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frrol

01/20/20 9:40 PM

#231344 RE: Doc328 #231342

Yes the paper is about allosteric agonists and mentions 2-73 but doesn't actually call it an allosteric agonist, just an agonist.
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georgejjl

01/20/20 11:01 PM

#231346 RE: Doc328 #231342

Allosteric modulators can be positive or negative effectors (PAMs or NAMs, respectively). PAMs increase the activity of the ligand, while NAMs block it (Figure 1).





https://www.frontiersin.org/articles/10.3389/fphar.2019.00223/full#F1

Functional responses of allosteric modulators. Positive and negative allosteric modulators (positive allosteric modulators and negative allosteric modulators) may modulate the affinity and/or the efficacy of orthosteric agonists.





Good luck and GOD bless,
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georgejjl

01/20/20 11:11 PM

#231347 RE: Doc328 #231342

Serendipitously, the (4R,5S)-isomer (E1R) was discovered to interact at the sigma-1 receptor by increasing the binding affinity of an orthosteric ligand, which is characteristic of a PAM.



https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5689070/pdf/nihms918934.pdf

Good luck and GOD bless,