Opioidergic: Difference between revisions

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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]
δ-PAM (see reference)^[2]
Cannabidiol^[3]
Tetrahydrocannabinol^[3]
Sodium (Na⁺) ^[4]

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. doi:10.1073/pnas.1300393110. PMC 3696790. PMID 23754417.
^ 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: 4220–9. doi:10.1021/acs.jmedchem.5b00007. 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 Schmiedebergs Arch. Pharmacol. 372 (5): 354–61. doi:10.1007/s00210-006-0033-x. PMID 16489449.
^ 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. 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. doi:10.1073/pnas.1300393110. PMC 3696790. PMID 23754417.

[pmid25901762-2] 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: 4220–9. doi:10.1021/acs.jmedchem.5b00007. PMID 25901762.

[PMID16489449-3] Kathmann M, Flau K, Redmer A, Tränkle C, Schlicker E (February 2006). "Cannabidiol is an allosteric modulator at mu- and delta-opioid receptors". Naunyn Schmiedebergs Arch. Pharmacol. 372 (5): 354–61. doi:10.1007/s00210-006-0033-x. PMID 16489449.

[pmid25073009-4] 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. PMID 25073009.

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@@ Line 7: / Line 7: @@
 * BMS-986122: μ-PAM<ref name="pmid23754417"/>
 * δ-PAM (see reference)<ref name="pmid25901762">{{cite journal |vauthors=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 |title=Discovery, Synthesis, and Molecular Pharmacology of Selective Positive Allosteric Modulators of the δ-Opioid Receptor |journal=J. Med. Chem. |volume= 58|issue= |pages= 4220–9|year=2015 |pmid=25901762 |doi=10.1021/acs.jmedchem.5b00007 |url=}}</ref>
-* [[Cannabidiol]]<ref name="PMID16489449">{{cite journal | author = Kathmann M, Flau K, Redmer A, Tränkle C, Schlicker E | title = Cannabidiol is an allosteric modulator at mu- and delta-opioid receptors | journal = Naunyn Schmiedebergs Arch. Pharmacol. | volume = 372 | issue = 5 | pages = 354–61 | date = February 2006 | pmid = 16489449 | doi = 10.1007/s00210-006-0033-x }}</ref>
+* [[Cannabidiol]]<ref name="PMID16489449">{{cite journal |vauthors=Kathmann M, Flau K, Redmer A, Tränkle C, Schlicker E | title = Cannabidiol is an allosteric modulator at mu- and delta-opioid receptors | journal = Naunyn Schmiedebergs Arch. Pharmacol. | volume = 372 | issue = 5 | pages = 354–61 | date = February 2006 | pmid = 16489449 | doi = 10.1007/s00210-006-0033-x }}</ref>
 * [[Tetrahydrocannabinol]]<ref name="PMID16489449"/>
-* [[Sodium]] (Na<sup>+</sup>) <ref name="pmid25073009">{{cite journal |author=Shang Y, LeRouzic V, Schneider S, Bisignano P, Pasternak GW, Filizola M |title=Mechanistic insights into the allosteric modulation of opioid receptors by sodium ions |journal=Biochemistry |volume=53 |issue=31 |pages=5140–9 |year=2014 |pmid=25073009 |doi=10.1021/bi5006915 |url=}}</ref>
+* [[Sodium]] (Na<sup>+</sup>) <ref name="pmid25073009">{{cite journal |vauthors=Shang Y, LeRouzic V, Schneider S, Bisignano P, Pasternak GW, Filizola M |title=Mechanistic insights into the allosteric modulation of opioid receptors by sodium ions |journal=Biochemistry |volume=53 |issue=31 |pages=5140–9 |year=2014 |pmid=25073009 |doi=10.1021/bi5006915 |url=}}</ref>
 ==See also==