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Sinomenine - opiate or NMDA antagonist?

tantric

tantric

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Jan 2, 2004
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athens GA
i ran across this little gem while web wandering....

Sinomenine or cocculine is an alkaloid found in the root of the climbing plant Sinomenium acutum which is native to Japan and China. It is traditionally used in herbal medicine in these countries, as a treatment for rheumatism and arthritis.[1] However, its analgesic action against other kinds of pain is limited. Sinomenine is a morphinan derivative, related to opioids such as levorphanol and the non-opioid cough suppressant dextromethorphan. Its anti-rheumatic effects are thought to be primarily mediated via release of histamine,[2] but other effects such as inhibition of prostaglandin, leukotriene and nitric oxide synthesis may also be involved
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220px-Sinomenine.svg.png


it really looks a LOT like dxm...dammit, did my research, it attenuates morphine withdrawal. nice.....the new ibogaine.
 
NMDA antagonists pretty much all alleviate MOR agonist WD.

Taking memantine dropped my opioid tolerance from shooting a gram to 1.5g morphine to nodding hard off of maybe 60-80mg within days.
 
Unsure, scale is busted I need a new one, accidentally spilled SOCl2 on it and it kinda....well it melted it.
 
1,500mg to 80mg. Why are we not using these to reverse changes to receptors after long-term opioid dependence? Clearly, it must be doing something right with the receptors if one can achieve such an effect. Let's be honest, 1,500mg tolerance is... not the tolerance of a rookie opioid user.
 
1,500mg to 80mg. Why are we not using these to reverse changes to receptors after long-term opioid dependence? Clearly, it must be doing something right with the receptors if one can achieve such an effect. Let's be honest, 1,500mg tolerance is... not the tolerance of a rookie opioid user.

BTW, sinomenine might be neither an opioid nor an NMDA antagonist, but still it looks like a nice starting point for new synthetic d-morphinans with adjustable pharmacodynamics. Ibogaine and its plant source are definitely too expensive to synthesize selective nicotine antagonists that could be widely used medicinally, so perhaps let's try with d-morphinans.
 
adder said:
7Ibogaine and its plant source are definitely too expensive to synthesize selective nicotine antagonists that could be widely used medicinally, so perhaps let's try with d-morphinans.
Click to expand...
A company called Savant currently has 18-methoxycoronaridine in phase I trials. They managed to scale up and optimize synthesis of the ibogaine/coronaridine scaffold to the level where it is economical to develop these compounds for wide-spread medical use.
 
dose of memantine was maybe 100mg per dose. Eyeballing because I damaged my scale, partially melted the platter with SOCl2.

Then when raided by the pigs they fucked it completely.
 
The memantine I found to be a right bastard to eyeball, it's so fluffy ...


I wonder if it's possiblr to turn sinomenine into a DXM analog?
 
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