Kava lactones act as reversible MAO-B inhibitor

[apothecary]

http://www.ncbi.nlm.nih.gov/sites/entrez?c...st_uids=9832350

Inhibition of platelet MAO-B by kava pyrone-enriched extract from Piper methysticum Forster (kava-kava).

Uebelhack R, Franke L, Schewe HJ.

Department of Psychiatry, Humboldt-Universität zu Berlin (Charité), Germany.

Kava-kava, a psychoactive beverage, induces relaxation, improves social interaction, promotes sleep and plays an important role in the sociocultural life in the islands of the South Pacific. On the other hand, standardized extracts of kava-kava roots are used for the therapy of anxiety, tension and restlessness. Kava pyrones, the major constituents of kava kava, are generally considered to be responsible for the pharmacological activity in humans and animals. To obtain more information on the mechanisms by which kava-kava exerts psychotropic properties we investigated the in vitro effects of kava-kava extract and pure synthetic kava pyrones on human platelet MAO-B, in comparison to amitriptyline, imipramine and brofaromine. Kava-kava extract was found to be a reversible inhibitor of MAO-B in intact platelets (IC50 24 microM) and disrupted platelet homogenates (IC50 1.2 microM). Structural differences of kava pyrones resulted in a different potency of MAO-B inhibition. The order of potency was desmethoxyyangonin > (+/-)-methysticin > yangonin > (+/-)-dihydromethysticin > (+/-)- dihydrokavain > (+/-)-kavain. The two most potent kava pyrones, desmethoxyyangonin and (+/-)-methysticin displayed a competetive inhibition pattern with mean Ki 0.28 microM and 1.14 microM respectively. The inhibition of MAO-B by kava pyrone-enriched extracts might be an important mechanism for their psychotropic activity.

[friendly]

This is interesting news. Someone should try Kava with tryptamines and see if the synergy works there as well.

[apothecary]

After some initial experimentation appears to me that the kava is actually extremely effective in this regard.

500mg L-tyrosine was ingested in the morning of one day, with the usual nightly cup of kava that night. The subject usually only notices the 'increased catecholamine' effect of tyrosine ingestion for maybe 36 hours maximum with 24 being the usual. However with daily kava ingestion this increased level seem to be noticeable for longer than 48 hours, well into the third day after supplementation.

A few similar experiments with 3mg non-homeopathic melatonin were conducted but the subject noticed that if anything the efficiacy of the melatonin was decreased. Usually similar dosage would allow the subject to sleep very easily (i.e. not sedative, but with head on the pillow very easy to drift off) for up to 24 hours if wished, but when ingested alongside kava this effect was limited to around 9 hours.

[platypii]

I thought tryptamines were metabolised by MAO-A?

It would probably potentiate mescaline though....

[friendly]

Oops. Mea culpa; you are correct. I need to stop relying on my memory and check things out in reference books before I can make definitive statements anymore. Getting old sucks. I strongly advise against any of you doing it. All those smiling happy old people in the ads are on prozac, vicodin and viagra; it's all lies.

[incognito]

i drank ALOT of kava once (over a period of say 4 hrs) then consumed about 11 grams of dried fungus.

was the deepest ive ever gone, id like to think that the kava prolonged and enhanced the experience. I was glad when it was all over (2 days later) lol.

[The Dude]

i drank ALOT of kava once (over a period of say 4 hrs) then consumed about 11 grams of dried fungus.

was the deepest ive ever gone, id like to think that the kava prolonged and enhanced the experience. I was glad when it was all over (2 days later) lol.

wow

[incognito]

full effects lasted for say 8 hrs and the rest was residual.

[AndyAmine.]

Indeedy..

[t st tantra]

we need to find out more about the practical side of these things.............

as previously stated tryptamines[shrooms] would be expected to be potentiated only by an mao a i.

large doses of harmala alkaloids[over 10gm approx seed] are said to inhibit mao a and b.

raving.......a substance can be broken down by mao a or b,with mescaline for instance,if you inhibit one it is broken down by the other exclusively,so you choose which end products[effects] you get.

11grams,sorry forget the above............

t s t .

