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Self-treatment of opioid withdrawal using kratom (Mitragynia speciosa korth).
The predominant alkaloid of kratom, mitragynine, binds mu- and kappa-opioid receptors, but has additional receptor affinities that might augment its effectiveness at mitigating opioid withdrawal.
Mitragyna speciosa, a psychoactive tree from Southeast Asia with opioid activity.
Leaves from this tree have been traditionally been used for both their stimulant properties as well as an opium substitute and general structure-activity relationships (SARs) with respect to opioid activity.
Antinociceptive profile of salvinorin A, a structurally unique kappa opioid receptor agonist
The hallucinogen derived from Salvia divinorum, salvinorin A, has κ-opioid agonist discriminative stimulus effects in rats
Toward a structure-based model of salvinorin A recognition of the kappa-opioid receptor.
- Brian E Kane, C. McCurdy, D. Ferguson
- Biology, ChemistryJournal of medicinal chemistry
- 23 February 2008
A binding site model is proposed that aligns salvinorin A vertically within a pocket spanning transmembrane II and VII, with the 2' substituent directed toward the extracellular domains, which explains the role that hydrophobic contacts play in binding this lipophilic ligand and gives insight into the structural basis to the mu-opioid receptor selectivity of 2'-benzoyl salvin orin (herkinorin).
Opioid receptors and legal highs: Salvia divinorum and Kratom
Both Kratom alkaloids are reported to activate supraspinal mu- and delta- opioid receptors, explaining their use by chronic narcotics users to ameliorate opioid withdrawal symptoms.
A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity
The potential to use PROTAC technology to reduce on-target drug toxicities and rescue the therapeutic potential of previously undruggable targets is demonstrated and DT2216 may be developed as a safe first-in-class anticancer agent targeting BCL-XL.
Sigma Receptor Agonists: Receptor Binding and Effects on Mesolimbic Dopamine Neurotransmission Assessed by Microdialysis
Mephedrone (4-methylmethcathinone), a principal constituent of psychoactive bath salts, produces behavioral sensitization in rats.
A unique binding epitope for salvinorin A, a non‐nitrogenous kappa opioid receptor agonist
The results indicate that salvinorin A recognizes a cluster of residues in TM II and VII, including Q115, Y119, Y312, Y313, and Y320, which indicate that the ligand spans residues that are spaced one to two turns down the face of the helices within the receptor cavity.