Author Topic: Hydroxypropyl Beta Cyclodextrin (HPßCD) and...  (Read 145 times)

blowjay

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Hydroxypropyl Beta Cyclodextrin (HPßCD) and...
« on: March 08, 2012, 05:03:41 AM »
I do not see this being thrown around on this board at all but I have just remembered that I forgot to voice my idea about Hydroxypropyl Beta Cyclodextrin (HPßCD) being used with loperamide. I did not want to point this out on bluelight again as my last post has been un-noticed (might want to delete it too...) BUT it does seem to me like this could be something to play around with.

The reason of me leaving this a little blank and open is because I think it would be fun to get everyone thinking about new uses for this. I have thought of loperamide as one possible application and others are experimenting on different boards with this for cannabinoids and of course the NBOMe's but this compound seems to be very interesting and I would just like to hopefully get some ideas going.

I wonder how things such as NMT would fair with this guy, most likely still nothing but there has to be some thing that has not been considered that will be golden with HPßCD.

Not really too sure if I posted this in the right place but here is hoping.

dream0n

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Re: Hydroxypropyl Beta Cyclodextrin (HPßCD) and...
« Reply #1 on: March 08, 2012, 05:34:39 AM »
The compound increases absorption and bio-availability of compounds lacking in it.
To understand how this is possible, we take a look at how it opens up transport channels.. by looking at its space filling 3d mol. model.
http://en.wikipedia.org/wiki/Cyclodextrin


" This is the reason why cyclodextrins have attracted much interest in many fields, especially pharmaceutical applications: because inclusion compounds of cyclodextrins with hydrophobic molecules are able to penetrate body tissues, these can be used to release biologically active compounds under specific conditions." [cite^5  doi:10.1016/S0378-5173(98)00382-2 ]
« Last Edit: March 08, 2012, 05:40:00 AM by dream0n »
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blowjay

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Re: Hydroxypropyl Beta Cyclodextrin (HPßCD) and...
« Reply #2 on: March 08, 2012, 05:36:57 AM »
Wouldn't that mean that it could potentially help loperamide cross the BBB?

dream0n

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Re: Hydroxypropyl Beta Cyclodextrin (HPßCD) and...
« Reply #3 on: March 08, 2012, 05:41:02 AM »
Potentially, yes
off to bigger and better things - don't worry I will visit from time to time

blowjay

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Re: Hydroxypropyl Beta Cyclodextrin (HPßCD) and...
« Reply #4 on: March 08, 2012, 05:47:50 AM »
Well I have access to both what would a smart start be for such an experiment? Am not tolerant to anything and to give a background I am able to take 20-30 mg of oxycodone without problems as well as (at a seperate time) ~35-40 mg of hydrocodone. Not the biggest fan of this family of compounds but I like potential discoveries.

 Have had morphine and fentanyl and methadone and other random ass cousins of the bunch but the only doses I am familiar with are the previously mentioned -codone compounds.


dream0n

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Re: Hydroxypropyl Beta Cyclodextrin (HPßCD) and...
« Reply #5 on: March 08, 2012, 05:55:13 AM »
Starting with maybe 5mg loperamide, going up by 3mg every half hour to full hour until effects are noticed.
With respect to your previous doses possible 1/4 as much that would have been taken without complexing.
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Tsathoggua

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Re: Hydroxypropyl Beta Cyclodextrin (HPßCD) and...
« Reply #6 on: March 09, 2012, 05:08:14 AM »
And do for for fucks sake do some reading up before trying this on the potential POISON that it might metabolise to, appears to do so, in organisms W/ compromised BBBs.


Nomen mihi Legio est, quia multi sumus

I'm hyperbolic, hypergolic, viral, chiral. So motherfucking twisted my laevo is on the right side.

blowjay

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Re: Hydroxypropyl Beta Cyclodextrin (HPßCD) and...
« Reply #7 on: March 09, 2012, 10:01:16 AM »
And do for for fucks sake do some reading up before trying this on the potential POISON that it might metabolise to, appears to do so, in organisms W/ compromised BBBs.

Duly noted (will remove the bluelight post now), figured that it was a half-way 'safe' thing to be going about doing considering the money put into this chemical when getting developed by (wasn't it Janssen looking for something better than Fent or similar?). Well this does appear to be pretty much unknown... fuck?

I have no intention of trying to spread this shit into the wind if it works due to the addicts who are already everywhere but it would be very interesting to know that it could potentially work. Time to do some more reading it looks like.

But what you are saying unintentionally is that this would not compromise the BBB? The complexation by my understanding simply encapsulates the molecule, why would this do anything to the BBB?

I know this does not make it safe in any way from the dangers of the molecule itself crossing the BBB but wouldn't this method only be a means to have loperamide cross the BBB?

I am not going to be doing any experimentation without first reading up on this very much, it would help to know where to begin but I will not be one of those guys unless I have to. I just want to contribute a bit to the community and this seemed an interesting way but I sure as fuck don't want to spawn a generation of OTC junkies or OD myself.

antibody2

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Re: Hydroxypropyl Beta Cyclodextrin (HPßCD) and...
« Reply #8 on: August 10, 2012, 12:47:05 AM »
Ab2 has seen 25I-NBOMe advertised as having been complexed with cyclodextrin, it caught her attention too. A while back Ab2 got a hold of several different sizes to try an aqueous wacker RXN but never got around to that experiment. But thought it might be interesting to complex with other things too.

@Tsathoggua - is there any specific reading you are referring to? Ab2 seems to recall hearing of it being used in dietary supplements. So never really gave much though to its toxicity.

Enkidu

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Re: Hydroxypropyl Beta Cyclodextrin (HPßCD) and...
« Reply #9 on: August 10, 2012, 11:58:36 AM »
IIRC, the Hydroxypropyl variant is well tolerated. Other beta-cyclodextrines are not. I don't think that HPBCD will help anything get past the BBB because HPBCD is probably too large to be transported (if the loperamide-HPBCD complex is IV'd) and it won't be diffused across the membrane. The reason loperamide isn't CNS active is that it gets removed rapidly by the p-glycoprotien pump after it gets across the BBB.

Tsathoggua

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Re: Hydroxypropyl Beta Cyclodextrin (HPßCD) and...
« Reply #10 on: August 12, 2012, 07:23:34 PM »
There are various sources online that point out the possibility of loperamide metabolizing into a quat once inside cells, ala MPTP, which of course cannot leave the brain due to its charge, AFAIK experiments done on baby pigs with incomplete BBBs resulted in destruction of DAergic neurons.

So it seems, that were one to succeed in bypassing the BBB through whatever means and thus allowing loperamide to cross, it will form the toxic metabolite and this is charged and thus unable to leave the cells, frying the  crap out of them, to use the technical terminology.
Nomen mihi Legio est, quia multi sumus

I'm hyperbolic, hypergolic, viral, chiral. So motherfucking twisted my laevo is on the right side.