Salvinorin A Does Not Affect Seizure Threshold in Mice [PDF]
The κ-opioid receptor has recently gained attention as a new molecular target in the treatment of many psychiatric and neurological disorders including epilepsy.
Katarzyna Socała +2 more
doaj +4 more sources
Formal Total Synthesis of Salvinorin A [PDF]
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 ...
Marc Halang, Prof. Dr. Martin E. Maier
doaj +3 more sources
A Route to Potent, Selective, and Biased Salvinorin Chemical Space [PDF]
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 ...
Sarah J. Hill +5 more
doaj +5 more sources
Autoxidation of Salvinorin A under Basic Conditions [PDF]
[reaction: see text] Treatment of salvinorin A (1a) with KOH in MeOH gave the enedione 3, for which the dienone structure 7 was recently proposed. Also isolated, after methylation, were the secotriesters 4a-c. A mechanism for this unusual series of autoxidations is proposed.
Thomas A, Munro +4 more
openaire +3 more sources
The Salvinorin Analogue, Ethoxymethyl Ether Salvinorin B, Promotes Remyelination in Preclinical Models of Multiple Sclerosis [PDF]
Multiple sclerosis is a neurodegenerative disease associated with demyelination and neuroinflammation in the central nervous system. There is an urgent need to develop remyelinating therapies to better treat multiple sclerosis and other demyelinating ...
Kelly F. Paton +16 more
doaj +4 more sources
8-epi-Salvinorin B: crystal structure and affinity at the κ opioid receptor
There have been many reports of epimerization of salvinorins at C-8 under basic conditions, but little evidence has been presented to establish the structure of these compounds.
Thomas A. Munro +7 more
doaj +2 more sources
Salvinorin B methoxymethyl ether [PDF]
The title compound [MOM-SalB; systematic name: methyl (2S,4aR,6aR,7R,9S,10aS,10bR)-2-(3-fur-yl)-9-meth-oxy-meth-oxy-6a,10b-dimethyl-4,10-dioxo-2,4a,5,6,7,8,9,10a-octa-hydro-1H-benzo[f]isochromene-7-carboxyl-ate], C(23)H(30)O(8), is a deriv-ative of the κ-opioid salvinorin A with enhanced potency, selectivity, and duration of action.
Munro, Thomas A. +2 more
openaire +6 more sources
Unusual hemiacetal structure derived from Salvinorin A [PDF]
The salvinorin A analog dimethyl (2R,3aR,4R,6aR,7R,9S,9aS,9bS)-2-(3-furyl)-9,9a-dihydroxy-3a,6a-dimethyldodecahydrobenzo[de]chromene-4,7-dicarboxylate, C22H30O8, has a relatively simple spatial arrangement in which molecules are linked into layers by two
Paulo Carvalho +3 more
doaj +3 more sources
Virtual Screening of Phytochemicals From Medicinal Plants as Promising PDE5 Inhibitors Against Erectile Dysfunction. [PDF]
Phytochemicals from Algerian medicinal plants were virtually screened as potential phosphodiesterase‐5 (PDE5) inhibitors for erectile dysfunction therapy. Drug‐likeness and toxicity analyses identified catechin, ellagic acid, and rosmarinic acid as safe, bioavailable candidates.
Boudou F +7 more
europepmc +2 more sources
Possible Involvement of Hallucinogenic Effects in the Aversive Effects Induced by Kappa-Opioid and 5-HT<sub>2A</sub> <sub>/2C</sub> Receptor Agonists in Mice. [PDF]
This study developed a simple way to test new psychoactive substances (NPS) in mice. Two drugs, U50,488H and DOI caused aversive and abnormal behaviors in mice, likely linked to their hallucinogenic properties. These results suggest such behavioral tests could help quickly identify and regulate harmful psychoactive drugs. ABSTRACT Aim The regulation of
Kato H +5 more
europepmc +2 more sources

