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A new class of synthetic cannabinoids has emerged as new psychoactive substances (NPS). Similar in structure to JWH‐022, these substances contain alkene modifications to the tail region of the synthetic cannabinoid core structure, and nomenclature denotes these new analogues as pent‐4en or but‐3en species. Internationally, two analogues from this new series recently emerged: MDMB‐4en‐PINACA and MMB‐4en‐PICA. Previously, data regarding activity and potential toxicity were not available. In vitro assessment of cannabinoid receptor 1 (CB1) activation via the β‐arrestin 2 recruitment was studied for three (3) pent‐4en analogues, one (1) but‐3en analogue, and one (1) principal metabolite. MDMB‐4en‐PINACA (2.47 nM, 239%), MDMB‐4en‐PICA (11.5 nM, 302%), and MDMB‐3en‐BINACA (14.3 nM, 286%) were highly potent and efficacious (comparison: JWH‐018, 25.3 nM, 100%), while the potencies …