ETHNOPHARMACOLOGICAL RELEVANCE AND AIMS: The traditional use of the Hallucinogenic sage, Salvia divinorum has been of ethnopharmalogical interest for some time. This plant, endemic to Oaxaca Mexico and traditionally used by the Mazatec, is now utilized worldwide for its psychoactive effects. This use demonstrates a novel use pattern which is distinctly different from Mazatec use. This study...
The effects of salvinorin A (Salvia divinorum principal ingredient), a potent κ-opioid natural hallucinogen, on learning and memory were investigated. Wistar rats were tested in the 8-arm radial maze, for object recognition and passive avoidance tasks for spatial, episodic, and aversive memory. Attention was assessed using a latent inhibition task. Salvinorin A (80-640 μg/kg subcutaneous [sc])...
Previous structure-activity relationship studies of salvinorin A have shown that modification of the acetate functionality off the C-2 position to a methoxy methyl or methoxy ethyl ether moiety leads to increased potency at KOP receptors. However, the reason for this increase remains unclear. Here we report our efforts towards the synthesis and evaluation of C-2 constrained analogs of...
Salvia divinorum is a hallucinogenic plant with ethnopharmacological and recreational uses. It differs from classic serotonergic hallucinogens such as LSD and psilocin in both phenomenology and potent agonist activity of the active component salvinorin A at κ-opioid receptors. Awareness of S. divinorum has grown recently, with both an increase in its public representation and concern over its...
Salvia, a hallucinogenic plant legally available in most of the United States, has become a widely discussed drug in the media. The extant research on Salvia use relies on non-probability samples and studies of college students. There is a clear need for research that identifies the correlates of Salvia use using data from a large sample that is nationally representative. The current study...
Repeated exposure to drugs of abuse and stress increase dynorphin, a κ opioid receptor (KOR) ligand, in the nucleus accumbens (NAc). Acute KOR activation produces dysphoria that might contribute to addictive behavior. How repeated KOR activation modulates reward circuitry is not understood. We used intracranial self-stimulation (ICSS), a method that provides a behavioral index of reward...
The hallucinogenic compound, salvinorin A, is a potent κ-opioid receptor (KOR) agonist. However, other target(s) than the KOR, such as the cannabinoid CB1 receptor, have been proposed to explain its multiple pharmacological actions. Here, we have evaluated the effect of salvinorin A in lipopolysaccharide (LPS)-stimulated macrophages as well as in models of inflammation in vivo. Salvinorin A...
Salvia divinorum Epl. & Játiva-M. (Lamiaceae) is a potent hallucinogenic plant that is classified within Salvia subgenus Calosphace, section Dusenostachys, and hypothesized to be an interspecific hybrid. It is of ethnobotanical significance due to its employment in traditional healing ceremonies by the Mazatecs of Oaxaca, Mexico, and due to its unique pharmacology-a highly selective,...
Salvinorin A, the main active component of Salvia divinorum, is a potent and selective κ opioid receptor agonist. Synthetic derivatives of this substance may be useful in the development of medicinal treatments for pain, mood disorders, and drug dependence. Such developments require extensive preclinical screening of these compounds. The drug discrimination assay is a valuable method for...
Salvia divinorum is a psychoactive herb and an increasingly popular recreational drug used by young people in our country and abroad. Much of its increased popularity stems from its easy accessibility and affordability; its effects produce an intense and potent "high" and concomitant disorientation and hallucinations. The risks associated with Salvia are poorly defined due to a lack of...
Salvia divinorum, a hallucinogenic herb, has in recent years become popular among teenagers and young adults. Salvia is presently marketed as a "legal" alternative to other drugs of abuse, but little is known about the clinical toxicity of this substance. The purpose of this study is to describe the clinical and demographic features of this emerging substance of recreational abuse using data...
Salvia divinorum is a perennial sage native to Oaxaca, Mexico, that has been used traditionally in divination rituals and as a treatment for the "semimagical" disease panzón de borrego. Because of the intense "out-of-body" experiences reported after inhalation of the pyrolized smoke, S. divinorum has been gaining popularity as a recreational hallucinogen, and the United States and several other...
Abstract: Access to enantiopure synthetic platforms that can generate key intermediates for salvinorin A analogues through diastereoselective Diels–Alder cycloaddition between an enantiopure sulfinylquinone and semicyclic dienes is described.
Salvinorin A is a potent, selective nonnitrogenous kappa opioid agonist and the known psychoactive constituent of Salvia divinorum, a member of the mint family that has been used for centuries by Mazatec shamans of Mexico for divination and spiritual healing. S. divinorum has over the last several years gained increased popularity as a recreational drug. This is a double-blind, placebo...
As part of our continuing efforts toward more fully understanding the structure-activity relationships of the neoclerodane diterpene salvinorin A, we report the synthesis and biological characterization of unique cycloadducts through [4+2] Diels-Alder cycloaddition. Microwave-assisted methods were developed and successfully employed, aiding in functionalizing the chemically sensitive salvinorin...
Introduction Salvinorin A (1a), isolated from the hallucinogenic sage Salvia divinorum,[1] is a potent and selective κ opioid receptor (KOR) agonist.[2] Because it is the rst known non-nitrogenous compound to have biologically signicant actions at mammalian opioid receptors, 1a enables new approaches to studies of endogenous opioid receptor systems. KOR ligands, in particular, have attracted...
Salvinorin A (SA) is a highly selective kappa opioid receptor agonist and the putative psychoactive compound in Salvia divinorum (SD), an increasingly abused hallucinogenic plant. The objectives of this study were to characterize the physiological and subjective effects of SA versus placebo and measure drug and metabolite levels. Sublingual SA doses up to 4 mg were administered in dimethyl...
CONTEXT: Media and scientific reports have indicated an increase in recreational use of Salvia divinorum. Epidemiological data are lacking on the trends, prevalence, and correlates of S. divinorum use in large representative samples, as well as the extent of substance use and mental health problems among S. divinorum users. OBJECTIVE: To examine the national trend in prevalence of S. divinorum...
The synthesis and in vitro evaluation of a new series of salvinorin A analogues substituted at the C(2) position with natural amino acids is reported. Compound 12, containing Val, displayed high affinity and full agonist activity at the kappa-opioid receptor. Analogues with bulky and/or aromatic residues were inactive, showing the importance of size and electronegativity of C(2)-substituents...
Gli allucinogeni sono sostanze psicoattive capaci di causare ‘sostanziali e transitorie modificazioni della percezione, del pensiero e dell’umore’. Possono essere classificate in base al loro meccanismo d‘azione oppure in base alla loro struttura chimica.