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Updated: Oct 17, 2025

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Agathadiol, a labdane diterpenoid from juniper berries, is a positive allosteric modulator of CB1R
Stefano Salamone1, Giovanni Appendino1, Adil Khalili1
1Dipartimento di Scienze del Farmaco, Largo Donegani 2, 28100 Novara, Italy.
Abstract:
The neutral fraction of a juniper (Juniperus communis L.) berries acetone extract could positively modulate the activity of type 1 - cannabinoid receptor (CB1R). Bioactivity-directed fractionation identified the labdane diterpenoid agathadiol (4) as a positive allosteric modulator of CB1R, while closely related analogues were inactive. Agathadiol (4) is a minor constituent of juniper, but could be more conveniently obtained by semisynthesis from agathic acid (8), a major constituent of Manila copal.
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