Talk:Kanna: Difference between revisions

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The active compounds in kanna are mesembrine, mesembrenone, mesembrenol, and tortuosamine. It is believed that mesembrine and mesembrenone are responsible for the majority of kanna's effects.

Chemistry of Kanna (Sceletium tortuosum)

Kanna contains a variety of alkaloids, which are responsible for its psychoactive effects. The primary bioactive compounds are mesembrine-type alkaloids, along with other secondary metabolites.

1. Mesembrine Alkaloids (Primary Active Compounds)

Mesembrine – A serotonin reuptake inhibitor (SRI) and mild phosphodiesterase-4 (PDE4) inhibitor. It has a high affinity for the serotonin transporter (SERT), with a Ki value of 1.4 nM, meaning it strongly inhibits serotonin reuptake. It also inhibits PDE4 at a much weaker level (Ki = 7,800 nM) (Smith et al., 1998).

Mesembrenone – Functions as both an SRI and a PDE4 inhibitor, though it is weaker at serotonin reuptake inhibition than mesembrine (Ki = 27 nM for SERT). However, it more potently inhibits PDE4, with a Ki value of 470 nM, suggesting potential anti-inflammatory and cognitive-enhancing effects (Gericke & Viljoen, 2008).

Mesembrenol – A metabolite of mesembrine that is thought to contribute to Kanna’s anxiolytic and mood-enhancing effects. Specific pharmacological data on mesembrenol are limited.

Tortuosamine – A lesser-known alkaloid found in Kanna. Its precise pharmacological properties are not well studied, but it is suspected to play a minor role in Kanna's psychoactive profile (PubChem).

2. Additional Compounds

In addition to mesembrine alkaloids, Kanna also contains:

Flavonoids – Antioxidant compounds with potential neuroprotective and anti-inflammatory properties.

Tannins – Polyphenolic compounds that may affect taste and bioavailability.

Saponins – Plant-based glycosides with potential immune-modulating properties.

[[User:Planlos69|Planlos69]] ([[User talk:Planlos69|talk]]) 09:49, 30 January 2025 (UTC)

==Pharmacology==

The main psychoactive effects of kanna are a result of its action as a potent serotonin reuptake inhibitor ([[SRI]]), a [https://en.wikipedia.org/wiki/Phosphodiesterase-4_inhibitor PDE4 inhibitor], and ~~an upregulator of VMAT2~~ <ref>https://www.sciencedirect.com/science/article/pii/S0378874115302348?via%3Dihub</ref>.

The main psychoactive effects of kanna are a result of its action as a potent serotonin reuptake inhibitor ([[SRI]]), a [https://en.wikipedia.org/wiki/Phosphodiesterase-4_inhibitor PDE4 inhibitor], and a monoamine releasing agent. <ref>https://www.sciencedirect.com/science/article/pii/S0378874115302348?via%3Dihub</ref>.

The VMAT2 upregulation produced by kanna is a compensatory response produced by stimulants such as cocaine and methylphenidate <ref>https://pubmed.ncbi.nlm.nih.gov/16897597/</ref>. However, some online users have misinterpreted the findings of VMAT2 upregulation from kanna as evidence of being a different type of stimulant. This is false, and monoamine releasing agents upregulate VMAT2 as a compensatory mechanism, involved in tolerance. VMAT2 upregulation is evidence that a compound acts similar to monoamine releasers like cocaine and methylphenidate <ref>https://pmc.ncbi.nlm.nih.gov/articles/PMC6757793/</ref>

The VMAT2 upregulation produced by kanna is thought to be responsible for the effects of kanna as a stimulant and euphoriant, due to the increase of dopamine and noradrenaline. The potent SSRI activity and PDE4 inhibition are thought to be mainly responsible for the antidepressant, anxiolytic, and sedating effects produced by kanna.

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Pharmacology

Mechanism of Action

Kanna primarily works by inhibiting serotonin reuptake, increasing serotonin levels in the synaptic cleft. This leads to mood enhancement, anxiolysis, and mild euphoria.

Additionally, the PDE4 inhibition by mesembrenone may contribute to neuroprotection, anti-inflammatory effects, and cognitive benefits (Lima et al., 2022).

Pharmacokinetics

Half-life: Not well-documented, but estimated to be 4–6 hours based on anecdotal reports.

Bioavailability:

Oral & sublingual: High

Intranasal: Moderate

Inhaled (smoked/vaporized): Low

More research is needed to determine the exact metabolic pathways and elimination rates of mesembrine alkaloids in humans.

