Mesembrin

Generell information

Alkaloid som återfinns i några suckulenter, främst släktet Sceletium.

Mesembrin är en potent serotoninupptagningshämmare och verkar ångestdämpande men har även andra effekter. Växter som innehåller mesembrin har en tradition inom afrikansk herbalism och sedan början av 2000-talet förekommer den hos smartshops och svaga anekdotiska indikationer finns kring drogliknande effekter.

Historically, dried leaves of Sceletium have been used widely by indigenous groups native to southern Africa to elevate the mood and ease anxiety and tension and by shepherds as appetite suppressants during long journeys in dried areas (Gericke and Van Wyk, 1997). Furthermore, extracts prepared from Sceletium have been developed into commercial products for the treatment of central nervous system related disorders including Zembrin® , which is a standardised extract of Sceletium, used by patients for enhancing mood, decreasing anxiety and stress, and improving cognitive function (Dimpfel et al., 2017; Patnala and Kanfer, 2009).
— Makolo (2019)[1]
...The extract gave > 80% inhibition at GABA receptors (non-selective), serotonin (5-HT) transporter, δ2- and μ-opioid receptors, the cholecystokinin-1 receptor, and PDEs 3 and 4 (Harvey et al., 2011).

...Individual alkaloids isolated from Sceletium tortuosum extract were tested against the 5-HT transporter (SERT) and the Ki's for mesembrine, mesembrenone, and mesembrenol were 1.4, 27, and 63 nM, respectively (Harvey et al., 2011). These values are comparable to the marketed SSRI, fluoxetine (Tavoulari et al., 2009)

...The isolated alkaloids mesembrine, mesembrenone, and mesembrenol inhibited PDE4B with IC50s of 7.8, 0.47, and 16 μM, respectively (Harvey et al., 2011).

...The effects of a high mesembrine-content standardized extract, Trimesemine, (3% mesembrine (w/w)) on human astrocytes and mouse hippocampal cells in comparison to the effect elicited by the racemic mixture SSRI, citalopram (Coetzee et al., 2016). The mesembrine extract caused less down-regulation of expression of SERT than citalopram and a greater upregulation of expression of the vesicular monoaminetransporter-2 (VAMT-2) than citalopram. These results were interpreted by the authors as meaning that the primary mechanism of action of this extract is through monoamine release and that serotonin reuptake inhibition is secondary to this release effect.
— Krstenansky (2017)[2]

Den har även visat binda till CB1-receptorerna dock väldigt svagt, ca 1% av THC:s potential.

OBS! Mesembrin kan vara farlig i kombination med MAO-hämmare, alkohol, amfetamin etc. men ensam har den förhållandevis låg överdosrisk.

Arter

  • Sceletium anatomicum
  • Sceletium crassicaule
  • Sceletium expansum
  • Sceletium namaquense
  • Sceletium strictum
  • Sceletium tortuosum

Liknande alkaloider finns även i:

Det finns även spårmängder i vissa arter i släktena Narcissus och Delosperma.

Kemi

Löslig i alkohol, kloroform m.m.

Mesembrin.png
3a-(3,4-Dimethoxyphenyl)octahydro-1-methyl-6H-indol-6-one
Mesembrin (sv), mesembrine (en)
C17H23NO3
205-206 C (HCl)
289.37 g/mol
Läs under extrahering

Externa länkar

  1. Mesembrine: The archetypal psycho-active Sceletium alkaloid (Makolo, 2019)
  2. Mesembrine alkaloids: Review of their occurrence, chemistry, and pharmacology. (Krstenansky, 2017)

Wikipedia

Bild Mesembrine

US Patent US6288104: Pharmaceutical compositions containing mesembrine and related compounds

US Patent Application US20160038551A1: Stabilized Mesembrine Compositions

Sidan ändrades senast 5 augusti 2019 klockan 17.44.
Den här sidan har visats 5 141 gånger.

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