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InvisibleJessica Swift
यन्त्र
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Registered: 01/13/12
Posts: 1,723
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Structure of ‘salvia’ Receptor Solved
    #15980016 - 03/22/12 06:50 AM (12 years, 9 days ago)

http://www.sciencedaily.com/releases/2012/03/120321142018.htm

ScienceDaily (Mar. 21, 2012) — At the molecular level, drugs like salvinorin A (the active ingredient of the hallucinogenic plant Salvia divinorum) work by activating specific proteins, known as receptors, in the brain and body.

Salvinorin A, the most potent naturally occurring hallucinogen, is unusual in that it interacts with only one receptor in the human brain -- the kappa opioid receptor (KOR). Scientists know of four distinct types of opioid receptors, but until now the structure of the 'salvia receptor', and the details about how salvinorin A and other drugs interact with it, was a mystery.

In a research paper published March 21 in the journal Nature, scientists from the University of North Carolina at Chapel Hill, Scripps Research Foundation and two other institutions revealed the first-ever glimpse of the complete structure of the KOR. The finding could accelerate the development of new drugs to treat addiction, depression, anxiety, chronic pain and many other conditions.

"Once we see the structure of the receptor, it becomes easier for us to develop drugs that target the receptor in ways that might be beneficial for medical therapy," said Bryan Roth, MD, PhD, the Michael Hooker Distinguished Professor of Pharmacology at UNC and one of the paper's authors. "Drugs that block the receptor are potentially useful for treating a number of serious illnesses including chronic pain, cocaine addiction and other diseases."

The KOR is responsible for the action of drugs that affect human consciousness, awareness of pain and mood. The KOR is the only receptor that binds salvinorin A -- the active ingredient of the widely-abused hallucinogenic plant Salvia divinorum (also known as 'Magic mint', 'Salvia' and so on). Salvia use has surged among teenagers and young adults with more than 5 percent reporting usage in the past year.*

Knowing KOR's structure offers insights about how salvia and other drugs work. The finding also could help scientists design medicines that either activate or block KOR to benefit patients.

The research team crystallized KOR using JDTic, a drug currently in early-stage human trials; JDTic keeps KOR in an inactive state and blocks the actions of salvinorin A. In studies using animal models, JDTic has shown promise for treating cocaine and nicotine addiction, depression and anxiety.

The downside of JDTic and similar drugs targeting KOR is that they can exert their actions for weeks, whereas most prescribed medicines are cleared within 18-24 hours. "Now that we have the [KOR] structure, it opens up the possibility for us to make drugs that have the same action as JDTic but have better pharmaceutical properties," said Roth.

The research also resolves longstanding scientific debates about how drugs bind to KOR. The study found that compared to other receptors, the binding site on KOR is enormous, allowing drugs to bind to it in more than one way.

In addition, Roth said the research could help scientists develop drugs that activate KOR in the body without affecting the brain, which could be useful for treating chronic pain, kidney problems and many other disorders.

Co-authors include Eyal Vardy and Xi-Ping Huang at UNC-Chapel Hill; Huixian Wu, Daniel Wacker, Vsevolod Katritch, Mauro Mileni, Gye Won Han, Wei Liu, Aaron A. Thompson, Vadim Cherezov and Raymond C. Stevens from the Scripps Research Institute; F. Ivy Carroll and S. Wayne Mascarella from the Research Triangle Institute; and Richard B. Westkaemper and Philip D. Mosier from Virginia Commonwealth University.

The study was supported by funding from the National Institutes of Health.

* Source: National Institute on Drug Abuse InfoFacts; http://www.drugabuse.gov/publications/infofacts/salvia.

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InvisibleeLShaMukO
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Registered: 04/28/10
Posts: 1,686
Loc: far away
Re: Structure of ‘salvia’ Receptor Solved [Re: Jessica Swift]
    #15980055 - 03/22/12 07:10 AM (12 years, 9 days ago)

cool article jessica:thumbup:


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OfflineDest
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Registered: 06/14/09
Posts: 2,444
Last seen: 6 years, 7 months
Re: Structure of ‘salvia’ Receptor Solved [Re: eLShaMukO]
    #15980076 - 03/22/12 07:27 AM (12 years, 9 days ago)

first "breakthrough" to lvl 5 was on salvia. Not pleasant but is space travel ever comfortable?
It seems almost all psychedelic research is concerning the brain/CNS .if we turned our attention to how these extremely potent molecules affect other organs would we not have greater comprehension of their medical value? Salivorum compounds clearly have an effect on skeletal muscles....

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OfflineVisionaryFlicker
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Registered: 12/12/09
Posts: 2,456
Loc: Amsterdam Flag
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Re: Structure of ‘salvia’ Receptor Solved [Re: Dest]
    #15980085 - 03/22/12 07:30 AM (12 years, 9 days ago)

Quote:

Dest said:
first "breakthrough" to lvl 5 was on salvia. Not pleasant but is space travel ever comfortable?
It seems almost all psychedelic research is concerning the brain/CNS .if we turned our attention to how these extremely potent molecules affect other organs would we not have greater comprehension of their medical value? Salivorum compounds clearly have an effect on skeletal muscles....



