Adenosinergic
• Adrenergic
• Cannabinoidergic
• Cholinergic
• Dopaminergic
• GABAergic
• Glycinergic
• Histaminergic
• Melatonergic
• Monoaminergic
• Serotonergic

Notes and References

1. Burford NT, Clark MJ, Wehrman TS, etal . 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 . June 2013 . 23754417 . 3696790 . 10.1073/pnas.1300393110 . 2013PNAS..11010830B . free .
2. 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 . Ignavine: a novel allosteric modulator of the μ opioid receptor . Sci Rep . 6 . 31748 . August 2016 . 27530869 . 4987652 . 10.1038/srep31748 . 2016NatSR...631748O .
3. Meguro Y, Miyano K, Hirayama S, et al . Neuropeptide oxytocin enhances μ opioid receptor signaling as a positive allosteric modulator . J. Pharmacol. Sci. . 137 . 1 . 67–75 . May 2018 . 29716811 . 10.1016/j.jphs.2018.04.002 . free .
4. 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 . Discovery, Synthesis, and Molecular Pharmacology of Selective Positive Allosteric Modulators of the δ-Opioid Receptor . J. Med. Chem. . 58. 10. 4220–9. 2015 . 25901762 . 10.1021/acs.jmedchem.5b00007 . 4703104.
5. Kathmann M, Flau K, Redmer A, Tränkle C, Schlicker E . Cannabidiol is an allosteric modulator at mu- and delta-opioid receptors . Naunyn-Schmiedeberg's Arch. Pharmacol. . 372 . 5 . 354–61 . February 2006 . 16489449 . 10.1007/s00210-006-0033-x . 4877869 .
6. Shang Y, LeRouzic V, Schneider S, Bisignano P, Pasternak GW, Filizola M . Mechanistic insights into the allosteric modulation of opioid receptors by sodium ions . Biochemistry . 53 . 31 . 5140–9 . 2014 . 25073009 . 10.1021/bi5006915 . 4131901.