ACS Central ScienceAugust 23, 2023Sarah J Hill, Nathan Dao, Vuong Q. Dang et al.
The salvinorins serve as templates for next generation analgesics, antipruritics, and dissociative hallucinogens via selective and potent agonism of the kappa-opioid receptor (KOR). In contrast to most opioids, the salvinorins lack basic amines and bind with high affinity and selectivity via complex polyoxygenated scaffolds that have frustrated deep-seated modification by synthesis. Here we...
Natural products have served as rich sources of therapeutics dating back to the earliest human civilizations in the form of traditional medicines and more recently as single molecule therapies for a range of diseases. Their diverse biological activities stem from their often complex structures, which can endow natural products with desirable properties relative to synthetic molecules found in...
Kappa opioid receptor (KOR) agonists have preclinical antipsychostimulant effects; however, adverse side effects have limited their therapeutic development. In this preclinical study, conducted in Sprague Dawley rats, B6-SJL mice, and non-human primates (NHPs), we evaluated the G-protein-biased analogue of salvinorin A (SalA), 16-bromo salvinorin A (16-BrSalA), for its anticocaine effects, side...
FitoterapiaJune 1, 2023Caroline V. L. Moreira, Ana Luiza G Faria, Daiany P B Silva et al.2 citations
Previous studies have attributed the prominent analgesic, hallucinogenic, sedative, and anxiolytic properties of Salvia divinorum to Salvinorin A. However, the overall pharmacological profile of this isolate limits its clinical applications. To address these limitations, our study evaluates the C(22)-fused-heteroaromatic analogue of salvinorin A [2-O-salvinorin B benzofuran-2-carboxylate]...
Deviant BehaviorJanuary 12, 2023Jeff Yaremko, Kevin Walby1 citation
ABSTRACT Smoking a potent concentration of salvia divinorum (hereafter salvia) has the capacity to dissolve one’s ego and sense of self. Due to the catatonic state a strong dose of salvia produces, the substance has been considered alarming by claims-makers including politicians, media officials, police, and citizen groups. This paper examines news media accounts of salvia use in Canada and...
The natural product Salvinorin A (SalA) was the first nitrogen-lacking agonist discovered for the opioid receptors and exhibits high selectivity for the kappa opioid receptor (KOR) turning SalA into a promising analgesic to overcome the current opioid crisis. Since SalA’s suffers from poor pharmacokinetic properties, particularly the absence of gastrointestinal bioavailability, fast metabolic...
ChemistryOpenOctober 26, 2022Marc Halang, Martin E. Maier
Abstract The generation of the quaternary stereocenter at the C9 position of salvinorin A precursors by the Claisen rearrangement was investigated. The required allyl alcohol was prepared from a Wieland‐Miescher ketone using a known γ‐hydroxylation, reduction of the enone double bond, cyanohydrin formation, and elimination, yielding an unsaturated nitrile. A two‐step reduction led to the...
It's well known that exotoxicosis can originate various psychiatric clinical pictures. The psychic impact of "classic" substances of abuse is well known and easily detectable with the usual methods of examination. In the last years new psychoactive substances (NPS) are spreading worldwide, determining not easily recognizable situations, with a significant clinical and organizational impact on...
Son múltiples los motivos para afirmar que la Salvia divinorum es una de las plantas enteogénicas más singulares que existen en el planeta. Endémica de la sierra de Oaxaca, México, ha sido utilizada tradicionalmente por diversas culturas indígenas en complejos rituales mágicos, adivinatorios y curativos. En las últimas tres décadas, emergió en el mercado mexicano y mundial en la forma de...
While the hallucinogenic plant Salvia divinorum has been safely consumed by humans for centuries for religious or recreational purposes without long-term side effects, its active component, salvinorin A, and molecular mechanism of action were not known until recently [1]. Notably, salvinorin A is a potent kappa opioid receptor (KOR) agonist that is highly selective for KOR without significant...