What exactly do you base this rather bold assumption on dear sir?


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l'enfer c'est les autres

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OfflineDest
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Re: Structure of ‘salvia’ Receptor Solved [Re: VisionaryFlicker]
    #15980185 - 03/22/12 08:18 AM (12 years, 9 days ago)

look at the reaction of someone on salvia extract, you will see what im getting at. their diaphram is stimulated (laughing) then the body's skeletal muscles are the next to go all wonky. you could say that its the brain on drugs frying like an egg like a politician. However involantary skeletal muscle movement I do not belive is a coinceidence.

here is a rather extreme case of the response people get from a drug.

This is repeatable science, smoke enough salvia and you will get involuntary movement from volantary organs in some way shape or form.

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Invisibletealeaf
Just Touch It
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Registered: 09/21/06
Posts: 2,907
Re: Structure of ‘salvia’ Receptor Solved [Re: Dest]
    #15980219 - 03/22/12 08:29 AM (12 years, 9 days ago)

you mean they found the devil molecule in Salvia?

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InvisibleJessica Swift
यन्त्र
Female


Registered: 01/13/12
Posts: 1,723
Loc: Flag
Re: Structure of ‘salvia’ Receptor Solved [Re: tealeaf]
    #15980230 - 03/22/12 08:36 AM (12 years, 9 days ago)

Quote:

tealeaf said:
you mean they found the devil molecule in Salvia?




Those are in you, actually. But I get the drift. :smirk:

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Offlinereaction_s
Stranger

Registered: 03/05/12
Posts: 1
Last seen: 11 years, 11 months
Re: Structure of ‘salvia’ Receptor Solved [Re: Dest]
    #15980341 - 03/22/12 09:09 AM (12 years, 9 days ago)

SWIM recently found relief (hopefully) from chronic pain.

SWIM is on neuropathic, inflammatory and opiate medicines for pain.

SWIM's effort to diversify experiences serendipitously found Salvia.

Unfortunately SWIM's resident state decided that Saliva should be illegal.

SWIM has stated a journal to help track pain relief.

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InvisibleJessica Swift
यन्त्र
Female


Registered: 01/13/12
Posts: 1,723
Loc: Flag
Re: Structure of ‘salvia’ Receptor Solved [Re: reaction_s]
    #15980365 - 03/22/12 09:15 AM (12 years, 9 days ago)

No need to use SWIM. There is little evidence it helps anyway. It's just an anonymity placebo effect.

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OfflineConstantine
( ͡° ͜ʖ ͡°)
I'm a teapot


Registered: 05/01/11
Posts: 4,643
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Re: Structure of ‘salvia’ Receptor Solved [Re: reaction_s]
    #15980491 - 03/22/12 09:46 AM (12 years, 9 days ago)

SWIM - Someone Who Is Me

See how could they turn that around ?

Interesting article anyway, thanks for sharing! :thumbup: Salvia has always terrified me but I'm pretty sure we still have a lot more to learn from it.


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OfflineVisionary Tools
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Registered: 06/23/07
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Re: Structure of ‘salvia’ Receptor Solved [Re: reaction_s]
    #15980810 - 03/22/12 11:12 AM (12 years, 9 days ago)

Quote:

reaction_s said:
I recently found relief (hopefully) from chronic pain.

I am on neuropathic, inflammatory and opiate medicines for pain.

My efforts to diversify experiences serendipitously found Salvia.

Unfortunately my resident state decided that Saliva should be illegal.

I have stated a journal to help track pain relief.




There, fixed it for you.


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OfflineNature Boy
Stranger than most
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Registered: 07/09/07
Posts: 8,246
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Re: Structure of ‘salvia’ Receptor Solved [Re: Jessica Swift]
    #15980947 - 03/22/12 11:47 AM (12 years, 9 days ago)

Props to the scientists from the University of North Carolina at Chapel Hill and the Scripps Research Foundation for making the case for NOT making compounds such as salvia knee-jerked onto Schedule 1 by (over)reactionist politicians, thereby putting it out of the reach of legitimate study.  :thumbup:  :thumbup: 

N.B.


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All submitted posts under this user name are works of pure fiction or outright lies.  Any information, statement, or assertion contained therein should be considered pure unadulterated bullshit.  Note well:  Sorry, but I do not answer PM's unless you are a long-time trusted friend.  If you have a question, ask it in the appropriate thread.

                                                                               

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InvisibleLongStrangeTrip
Deadhead


Registered: 09/19/09
Posts: 5,382
Re: Structure of ‘salvia’ Receptor Solved [Re: Nature Boy] * 1
    #15981044 - 03/22/12 12:11 PM (12 years, 9 days ago)

Quote:

The downside of JDTic and similar drugs targeting KOR is that they can exert their actions for weeks, whereas most prescribed medicines are cleared within 18-24 hours. "Now that we have the [KOR] structure, it opens up the possibility for us to make drugs that have the same action as JDTic but have better pharmaceutical properties," said Roth.




