Abstract Salvinorin A (SA) is a κ-opioid receptor agonist and atypical dissociative hallucinogen found in Salvia divinorum . Despite the resurgence of hallucinogen studies, the effects of κ-opioid agonists on human brain function are not well-understood. This placebo-controlled, within-subject study used functional magnetic resonance imaging for the first time to explore the effects of inhaled...
In the search for safer, non-addictive analgesics, kappa opioid receptor (KOPr) agonists are a potential target, as unlike mu-opioid analgesics, they do not have abuse potential. Salvinorin A (SalA) is a potent and selective KOPr agonist, however, clinical utility is limited by the short duration of action and aversive side effects. Biasing KOPr signaling toward G-protein activation has been...
Previous structure-activity relationship (SAR) studies identified the first centrally-acting, non-nitrogenous μ opioid receptor (MOR) agonist, kurkinorin (1), derived from salvinorin A. In an effort to further probe the physiological effects induced upon activation of MORs with this non-morphine scaffold, a variety of analogues were synthesized and evaluated in vitro for their ability to...
MoleculesMarch 7, 2020Katarzyna Socała, Urszula Doboszewska, Piotr Wlaź
The κ-opioid receptor has recently gained attention as a new molecular target in the treatment of many psychiatric and neurological disorders including epilepsy. Salvinorin A is a potent plant-derived hallucinogen that acts as a highly selective κ-opioid receptor agonist. It has unique structure and pharmacological properties, but its influence on seizure susceptibility has not been studied so...
ETHNOPHARMACOLOGICAL RELEVANCE Salvia divinorum Epling & Játiva is a Mexican plant used not only in rituals but also in traditional medicine for pain relief. One of the most known bioactive compounds is salvinorin A, which acts centrally in kappa-type opioid receptors. AIM OF THE STUDY Despite its traditional use as a medicinal plant, there is not enough scientific investigation to reinforce...
The study goal is to document the prevalence of salvia use among patients admitted for detoxification of other illicit drug use and to determine its effect. This cross-sectional study included 47 heavy drug users who were admitted for detoxification of other illicit drug abuse at a psychiatric hospital in Lebanon. The prevalence of salvia use was 66%. The salvia effect started and dissipated...
The FASEB JournalApril 1, 2019Aboozar Ali, Cynthia Franklin, Yolanda Rangel et al.
Intracerebroventricular (ICV) injection of the kappa opioid agonists produces a marked diuresis in rats via inhibition of vasopressin secretion. Salvinorin A (SalA) is a plant‐derived high affinity agonist for the kappa opioid receptor (KOR). Previous studies have proposed that SalA has similar potency and efficacy as other synthetic kappa agonists in mediating the CNS effects of KOR...
Introduction: Drug addiction is a chronic and relapsing disorder that has widespread socioeconomic and health consequences. Globally, there are over 29.5 million people who are drug dependent, and New Zealand has one of the highest rates of drug use rates in the developed world. Currently, there are no Food and Drug Administration (FDA) approved pharmacotherapies that target psychostimulant...
Over the years, pain has contributed to low life quality, poor health, and economic loss. Opioids are very effective analgesic drugs for treating mild, moderate, or severe pain. Therapeutic application of opioids has been limited by short and long-term side effects. These side effects and opioid-overuse crisis has intensified interest in the search for new molecular targets and drugs. The...
Modern rituals based on the use of shamanic plants are becoming more popular in the European countries and in the USA since the last decades. Salvia divinorum (SD) is such a plant, for ages and still used by the Mazatec shamans for initiation purposes. SD contains a great number of diterpenes of which Salvinorin A is quite remarkable, as to date it is the strongest psychedelic plant compound we...