Canna~Fangled Abstracts

The Chemistry and Pharmacology of Synthetic Cannabinoid Receptor Agonist New Psychoactive Substances: Evolution.

By August 14, 2018No Comments
2018 Aug 14. doi: 10.1007/164_2018_144.
[Epub ahead of print]

Abstract

Synthetic cannabinoid receptor agonists (SCRAs) are the largest and most structurally diverse class of new psychoactive substances (NPS). Although the earliest SCRA NPS were simply repurposed from historical academic manuscripts or pharmaceutical patents describing cannabinoid ligands, recent examples bear hallmarks of rational design. SCRA NPS manufacturers have applied traditional medicinal chemistry strategies (such as molecular hybridization, bioisosteric replacement, and scaffold hopping) to existing cannabinoid templates in order to generate new molecules that circumvent structure-based legislation. Most SCRAs potently activate cannabinoid type 1 and type 2 receptors (CB1 and CB2, respectively), with the former contributing to the psychoactivity of these substances. SCRAs are generally more toxic than the Δ9-tetrahydrocannabinol (Δ9-THC) found in cannabis, and this may be due to ligand bias, metabolism, or off-target activity. This chapter will chart the evolution of recently identified SCRA NPS chemotypes, as well as their putative manufacturing by-products and thermolytic degradants, and describe structure-activity relationships within each class.

KEYWORDS:

AB-CHMINACA; AB-FUBINACA; AB-PINACA; AMB-FUBINACA; CP 55,940; Cannabinoid; JWH-018; MDMB-CHMICA; NPS; XLR-11; Δ9-Tetrahydrocannabinol

PMID: 30105473
DOI: 10.1007/164_2018_144

LinkOut – more resources

Full Text Sources

  • Icon for Springer

Miscellaneous