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==Allosteric modulators==
==Allosteric modulators==
[[File:BMS-986121.png|thumb|right|210px|BMS-986121]]
[[File:BMS-986121.png|thumb|right|210px|BMS-986121]]
* BMS-986121: μ-PAM<ref name="pmid23754417">{{cite journal |vauthors=Burford NT, Clark MJ, Wehrman TS, etal |title=Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=110 |issue=26 |pages=10830–5 |date=June 2013 |pmid=23754417 |pmc=3696790 |doi=10.1073/pnas.1300393110 }}</ref>
* BMS-986121: μ-PAM<ref name="pmid23754417">{{cite journal |vauthors=Burford NT, Clark MJ, Wehrman TS, etal |title=Discovery of positive allosteric modulators and silent allosteric modulators of the μ-opioid receptor |journal=Proc. Natl. Acad. Sci. U.S.A. |volume=110 |issue=26 |pages=10830–5 |date=June 2013 |pmid=23754417 |pmc=3696790 |doi=10.1073/pnas.1300393110 |bibcode=2013PNAS..11010830B |doi-access=free }}</ref>
* BMS-986122: μ-PAM<ref name="pmid23754417"/>
* BMS-986122: μ-PAM<ref name="pmid23754417"/>
* Ignavine<ref name="pmid27530869">{{cite journal |vauthors=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 |title=Ignavine: a novel allosteric modulator of the μ opioid receptor |journal=Sci Rep |volume=6 |pages=31748 |date=August 2016 |pmid=27530869 |pmc=4987652 |doi=10.1038/srep31748 }}</ref>
* Ignavine<ref name="pmid27530869">{{cite journal |vauthors=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 |title=Ignavine: a novel allosteric modulator of the μ opioid receptor |journal=Sci Rep |volume=6 |pages=31748 |date=August 2016 |pmid=27530869 |pmc=4987652 |doi=10.1038/srep31748 |bibcode=2016NatSR...631748O }}</ref>
* [[Oxytocin]]: μ-PAM<ref name="pmid29716811">{{cite journal |vauthors=Meguro Y, Miyano K, Hirayama S, et al |title=Neuropeptide oxytocin enhances μ opioid receptor signaling as a positive allosteric modulator |journal=J. Pharmacol. Sci. |volume=137 |issue=1 |pages=67–75 |date=May 2018 |pmid=29716811 |doi=10.1016/j.jphs.2018.04.002 |doi-access=free }}</ref>
* [[Oxytocin]]: μ-PAM<ref name="pmid29716811">{{cite journal |vauthors=Meguro Y, Miyano K, Hirayama S, et al |title=Neuropeptide oxytocin enhances μ opioid receptor signaling as a positive allosteric modulator |journal=J. Pharmacol. Sci. |volume=137 |issue=1 |pages=67–75 |date=May 2018 |pmid=29716811 |doi=10.1016/j.jphs.2018.04.002 |doi-access=free }}</ref>
* 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= 10|pages= 4220–9|year=2015 |pmid=25901762 |doi=10.1021/acs.jmedchem.5b00007 |pmc=4703104}}</ref>
* 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= 10|pages= 4220–9|year=2015 |pmid=25901762 |doi=10.1021/acs.jmedchem.5b00007 |pmc=4703104}}</ref>

Revision as of 08:30, 12 September 2021

Structural correlation between met-enkephalin, an opioid peptide, (left) and morphine, an opiate drug, (right)
Main article: Opioid

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

See also

References

  1. ^ 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.
  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 (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.
  3. ^ 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.
  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 (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.
  5. ^ 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. S2CID 4877869.
  6. ^ 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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