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Bilaid A1 is a tetrapeptide agonist of the μ-opioid receptor (K_i = 750 nM in HEK293 cell membranes expressing the human receptor) and a derivative of bilaid A .¹ It inhibits forskolin-induced cAMP accumulation by 47% in HEK293 cells expressing the human μ-opioid receptor when used at a concentration of 10 μM.

Bilaid A1e (Compound 1e) is a tetrapeptide agonist of the μ-opioid receptor (Ki = 750 nM). Bilaid A1e can be isolated from an Australian estuarine isolate of Penicillium sp. Bilaid A1e can be used for pain research[1].

μ Opioid Receptor/MOR: 750 nM (Ki)

1. Dekan, Z., Sianati, S., Yousuf, A., et al. A tetrapeptide class of biased analgesics from an Australian fungus targets the μ-opioid receptor Proc. Natl. Acad. Sci. USA 116(44),22353-22358(2019).