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A tetrapeptide μ-opioid receptor agonist
Bilaid A is a tetrapeptide agonist of the μ-opioid receptor (Ki = 3.1 μM using HEK293 cell membranes expressing the human receptor) that has been found in Penicillium.1 It inhibits forskolin-induced cAMP accumulation in HEK293 cells expressing the human μ-opioid receptor by 21% when used at a concentration of 10 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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