The type 1 and type 2 cannabinoid receptors are G protein-coupled receptors implicated in a variety of physiological processes and diseases. Synthetic cannabinoid receptor agonists (SCRAs) were originally developed to explore the therapeutic benefits of cannabinoid receptor activation, although more recently, these compounds have been diverted to the recreational drug market and are increasingly associated with incidences of toxicity. A prominent concept in contemporary pharmacology is functional selectivity or biased agonism, which describes the ability of ligands to elicit differential activation of signalling pathways through stabilisation of distinct receptor conformations. Biased agonists may maximise drug effectiveness by reducing on-target adverse effects if they are mediated by signalling pathways distinct from those that drive the therapeutic effects. For the cannabinoid receptors, it remains unclear as to which signalling pathways mediate desirable and adverse effects. However, given their structural diversity and potential to induce a plethora of signalling effects, SCRAs provide the most promising prospect for detecting and studying bias at the cannabinoid receptors. This review summarises the emerging evidence of SCRA bias at the cannabinoid receptors.

1 型和 2 型大麻素受体是 G 蛋白偶联受体，与多种生理过程和疾病有关。合成大麻素受体激动剂 (SCRA) 最初是为了探索大麻素受体激活的治疗益处而开发的，尽管最近，这些化合物已转向娱乐性药物市场，并且越来越多地与毒性发生率相关。当代药理学中的一个突出概念是功能选择性或偏向激动，它描述了配体通过稳定不同受体构象引发信号通路差异激活的能力。如果偏向激动剂由与驱动治疗效果不同的信号通路介导，则它们可以通过减少靶向不良反应来最大限度地提高药物有效性。对于大麻素受体，尚不清楚哪些信号通路介导了理想的和不利的影响。然而，鉴于其结构多样性和诱导过多信号效应的潜力，SCRA 为检测和研究大麻素受体的偏差提供了最有希望的前景。本综述总结了大麻素受体 SCRA 偏倚的新证据。SCRA 为检测和研究大麻素受体的偏差提供了最有希望的前景。本综述总结了大麻素受体 SCRA 偏倚的新证据。SCRA 为检测和研究大麻素受体的偏差提供了最有希望的前景。本综述总结了大麻素受体 SCRA 偏倚的新证据。