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Levonantradol : ウィキペディア英語版
Levonantradol

Levonantradol (CP 50,556-1) is a synthetic cannabinoid analog of dronabinol (Marinol) developed by Pfizer in the 1980s. It is around 30x more potent than THC, and exhibits antiemetic and analgesic effects via activation of CB1 and CB2 cannabinoid receptors.〔Little PJ, ''et al.'' Pharmacology and stereoselectivity of structurally novel cannabinoids in mice. ''Journal of Pharmacology and Experimental Therapeutics'' 1988; 247:1046–1051.〕 Levonantradol is not currently used in medicine as dronabinol or nabilone are felt to be more useful for most conditions, however it is widely used in research into the potential therapeutic applications of cannabinoids.〔Tramer MR, ''et al.'' Cannabinoids for control of chemotherapy induced nausea and vomiting: quantitative systematic review. ''British Medical Journal'' 2001 Jul 7;323(7303):16-21.〕〔Campbell FA, ''et al.'' Are cannabinoids an effective and safe treatment option in the management of pain? A qualitative systematic review. ''British Medical Journal''. 2001 Jul 7;323(7303):13-6.〕〔Ben Amar M. Cannabinoids in medicine: A review of their therapeutic potential. ''Journal of Ethnopharmacology''. 2006 Apr 21;105(1-2):1-25.〕
==Pharmacodynamics==
Levonantradol is a full CB1 receptor agonist. Cannabinoid receptors belong to the superfamily of G-protein coupled receptors (GPCRs), and endogenous cannabinoids naturally activate GPCRs. GPCRs modulate the inhibition of adenylyl cyclase and accumulation of the second messenger, cyclic adenosine monophosphate (cAMP). The CB1 receptor is the most common GPCR in the central nervous system. The activation of CB1Rs decrease calcium conductance and increase potassium conductance in the brain. CB signaling naturally modulates synaptic transmission and mediates psychoactivity, and synthetic cannabinoids mimic these same actions. Although the efficacy of Levonantradol is dependent on the level of GCPR activity, Full agonists like Levonantradol have the ability to activate GPCRs and convert Gα into a high affinity state for GTP or low affinity state for GDP. Previous studies suggest that Levonantradol has a higher binding affinity and efficacy than other similar synthetic cannabinoids (e.g. Δ9-THC).

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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