[t st tantra]

2. The pharmaceutical composition according to claim 1, wherein the DSHEA compliant inhibitor wherein the inhibitor is selected from the group of Piper longum and Piper methisticum Kava (including but not limited to the pure moieties contained in Piper longum and/or Piper methisticum Kava: piperine, desmethoxyyangonin, (+/-)-methysticin, yangonin, (+/-)-dihydromethysticin, (+/-)-dihydrokavain, (+/-)-kavain.), Ginkgo biloba (including but not limited to the pure moieties contained in Ginko biloba: kaempferol and isorhamnetin), Hypericum perforatum L (aka--St. John's wort including but not limited to the pure moieties contained in Hypericum perforatum: quercetin and hypericin), other Hypericum species including, Hypericum caprifoliatum, Hypericum carinatum, Hypericum connatum, Hypericum cordatum, Hypericum myrianthum, Hypericum piriai, Hypericum polyanthemum and Hypericum brasiliense (including but not limited to the pure moieties contained in some or all species of Hypericum: 6-isobutyryl-5,7-dimethoxy-2,2-dimethylbenzopyran, 7-hydroxy-6-isobutyryl-5-methoxy-2,2-dimethylbenzopyran, 5-hydroxy-6-isobutyryl-7-methoxy-2,2dimethylbenzopyran), Evodia rutaecarpa (including but not limited to the following moieties found in Evodia rutaecarpa: 1-methyl-2-undecyl-4(1H)-quinolone, evodiamine, rutaecarpine, limonin, and goshuyuamide II), Rhizoma acori gramine (including but not limited to the following moieties found in Rhizoma acori gramine: eugenol and beta-asarone), Sinofranchetia chinensis (including but not limited to the following moieties found in Sinofranchetia chinensis: liquiritigenin and isoliquiritigenin), Uncaria rhynchophylla (including but not limited to the following moieties found in Uncaria rhynchophylla: (+)-catechin and (-)-epicatechin.), Salvia divinorum (including but not limited to the following moiety found in Salvia divinorum: salvinorin A), Bacopa monniera (including but not limited to the following moiety found in Bacopa monniera: Bacoside A), Cudrania tricuspidata (including but not limited to the following moieties found in Cudrania tricuspidata: Gancaonin A, 4'-O-methylalpinumisoflavone, and alpinumisoflavone), Lithospermum erythrorhizon (including but not limited to the following moieties found in Lithospermum erythrorhizon: acetylshikonin, shikonin, and shikonofuran E), Sophora flavescens (including but not limited to the following moieties found in Sophora flavescens: formononetin, kushenol F, oxymatrine, trifolirhizin, and beta-sitosterol), Melastoma candidum (including but not limited to the following moieties found in Melastoma candidum: quercitrin, isoquercitrin and rutin), Coptis chinensis (including but not limited to the following moieties found in Coptis chinensis: jatrorrhizine, berberine and palmatine), Opuntia ficus-indica (including but not limited to the following moieties found in Opuntia ficus-indic: 1-monomethyl citrate, 1,3-dimethyl citrate, trimethyl citrate and 1-methyl malate, Uncaria tomentosa, Uncaria gambir, Radix Paeoniae Alba, Green tea (including but not limited to the following moieties found in Green tea (-)-epicatechin, (-)-epicatechin-3-gallate, (-)-epigallocatechin and (-)-epigallocatechin-3-gallate), various types of yams (Dioscorea species--including but not limited to the following moieties found in various yam species: diosgenin, 5-keto-diosgenin, 6-keto-diosgenin) or the pure moiety/supplement hordenine (N,N-dimethyltyramine) which is found in barley and grasses).