[[User:Planlos69|Planlos69]] ([[User talk:Planlos69|talk]]) 09:49, 30 January 2025 (UTC)

==Subjective effects==

@@ Line 11: / Line 11: @@
 {{chemistry}}
 The active compounds in kanna are mesembrine, mesembrenone, mesembrenol, and tortuosamine. It is believed that mesembrine and mesembrenone are responsible for the majority of kanna's effects.
+Chemistry of Kanna (Sceletium tortuosum)
+Kanna contains a variety of alkaloids, which are responsible for its psychoactive effects. The primary bioactive compounds are mesembrine-type alkaloids, along with other secondary metabolites.
+. Mesembrine Alkaloids (Primary Active Compounds)
+Mesembrine – A serotonin reuptake inhibitor (SRI) and mild phosphodiesterase-4 (PDE4) inhibitor. It has a high affinity for the serotonin transporter (SERT), with a K<sub>i</sub> value of 1.4 nM, meaning it strongly inhibits serotonin reuptake. It also inhibits PDE4 at a much weaker level (K<sub>i</sub> = 7,800 nM) (Smith et al., 1998).
+Mesembrenone – Functions as both an SRI and a PDE4 inhibitor, though it is weaker at serotonin reuptake inhibition than mesembrine (K<sub>i</sub> = 27 nM for SERT). However, it more potently inhibits PDE4, with a K<sub>i</sub> value of 470 nM, suggesting potential anti-inflammatory and cognitive-enhancing effects (Gericke & Viljoen, 2008).
+Mesembrenol – A metabolite of mesembrine that is thought to contribute to Kanna’s anxiolytic and mood-enhancing effects. Specific pharmacological data on mesembrenol are limited.
+Tortuosamine – A lesser-known alkaloid found in Kanna. Its precise pharmacological properties are not well studied, but it is suspected to play a minor role in Kanna's psychoactive profile (PubChem).
+. Additional Compounds
+In addition to mesembrine alkaloids, Kanna also contains:
+Flavonoids – Antioxidant compounds with potential neuroprotective and anti-inflammatory properties.
+Tannins – Polyphenolic compounds that may affect taste and bioavailability.
+Saponins – Plant-based glycosides with potential immune-modulating properties.
+ [[User:Planlos69|Planlos69]] ([[User talk:Planlos69|talk]]) 09:49, 30 January 2025 (UTC)
 ==Pharmacology==
 {{pharmacology}}
-The main psychoactive effects of kanna are a result of its action as a potent serotonin reuptake inhibitor ([[SRI]]), a [https://en.wikipedia.org/wiki/Phosphodiesterase-4_inhibitor PDE4 inhibitor], and an upregulator of VMAT2 <ref>https://www.sciencedirect.com/science/article/pii/S0378874115302348?via%3Dihub</ref>.
+The main psychoactive effects of kanna are a result of its action as a potent serotonin reuptake inhibitor ([[SRI]]), a [https://en.wikipedia.org/wiki/Phosphodiesterase-4_inhibitor PDE4 inhibitor], and a monoamine releasing agent. <ref>https://www.sciencedirect.com/science/article/pii/S0378874115302348?via%3Dihub</ref>.
+The VMAT2 upregulation produced by kanna is a compensatory response produced by stimulants such as cocaine and methylphenidate <ref>https://pubmed.ncbi.nlm.nih.gov/16897597/</ref>. However, some online users have misinterpreted the findings of VMAT2 upregulation from kanna as evidence of being a different type of stimulant. This is false, and monoamine releasing agents upregulate VMAT2 as a compensatory mechanism, involved in tolerance. VMAT2 upregulation is evidence that a compound acts similar to monoamine releasers like cocaine and methylphenidate <ref>https://pmc.ncbi.nlm.nih.gov/articles/PMC6757793/</ref>
-The VMAT2 upregulation produced by kanna is thought to be responsible for the effects of kanna as a stimulant and euphoriant, due to the increase of dopamine and noradrenaline. The potent SSRI activity and PDE4 inhibition are thought to be mainly responsible for the antidepressant, anxiolytic, and sedating effects produced by kanna.
 {| class="wikitable"
 |-
@@ Line 31: / Line 63: @@
 | ND || ND
 |}
+Pharmacology
+Mechanism of Action
+Kanna primarily works by inhibiting serotonin reuptake, increasing serotonin levels in the synaptic cleft. This leads to mood enhancement, anxiolysis, and mild euphoria.
+Additionally, the PDE4 inhibition by mesembrenone may contribute to neuroprotection, anti-inflammatory effects, and cognitive benefits (Lima et al., 2022).
+Pharmacokinetics
+Half-life: Not well-documented, but estimated to be 4–6 hours based on anecdotal reports.
+Bioavailability:
+Oral & sublingual: High
+Intranasal: Moderate
+Inhaled (smoked/vaporized): Low
+More research is needed to determine the exact metabolic pathways and elimination rates of mesembrine alkaloids in humans.
+ [[User:Planlos69|Planlos69]] ([[User talk:Planlos69|talk]]) 09:49, 30 January 2025 (UTC)
 ==Subjective effects==