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In Vitro Metabolism of 1‐Benzoyl‐Lysergic Acid Diethylamide (1Bz‐LSD) and Identification of a Deethylated Metabolite (1Bz‐LAE) Using a Synthesized Reference Standard

Yuki Azuma, Akiko Asada, Misa Tanaka, Takahiro Doi

Drug Testing and Analysis February 17, 2026 DOI: 10.1002/dta.70042 (opens in new tab)

Study at a glance

AI-extracted from the abstract
Characteristics In vitro study Peer reviewed
Population Human liver microsomes
Topics LSD
Keywords Metabolism Metabolic pathway Microsome Moiety Biochemistry Analyte Pharmacology Identification biology Active metabolite In vitro toxicology Primary metabolite
Key points The deethylated metabolite 1-benzoyl-lysergic acid ethylamide (1Bz-LAE) was identified as a prolonged-detectable marker for 1Bz-LSD consumption.

Abstract

Lysergic acid diethylamide (LSD) analogs represent an emerging class of new psychoactive substances (NPS). These compounds are often rapidly metabolized, making direct detection of the parent compound in biological samples difficult. Therefore, metabolite detection serves as a critical and effective strategy for the confirmation of consumption. However, the metabolic pathways of these analogs remain largely uncharacterized, and synthesized metabolite standards for definitive identification are mostly unavailable. This study investigated the newly emerged LSD analog, (8R)-1-benzoyl-N,N-diethyl-6-methyl-9,10-didehydroergoline-8-carboxamide (1-benzoyl-LSD, 1Bz-LSD), which features a benzoyl moiety at the N1 position. The objectives were to characterize its metabolic fate and synthesize a targeted metabolite analyte for the confirmation of consumption. In vitro metabolism of 1Bz-LSD was examined using human liver microsomes and analyzed through liquid chromatography-quadrupole time-of-flight mass spectrometry. The parent compound was rapidly metabolized, yielding 15 metabolites, including LSD. Among these, a deethylated metabolite was detectable over a prolonged period, indicating its potential as a targeted analyte. To confirm its structure, this metabolite was chemically synthesized and identified as 1-benzoyl-lysergic acid ethylamide (1Bz-LAE). The synthesis and identification of 1Bz-LAE provide a crucial analytical foundation for the investigations of 1Bz-LSD use, with this metabolite anticipated to function as a valuable marker.

Comparable studies

Other preclinical and animal studies on LSD, most cited first.

Study Year Design Participants
Transcriptome Fingerprints Distinguish Hallucinogenic and Nonhallucinogenic 5-Hydroxytryptamine 2A Receptor Agonist Effects in Mouse Somatosensory Cortex Human embryonic kidney 293 cells stably expressing 5-HT2ARs; wild-type and 5-HT2AR... 2003 Experimental study
Evidence for a central 5‐hydroxytryptamine receptor stimulation by lysergic acid diethylamide Rats 1968 Experimental study
Psychedelics, but Not Ketamine, Produce Persistent Antidepressant-like Effects in a Rodent Experimental System for the Study of Depression Rats 2020 Preclinical study
Lysergic acid diethylamide (LSD) promotes social behavior through mTORC1 in the excitatory neurotransmission Male mice 2021 Multidisciplinary experimental study with in vivo electrophysiology, optogenetics, behavioral paradigms, molecular biology, and conditional knockout mice
A non-hallucinogenic LSD analog with therapeutic potential for mood disorders. Mice and cultured rat cortical neurons 2023 Preclinical study

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