ANT-429 / Antyra - LARVOL DELTA

Pharmacological Characterization of Substituted Nitazenes at Opioid Receptors (CPDD 2025) - "Financial Support : US DOJ-DEA [Grant D-22-OD-0001] PVARF [Grant 429999] Aims: Nitazenes (2-benzylbenzimidazole opioids) were originally developed in the 1950s as synthetic opioid analgesics but were never approved for therapeutic use... In this group of nitazenes, approximately half were higher or comparable affinity and potency relative to fentanyl... Nitazenes are appearing in drug samples seized by the DEA and have been 1 repeatedly identified in fatal and non-fatal intoxications around the world. The affinity, potency, and efficacy values reported herein for the nitazenes evaluated highlight key structure activity relationships, including newly described motifs that reduce selectivity for MOR versus KOR, conferring a more morphine-like pattern of binding and function at opioid receptors."

Pain

Pharmacology of Newer Synthetic Cannabinoids at the CB1 Receptor (CPDD 2024) - "Financial Support : Study funding was provided by the US Department of Justice Drug Enforcement Administration [Grant D-23-OD-0001] (A.J., A.I.A.), Department of Veterans Affairs Career Scientist Program [Grant 14S-RCS-006] (A.J.), the Oregon Health & Science University Physician-Scientist Award [Grant 60678300] (A.I.A.), and the Portland Veterans Affairs Research Foundation [Grant 429999] (A.I.A.)... Many new SCs, which are often variants of PINACA, PICA, and BUTINACA core structures, have high affinities and potencies at the CB1 receptor and present new potential for abuse and safety concerns."

Pharmacological Characterization of Substituted Nitazenes at Opioid Receptors (CPDD 2024) - "Financial Support : Study funding was provided by the US Department of Justice Drug Enforcement Administration [Grant D-23-OD-0001] (A.J., A.I.A.), Department of Veterans Affairs Career Scientist Program [Grant 14S-RCS-006] (A.J.), the Oregon Health & Science University Physician-Scientist Award [Grant 60678300] (A.I.A.), and the Portland Veterans Affairs Research Foundation [Grant 429999] (A.I.A.)...Dunnett’s multiple comparisons test compared test compounds to fentanyl... Many substituted nitazenes are very high affinity/high potency MOR agonists which suggests high toxicity and overdose at low doses."

Addiction (Opioid and Alcohol)