This statement disturbs me.

Does anyone else feel like this? Seems that the reason a drug that exerts actions for weeks looks bad, compared to those that only do so for 18-24 hrs, because pharmaceutical companies are in the business of selling drugs.

God forbid we have something that necessitates 2 doses a month as opposed to 31 doses a month :suicide:


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Nothing I say or do is factual; every single thing I write is a work of fiction. Got no idea what I'm talking about here~

"Once in awhile, you get shown the light, in the strangest of places if you look at it right"~  (Grateful Dead)

"o puer, qui omnia nomini debes"; "You, boy, who owe's everything to a name"~ Mark Anthony

"Nihil est incertius vulgo, nihil obscurius voluntate hominum, nihil fallacius ratione tota comitiorum."; "Nothing is more unpredictable than the mob, nothing more obscure than public opinion, nothing more deceptive than the whole political system."~ Cicero


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InvisibleAdden
I'm a teapot
Registered: 06/04/03
Posts: 39,201
Loc: Flag
Re: Structure of ‘salvia’ Receptor Solved [Re: LongStrangeTrip]
    #15981146 - 03/22/12 12:41 PM (12 years, 9 days ago)

If this does truly have pain killing effects and more studies are done that prove Salvinorin-A assist in relieving chronic pain, you folks can expect this to reach Schedule I status so nobody but the pharmaceutical companies can touch it.

People said years ago "get your cuttings now".

Spring is in the air...


@tealeaf - Salvinorin-A was readily available through vendors long before most people knew what it was, including media, LEO, average drug user etc.

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Invisibleopenmind
curious
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Registered: 08/03/07
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Re: Structure of ‘salvia’ Receptor Solved [Re: LongStrangeTrip] * 1
    #15981628 - 03/22/12 02:20 PM (12 years, 9 days ago)

Quote:

LongStrangeTrip said:
Quote:

The downside of JDTic and similar drugs targeting KOR is that they can exert their actions for weeks, whereas most prescribed medicines are cleared within 18-24 hours. "Now that we have the [KOR] structure, it opens up the possibility for us to make drugs that have the same action as JDTic but have better pharmaceutical properties," said Roth.




This statement disturbs me.

Does anyone else feel like this? Seems that the reason a drug that exerts actions for weeks looks bad, compared to those that only do so for 18-24 hrs, because pharmaceutical companies are in the business of selling drugs.

God forbid we have something that necessitates 2 doses a month as opposed to 31 doses a month :suicide:






That was my first thoughts & reaction when I read that bit as well...






-OM

.


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Offlineaj123
smot poking
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Re: Structure of ‘salvia’ Receptor Solved [Re: openmind]
    #15982014 - 03/22/12 03:47 PM (12 years, 9 days ago)

I doubt its solely about money, what if someone was to react negatively to a drug that lasted weeks?


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OfflineKumara
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Registered: 02/24/09
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Last seen: 2 months, 11 days
Re: Structure of ‘salvia’ Receptor Solved [Re: Dest]
    #15982418 - 03/22/12 05:22 PM (12 years, 9 days ago)

Quote:

Dest said:
look at the reaction of someone on salvia extract, you will see what im getting at. their diaphram is stimulated (laughing) then the body's skeletal muscles are the next to go all wonky. you could say that its the brain on drugs frying like an egg like a politician. However involantary skeletal muscle movement I do not belive is a coinceidence.

here is a rather extreme case of the response people get from a drug.

This is repeatable science, smoke enough salvia and you will get involuntary movement from volantary organs in some way shape or form.





I don't think it's the salvia per se, when the body is relaxed enough or the "mind gets out of the way" so to speak, the body will move involuntarily.  Which is why meditation is so frightening and difficult for some people, letting go = losing control = the body doing something involuntary and "crazy".  There is a practice called "LifeStream" which teaches people to relax enough to allow the body to move involuntarily, releasing trapped feelings and trauma, completing incomplete movements, et cetera.

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OfflineKupo
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Registered: 08/07/08
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Re: Structure of ‘salvia’ Receptor Solved [Re: Jessica Swift]
    #15982919 - 03/22/12 07:06 PM (12 years, 9 days ago)

Salvia rocks.

That's all I have to add.

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OfflineKonyap


Registered: 06/30/07
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Loc: Planet Piss
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Re: Structure of ‘salvia’ Receptor Solved [Re: Kumara]
    #15983711 - 03/22/12 09:47 PM (12 years, 9 days ago)

hmm sometimes i go to sleep and i jolt or kick a little if im falling asleep if also noticed my dreams are wayy more tactile unlike the vivedness im used to.

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Invisiblevenetianblinds
cabbage


Registered: 05/25/11
Posts: 2,532
Loc: Flag
Re: Structure of ‘salvia’ Receptor Solved [Re: Konyap]
    #15984356 - 03/23/12 02:03 AM (12 years, 9 days ago)

id volunteer to expirimentally trip on salvia for a few weeks, in the name of science


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How do you know but ev’ry Bird that cuts the airy way,
Is an immense world of delight, clos’d by your senses five?

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