Drug Testing and Analysis
June 6, 2016
S. Brandt, P. Kavanagh, F. Westphal et al.
62 citations
Two new psychoactive substances, AL-LAD and LSZ, which are analogs of LSD, were analytically characterized using multiple techniques including NMR, mass spectrometry, and infrared analysis. In male mice, both compounds produced LSD-like behavioral responses in a head-twitch assay, with dose-dependent effects peaking at 200 µg/kg. LSZ was equipotent to LSD (ED50 = 114.2 nmol/kg vs. 132.8 nmol/kg), while AL-LAD was slightly less potent (ED50 = 174.9 nmol/kg). The direct translation of these potency comparisons to humans requires further study. Providing chemical and pharmacological data on emerging substances aids research communities focused on substance use and forensic identification.
Drug Testing and Analysis
May 10, 2017
S. Brandt, P. Kavanagh, F. Westphal et al.
44 citations
Two new lysergamides, ETH-LAD and 1P-ETH-LAD, were characterized using multiple analytical techniques including GC-MS, mass spectrometry, infrared analysis, HPLC, and NMR. 1P-ETH-LAD had not previously been described in scientific literature. When incubated with human serum at 37°C, 1P-ETH-LAD converted to ETH-LAD over time, suggesting it may act as a pro-drug. 1P-ETH-LAD remained detectable in serum after 24 hours. This work provides analytical data for clinicians and toxicologists who may encounter these substances on the new psychoactive substances market.
Biochemical Pharmacology
April 13, 2020
A. Jensen, A. Halberstadt, Emil Märcher-Rørsted et al.
25 citations
Modifications to specific positions on the 25CN-NBOH molecule, a highly selective 5-HT2A receptor agonist, can retain or reduce its activity. Six new analogs were tested; 3′-methyl and fused-ring variants kept high 5-HT2A receptor activity, while 3′-methoxy and 3′-ethyl versions lost binding and potency. All six analogs showed only partial agonism or antagonism. In mice, 25CN-NBOH and a close analog triggered head-twitch responses (a hallmark of 5-HT2A activation) and reduced marble-burying behavior, suggesting potential benefits for cognitive rigidity disorders. A tritium-labeled version of 25CN-NBOH showed high binding affinity and selectivity for 5-HT2A receptors in rat brain tissue, providing a new tool for future receptor studies.
Psychopharmacology
March 1, 2019
A. Halberstadt, S. Brandt, D. Walther et al.
A class of designer drugs derived from 2-aminoindan (2-AI) interacts with monoamine transporters in ways that predict distinct psychoactive effects. 2-AI itself acts as a selective substrate for norepinephrine and dopamine transporters, suggesting (+)-amphetamine-like effects and abuse potential. Adding ring substitutions increases potency at the serotonin transporter while reducing potency at dopamine and norepinephrine transporters. Among the derivatives, MMAI is highly selective for the serotonin transporter, with 100-fold lower potency at norepinephrine and dopamine transporters, while MDAI and 5-MeO-AI show moderate serotonin selectivity. The compounds also bind to α2-adrenoceptor subtypes, with 2-AI having highest affinity for α2C receptors (Ki = 41 nM). Ring-substituted derivatives may produce MDMA-like effects with less abuse liability.