New Natural Noncannabinoid Ligands for Cannabinoid Type-2 (CB2) Receptors

[Julie Gardener]

New Natural Noncannabinoid Ligands for Cannabinoid Type-2 (CB2) Receptors​

JÃœRG GERTSCH, STEFAN RADUNER and KARL-HEINZ ALTMANN
Institute of Pharmaceutical Sciences, ETH Zurich, Zürich, Switzerland
ETH Zürich, Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, ETH Hönggerberg. HCI H496, Wolfgang-Pauli-Str. 10, CH-8093, Zürich, Switzerland, Fax: +41-44-6331360
2006, Vol. 26, No. 5-6 , Pages 709-730

Abstract

Since the discovery that Δ 9-tetrahydrocannabinol and related cannabinoids from Cannabis sativa L. act on specific physiological receptors in the human body and the subsequent elucidation of the mammalian endogenous cannabinoid system, no other natural product class has been reported to mimic the effects of cannabinoids. We recently found that N-alkyl amides from purple coneflower (Echinacea spp.) constitute a new class of cannabinomimetics, which specifically engage and activate the cannabinoid type-2 (CB2) receptors. Cannabinoid type-1 (CB1) and CB2 receptors belong to the family of G protein-coupled receptors and are the primary targets of the endogenous cannabinoids N-arachidonoyl ethanolamine and 2-arachidonoyl glyerol. CB2 receptors are believed to play an important role in distinct pathophysiological processes, including metabolic dysregulation, inflammation, pain, and bone loss. CB2 receptors have, therefore, become of interest as new targets in drug discovery. This review focuses on N-alkyl amide secondary metabolites from plants and underscores that this group of compounds may provide novel lead structures for the development of CB2-directed drugs.

Source: Informa Healthcare - Journal of Receptors and Signal Transduction - 26(5-6):709 - Summary