2-bromo-D-lysergic acid diethylamide (NYPRG-101) / Ceruvia Lifesci, Yale University - LARVOL DELTA

A highly sensitive UHPLC-MS/MS method for determining 15 designer LSD analogs in biological samples with application to stability studies. (PubMed, Analyst) - "In the presented paper, an UHPLC-QqQ-MS/MS method was developed for trace determination (fg mL-1) of LSD, its designer analogs (ALD-52, AL-LAD, LAMPA, LSM-775, LSZ, MiPLA, 1B-LSD, 1cP-LSD, 1cP-MiPLA, 1P-LSD, 1P-MiPLA, 1V-LSD and 2-Bromo-LSD) and its metabolite (2-oxo-3-OH-LSD) with simultaneous separation of structural isomers...The presented method is the most sensitive to date for analyzing designer LSD analogs in biological samples, with potential for routine clinical and forensic use, enhancing detection of emerging illicit compounds. By examining the mass spectra (QTOF-MS/MS) obtained in this study and reviewing the literature on analytical characterization of LSD analogs, we proposed fragmentation patterns to aid in future identification of new designer LSD analogs (NPS)."

Journal

2-Bromo-LSD: A Non-Hallucinogenic LSD analogue with therapeutic potential in mood disorders (Neuroscience 2023) - "This symposium will discuss the drugs' receptor targets, downstream pathways, and implicated brain regions. These data will help in the fields of clinical application and targeted drug discovery."

CNS Disorders • Mood Disorders • Psychiatry

A non-hallucinogenic LSD analogue with therapeutic potential in mood disorders (CAN-ACN 2023) - "2-Bromo-LSD (2-Br-LSD/BETR-001) is an LSD derivative with 5-HT2A partial agonist activity that lacks hallucinogenic effects...Our findings demonstrate that 2-Br-LSD induces cortical plasticity in vitro and in vivo, promotes active stress-coping behaviours, and reveres the behavioural effects of chronic stress. These results show that 2-Br-LSD possesses therapeutic potential and represents a promising alternative to classic psychedelics in treating depression."

CNS Disorders • Depression • Mental Retardation • Mood Disorders • Psychiatry

A Non-Hallucinogenic LSD Analogue With Therapeutic Potential in Mood Disorders (SOBP 2023) - "2-Bromo-LSD (2-Br-LSD/BETR-001) is an LSD derivative with 5-HT2A partial agonist activity that lacks hallucinogenic effects...Conclusions Our findings demonstrate that 2-Br-LSD induces cortical plasticity in vitro and in vivo, promotes active stress-coping behaviours, and reveres the behavioural effects of chronic stress. These results show that 2-Br-LSD possesses therapeutic potential and represents a promising alternative to classic psychedelics in treating depression."

CNS Disorders • Depression • Mental Retardation • Mood Disorders • Psychiatry

A non-hallucinogenic LSD analog with therapeutic potential for mood disorders. (PubMed, Cell Rep) - "Here we profiled the non-hallucinogenic lysergic acid diethylamide (LSD) analog 2-bromo-LSD (2-Br-LSD) at more than 33 aminergic G protein-coupled receptors (GPCRs). 2-Br-LSD also reverses the behavioral effects of chronic stress. Overall, 2-Br-LSD has an improved pharmacological profile compared with LSD and may have profound therapeutic value for mood disorders and other indications."

Journal • CNS Disorders • Depression • Mood Disorders • Psychiatry

Ceruvia Lifesciences Announces First Participant Dosed in BOL-148 Phase 1 Clinical Trial (PRNewswire) - “Ceruvia Lifesciences…announced the first participant has been dosed in their Phase 1 clinical trial of NYPRG-101 (2-bromo-d-lysergic acid diethylamide) in healthy adult participants….‘We believe that NYPRG-101 offers great promise to provide meaningful relief from the disability and psychosocial burdens that impact the lives of several patient populations, including those suffering from migraine and cluster headaches’….Ceruvia's Phase 1 clinical trial is a single ascending dose study to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of NYPRG-101 in healthy adult participants. Up to 40 participants will be enrolled and randomized into ascending dose cohorts, each receiving a single dose of NYPRG-101.”

Trial status • CNS Disorders • Migraine • Psychiatry

A Non-Hallucinogenic LSD Analog With Therapeutic Potential for Mood Disorders (ACNP 2022) - "2-Bromo-LSD (2-Br-LSD, BETR-001) is an LSD derivative with 5-HT2A partial agonist activity that lacks hallucinogenic effects and has been safely used for cluster headache treatment...The maximal effect was achieved with the 1 uM dose comparable to the 10 uM ketamine treatment... Our findings demonstrate that 2-Br-LSD induces structural plasticity in cortical neurons in vitro and in vivo, promotes active stress-coping behaviours and reverses the behavioural effects of CVS. These results show that 2-Br-LSD may possess a therapeutic potential and represents a promising alternative to psychedelics in treating MDD."

CNS Disorders • Depression • Major Depressive Disorder • Mental Retardation • Mood Disorders • Pain • Psychiatry

Investigation of the Pharmacological Properties of 2-Br-LSD, a Non-Hallucinogenic LSD Analog (ACNP 2022) - "Similar to LSD, the closely related derivative 2-bromo-LSD (2-Br-LSD, TD-0418A) is also being investigated as a potential treatment for depression and headache. Overall, 2-Br-LSD has an improved pharmacological profile compared to LSD. 2-Br-LSD appears to act as a non-hallucinogenic 5-HT2A agonist, similar to the isolysergic acid derivative lisuride. Our studies provide insight into the non-hallucinogenic activity of 2-Br-LSD, which is probably a consequence of its weak partial agonist activity at the 5-HT2A receptor."

CNS Disorders • Depression • Mental Retardation • Mood Disorders • Pain • Psychiatry • Substance Abuse • ARRB1

Ceruvia Lifesciences Submits FDA Investigational New Drug Application for NYPRG-101 Migraine Prevention Program (PRNewswire) - "Ceruvia Lifesciences...announced the submission of an IND application to begin a Phase 1, single center, randomized, double blind, placebo controlled, single ascending dose study to assess the safety, tolerability, pharmacokinetics and pharmacodynamics of NYPRG-101 (2-bromo-D-lysergic acid diethylamide) in healthy adult participants....This Phase 1 single ascending dose (SAD) trial, to be held at a single clinical research site in the United States, will evaluate the safety, tolerability, pharmacokinetics and effects on neurocognitive functioning of healthy adult participants."

IND • New P1 trial • CNS Disorders • Migraine • Pain