Cudrania tricuspidata (including but not limited to the following moieties found in Cudrania tricuspidata: Gancaonin A, 4'-O-methylalpinumisoflavone, and alpinumisoflavone), Lithospermum erythrorhizon (including but not limited to the following moieties found in Lithospermum erythrorhizon: acetylshikonin, shikonin, and shikonofuran E), Sophora flavescens (including but not limited to the following moieties found in Sophora flavescens: formononetin, kushenol F, oxymatrine, trifolirhizin, and beta-sitosterol), Melastoma candidum (including but not limited to the following moieties found in Melastoma candidum: quercitrin, isoquercitrin and rutin), Coptis chinensis (including but not limited to the following moieties found in Coptis chinensis: jatrorrhizine, berberine and palmatine), Opuntia ficus-indica (including but not limited to the following moieties found in Opuntia ficus-indic: 1-monomethyl citrate, 1,3-dimethyl citrate, trimethyl citrate and 1-methyl malate, Uncaria tomentosa, Uncaria gambir, Radix Paeoniae Alba, Green tea (including but not limited to the following moieties found in Green tea (-)-epicatechin, (-)-epicatechin-3-gallate, (-)-epigallocatechin and (-)-epigallocatechin-3-gallate), various types of yams (Dioscorea species--including but not limited to the following moieties found in various yam species: diosgenin, 5-keto-diosgenin, 6-keto-diosgenin) or the pure moiety/supplement hordenine (N,N-dimethyltyramine) which is found in barley and grasses).

http://www.freepatentsonline.com/20070190187.htm

t s t .

[platypii]

How would MAO-b inhibition affect someone on SSRI medication, as I am...? One would think it would be dangerous; yet I have NEVER felt that. Anyway, I've heard of people using Selegiline (prescribed for their dog, the bastards) in a crude and unsuccessful pharmahusca attmept. Either way, DMT is pretty active anally, so if people wanna prolong the effects of it, for example not that they would, squirt 100mg upwards

[Flip]

Getting old sucks. I strongly advise against any of you doing it. All those smiling happy old people in the ads are on prozac, vicodin and viagra; it's all lies.

LOL I hear that Cognitol™ works wonders for that sorta thing... available without prescription!

[Flip]

Getting old sucks. I strongly advise against any of you doing it. All those smiling happy old people in the ads are on prozac, vicodin and viagra; it's all lies.

LOL I hear that Cognitol™ works wonders for that sorta thing... available without prescription!

[t st tantra]

be selfsuficient grow and produce your own cognitol from oz celastrus sp ,i have a few plants available.

bushwalking on cognitol and low dose entheogens produces 4 me a powerful state of mentation in which i have thought trains i think would otherwise have taken years to think through.then i'm on to the next and it all gets lost.some catha actives apparently.not cathine types.

t s t .

[friendly]

Cognitol does indeed synergize with entheogens, and you are right; I should be taking it.

I am taking a sabbattical from all supplements for a few months to get back to baseline so I cxan notice the effects more easily.

That being said, I just recently had a liter of Celastrus oil bound to lecithin and extracted to a 20:1 dry orange powder with super critical CO2.

I haven't yet tried it as I have a large contract that goes until 12/15 for extract production and seeing as I will have to bioassay the new Cognitol extract and I don't want to be bouncing off the walls while extracting, I am holding off t=for another week or so.

I first used Celastrus paniculatis seeds for the oil, and they are the freshest, strongest source. The oil from one seed was enough to rocket me into the strartospere the first time I tried it.

I crushed the seed betwen by thumbnails and licked the oil off them, not expecting any result from such a small amount.

The rush took me completely by surprise and made me realize immediately what I had found.

[friendly]

A tea from Maytenus ebenifolia bark, a tree (also known as chuchuasi and a few other Latin names--taxonomy wars, again) from the Amazon, and a member of the Celastraceae family is sometimes used in the week of fasting prior to ingestion of Ayahuasca to help clarify one's mind and provide energy prior to the ceremony. Maytenine, a compound isolated from the bark of the tree has remarkably similar properties to those of Cognitol , and was patented for the same uses by an Italian company, but I don't think they are still around.

The point of this is; there are many related species---one of my favorite themes---as yet uninvestigated which may well possess similar properties to those better known and desirable species just waiting for someone like any of you to come along with an open and curious mind and be the first to find it out.

Various psychoactive Salvias, Mesembrine containing succulents and assorted Nymphaea species are good examples of this principle in action, and I expect there will be many more uncovered as the body of knowledge grows.

Psychotria species might be a good place--if obvious--to look. You guys are already on to the Acacia thing.

ktrout has done incredible work with trichos, and that body of knowledge is growing exponentially from all directions, as is fungal research and discovery.

Sorry to get so far away from Kavalactones...