Saturday, November 22, 2008

Kratom Derivatives

I found another kratom paper discussing the synthesis of compounds derived from mitragynine and their effects in mice. From the paper:

The oxidative derivatives of mitragynine, i.e., mitragynine pseudoindoxyl and 7-hydroxymitragynine, were found as opioid agonists with higher potency than morphine in the experiment with guinea pig ileum.

[7-hydroxymitragynine], a minor constituent of M. speciosa [kratom], was found to exhibit high potency to opioid receptors: about 13- and 46-fold higher than those of [mitragynine pseudoindoxyl] and [mitragynine], respectively.

The intrinsic activity of [7-hydroxymitragynine] suggested its full agonistic property on opioid receptors.

In other words, the main active alkaloid of kratom is a full agonist (activator) of μ-opioid receptors and is quite potent. Furthermore:

It was also found that the methoxy group on the indole ring at the C9 position as well as the Nb lone electron pair in the fundamental structure of Corynanthe type indole alkaloid are essential structural functions for opioid agonistic activity. With altering the functional group at the C9 position, i.e., OMe -> OH -> H, of mitragynine, the activities of compounds dramatically shifted from that of full agonists through partial agonists to that of antagonists on opioid receptors.

So it's relatively easy to modify mitragynine to be a full agonist, partial agonist, or antagonist. The medical implications for this could be huge, with designer pharmaceuticals with just the correct proportions of each of these to provide effective pain relief while also preventing a tolerance buildup. This also explains the antagonistic properties of kratom; the process they did of OMe -> OH -> H is the opposite of the process the plant uses to synthesis mitragynine. So these intermediates are present in the leaf, most likely being responsible for kratom also being an opioid antagonist as well as an agonist.

The full text of the paper can be found here on Scribd. There is also a link to download the PDF on there.

Tuesday, November 18, 2008

Kratom ban no longer a threat in Massachusetts

In 2007, a bill was proposed in Massachusetts that would have outlawed salvia divinorum along with kratom and khat.

The Amherst Student News gives an update on this issue. The bill to ban salvia is still moving forward, however, kratom and khat were removed from the bill. According to Rep. Vinny deMacedo, R-Plymouth, "There was not a lot of support for it.. They were removed so we could move the salvia piece forward. Albeit, Chief of Police Hayes felt strongly about keeping them on."

It is fortunate that the representatives proposing the bill decided it wasn't worth criminalizing kratom. It is widely recognized as a legitimate herbal remedy so it would be a shame to outlaw it.

Monday, November 10, 2008

Wholesale Kratom

Wholesale kratom is available from several different sources.

The world's largest supplier of Bali kratom is Wholesale Shamanic Herbs, also operating a retail website, Psychoactive Herbs.

You can also get wholesale kratom from Get Kratom.

Wednesday, November 5, 2008

Kratom Instructions

Kratom tastes extremely bitter. The best way to mask it is with sugar. Lots and lots of sugar. Maybe some splenda and honey too. Honey really cuts the bitterness. Best is to add sugar to the pot so it dissolves, then add a little honey to your cup.

Suggested Instructions:

Start by boiling a saucepot with the amount of tea you want; I suggest 2 cups, or 32 ounces, per person. More or less water can be used, as this only affects how concentrated (and bitter) the kratom is. As long as you drink it all, the effect will be the same.

After the water is boiling, turn the heat off. For a first time user, measure slightly approximately 1 tablespoon (6-7 grams) of kratom leaf powder per person and add to the pot. More experienced users can use up to 2 tablespoons (12-14 grams). After the kratom is in, pour in a lot of sugar and stir. If you prefer to use artificial sweeteners instead of sugar, these can be added to your cup at the end if it's more convenient.

Allow the kratom to steep for at least 15-20 minutes, or until cool enough to drink, stirring occasionally. Let it sit for five minutes after last stirring to allow the kratom powder to settle. Then, pour it into a pitcher, taking care so that the powder stays in the bottom of the pot.

After it's in the pitcher, pour it into a french press to filter out any powder that remains. If you do not have a french press, simply let it sit again so the powder settles on the bottom.

Enjoy, and remember that the more sugar (and honey) you add, the better it will taste, within reason. If you at any point don't feel well, lay down on your back and it will immediately go away.

You can put the powder back in the pot and add more water to boil again. There will be some effect, but it will be much weaker. There is almost no effect on a third preparation of the same powder.