The Chemistry and Pharmacology of Synthetic Cannabinoid Receptor Agonists as New Psychoactive Substances: Origins.
Samuel D Banister, Mark Connor
Handbook of experimental pharmacology 2018 DOI: 10.1007/164_2018_143 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Review Peer reviewed |
|---|---|
| Keywords | Anandamide Cp 55,940 Cannabinoid Jwh-018 Nps Win 55,212-2 Xlr-11 Δ9-tetrahydrocannabinol |
| Key findings | The chapter argues that most SCRAs are potent, high-efficacy agonists at CB1 and CB2 receptors, producing effects qualitatively similar to Δ9-THC but frequently associated with serious adverse effects including cardiotoxicity, nephrotoxicity, and death. It contends that the dynamic SCRA marketplace hampers pharmacological and toxicological characterization, and that beyond basic receptor profiling, little is known about acute or chronic effects. |
Abstract
Synthetic cannabinoid receptor agonists (SCRAs) have proliferated as new psychoactive substances (NPS) over the past decade. Relative to other classes of NPS, SCRAs are structurally heterogeneous; however, most SCRAs act as potent, high-efficacy agonists of cannabinoid type 1 and type 2 receptors (CB1 and CB2, respectively). Characterization of the pharmacology and toxicology of these substances is hindered by the dynamic nature of the SCRA marketplace. Beyond basic pharmacological profiling at CB1 and CB2 receptors, very little is known about the acute or chronic effects of SCRAs. Many of the effects of SCRAs are qualitatively similar to those of the Δ9-tetrahydrocannabinol (Δ9-THC) found in cannabis. However, unlike Δ9-THC, SCRAs are frequently associated with serious adverse effects, including cardiotoxicity, nephrotoxicity, and death. This chapter will provide an overview of the structure and function of the primary target for SCRAs, the CB1 receptor, and survey the structure-activity relationships of the historical SCRAs that served as templates for the earliest generations of NPS.
Citations in the library
Cited by 7
- Designer drugs: mechanism of action and adverse effects Archives of Toxicology April 1, 2020
- Positive Allosteric Modulation of the 5-HT1A Receptor by Indole-Based Synthetic Cannabinoids Abused by Humans ACS Chemical Neuroscience April 23, 2020
- Subtle Structural Modification of a Synthetic Cannabinoid Receptor Agonist Drastically Increases its Efficacy at the CB1 Receptor ACS Chemical Neuroscience October 17, 2023
- Pharmaco-toxicological effects of the synthetic cannabinoids 4F-ABUTINACA, SDB-005, and JWH-018 in mice. In vitro and in vivo studies. European Journal of Pharmacology April 1, 2025
- Clinical features associated with ADB-BUTINACA exposure in patients attending emergency departments in England. Clinical Toxicology October 1, 2022
and 2 more in the library
Cites 6
- Fluorine in psychedelic phenethylamines Drug Testing and Analysis February 28, 2012
- Crystal Structure of the Human Cannabinoid Receptor CB1. Cell October 20, 2016
- Cluster of Acute Toxicity from Ingestion of Synthetic Cannabinoid-Laced Brownies. Journal of Medical Toxicology December 1, 2015
- Cannabinoids in disguise: Δ9-tetrahydrocannabinol-like effects of tetramethylcyclopropyl ketone indoles. Neuropharmacology December 2013
- Phytocannabinoids beyond the Cannabis plant - do they exist? British Journal of Pharmacology June 1, 2010
and 1 more in the library