Matches in SemOpenAlex for { <https://semopenalex.org/work/W4236076890> ?p ?o ?g. }
Showing items 1 to 68 of
68
with 100 items per page.
- W4236076890 abstract "<p>The seeds of the akuamma tree (<i>Picralima nitida</i>) have been used as a traditional treatment for pain and fever. Previous studies have attributed these effects to a series of indole alkaloids found within the seed extracts; however, these pharmacological studies were significantly limited in scope. Herein, an isolation protocol employing pH-zone-refining countercurrent chromatography is developed to provide six of the akuamma alkaloids in high purity and quantities sufficient for more extensive biological evaluation. Five of these alkaloids, akuammine, pseudo-akuammigine, picraline, akuammicine, and akuammiline, were evaluated against a panel of >40 central nervous system receptors to identify that their primary targets are the opioid receptors. Detailed<i> in vitro </i>investigations revealed one alkaloid as a potent kappa opioid receptor agonist and three alkaloids with micromolar activity at the mu opioid receptor. The mu opioid receptor agonists were further evaluated for analgesic properties but demonstrated limited efficacy in assays of thermal nociception. These findings contradict previous reports of the antinociceptive properties of the akuamma alkaloids and the traditional use of akuamma seeds as analgesics. Nevertheless, their opioid preferring activity does suggest the akuamma alkaloids provide distinct scaffolds from which to develop novel opioids with unique pharmacologically properties and therapeutic utility. <b><br></b></p>" @default.
- W4236076890 created "2022-05-12" @default.
- W4236076890 creator A5018023844 @default.
- W4236076890 creator A5022930456 @default.
- W4236076890 creator A5023315844 @default.
- W4236076890 creator A5029532424 @default.
- W4236076890 creator A5042216362 @default.
- W4236076890 creator A5051204828 @default.
- W4236076890 creator A5073407478 @default.
- W4236076890 creator A5076748220 @default.
- W4236076890 date "2020-09-28" @default.
- W4236076890 modified "2023-09-29" @default.
- W4236076890 title "Isolation and Pharmacological Characterization of Six Opioidergic Picralima nitida Alkaloids" @default.
- W4236076890 doi "https://doi.org/10.26434/chemrxiv.13007804" @default.
- W4236076890 hasPublicationYear "2020" @default.
- W4236076890 type Work @default.
- W4236076890 citedByCount "0" @default.
- W4236076890 crossrefType "posted-content" @default.
- W4236076890 hasAuthorship W4236076890A5018023844 @default.
- W4236076890 hasAuthorship W4236076890A5022930456 @default.
- W4236076890 hasAuthorship W4236076890A5023315844 @default.
- W4236076890 hasAuthorship W4236076890A5029532424 @default.
- W4236076890 hasAuthorship W4236076890A5042216362 @default.
- W4236076890 hasAuthorship W4236076890A5051204828 @default.
- W4236076890 hasAuthorship W4236076890A5073407478 @default.
- W4236076890 hasAuthorship W4236076890A5076748220 @default.
- W4236076890 hasBestOaLocation W42360768901 @default.
- W4236076890 hasConcept C170493617 @default.
- W4236076890 hasConcept C185592680 @default.
- W4236076890 hasConcept C2777667214 @default.
- W4236076890 hasConcept C2778750930 @default.
- W4236076890 hasConcept C2778938600 @default.
- W4236076890 hasConcept C2779004600 @default.
- W4236076890 hasConcept C2780820201 @default.
- W4236076890 hasConcept C2781063702 @default.
- W4236076890 hasConcept C55493867 @default.
- W4236076890 hasConcept C71240020 @default.
- W4236076890 hasConcept C71924100 @default.
- W4236076890 hasConcept C98274493 @default.
- W4236076890 hasConceptScore W4236076890C170493617 @default.
- W4236076890 hasConceptScore W4236076890C185592680 @default.
- W4236076890 hasConceptScore W4236076890C2777667214 @default.
- W4236076890 hasConceptScore W4236076890C2778750930 @default.
- W4236076890 hasConceptScore W4236076890C2778938600 @default.
- W4236076890 hasConceptScore W4236076890C2779004600 @default.
- W4236076890 hasConceptScore W4236076890C2780820201 @default.
- W4236076890 hasConceptScore W4236076890C2781063702 @default.
- W4236076890 hasConceptScore W4236076890C55493867 @default.
- W4236076890 hasConceptScore W4236076890C71240020 @default.
- W4236076890 hasConceptScore W4236076890C71924100 @default.
- W4236076890 hasConceptScore W4236076890C98274493 @default.
- W4236076890 hasLocation W42360768901 @default.
- W4236076890 hasLocation W42360768902 @default.
- W4236076890 hasOpenAccess W4236076890 @default.
- W4236076890 hasPrimaryLocation W42360768901 @default.
- W4236076890 hasRelatedWork W12810935 @default.
- W4236076890 hasRelatedWork W13718353 @default.
- W4236076890 hasRelatedWork W21365089 @default.
- W4236076890 hasRelatedWork W22405011 @default.
- W4236076890 hasRelatedWork W24754299 @default.
- W4236076890 hasRelatedWork W30128251 @default.
- W4236076890 hasRelatedWork W3346678 @default.
- W4236076890 hasRelatedWork W6812723 @default.
- W4236076890 hasRelatedWork W9919773 @default.
- W4236076890 hasRelatedWork W21761194 @default.
- W4236076890 isParatext "false" @default.
- W4236076890 isRetracted "false" @default.
- W4236076890 workType "article" @default.