A tetrapeptide ?-opioid receptor agonist
Bilaid C is a tetrapeptide µ-opioid receptor agonist (Ki = 210 nM in HEK293 cell membranes expressing the human receptor) that has been found in Penicillium.1 It inhibits forskolin-induced cAMP accumulation by 77% in HEK293 cells expressing the human µ-opioid receptor when used at a concentration of 10 µM. Bilaid C induces inward rectifying potassium channel (Kir) currents in rat locus coeruleus slices that endogenously express high levels of the µ-opioid receptor (EC50 = 4.2 µM).
1.Dekan, Z., Sianati, S., Yousuf, A., et al.A tetrapeptide class of biased analgesics from an Australian fungus targets the µ-opioid receptorProc. Natl. Acad. Sci. USA116(44)22353-22358(2019)
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