• N&PD Moderators: Skorpio | thegreenhand

cannabinoid receptor type 1 inverse agonist / discussion of falcarinol

Falcarinol: need more information on this chemical specifically of this reason; It is structurally related to the oenanthotoxin and cicutoxin.
now, why would that matter? it is present in carrots and its relation to those two toxins is not very comfortable considering; noncompetitive gamma-aminobutyric acid (GABA) antagonist & potent, noncompetitive antagonist of the gamma-aminobutyric acid (GABA) receptor !
now, i understand the amount in carrots is minimum BUT when i am withdrawing from benzos or alcohol, i feel like ill get a seizure consuming carrots. and i know, its just perhaps one thing out of many i concentrate on when in fact ANYTHING can be a factor when withdrawing from benzos or alcohol. BUT, i can feel i am onto something unique here... please help me out a bit, thanks!
 
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Like rimonabant times 10.

Inverse agonists produce the opposite effect. Antagonists just block the receptor.
 
rimonabant... was withdrawn worldwide in 2008 due to serious psychiatric side effects. yikes
are those type of inverse agonists THAT horrible? main reason i posted asking this, concerns carrots and more specifically, a chemical called falcarinol which is actually considered an inverse agonist of the cannabinoid receptor. something to start thinking about now...
 
With that single mechanism, most would likely experience intense dysphoria. Carrots don't have that much in them/are countered by other phytochemicals. They're suppsoed to be good for the eyes, but if you eat too much you'll turn orangish--no joke, it happens.
 
uhm yeah turning orange. thats not important at all. how do you know they dont have enough thats bioavailable? from what i read, they have a decent amount and this chemical is potent, very bioavailable. perhaps the dietary fiber might slow down its bioavailability a bit but i cannot see anything else stopping it from completely entering our blood stream. as far as i know, im the first person ever to notice carrots arent some innocent little vegetable for the kids. this stuff harbours some serious chemicals in there which might be detrimental to health. as i mentioned in the other thread about falcarinol, i would get really shakey and uncomfortable especially when consumed while withdrawing from drugs and alcohol
 
as far as i know, im the first person ever to notice carrots arent some innocent little vegetable

You definitely aren't the first to see through the misconception that all veggies are good and completely harmless. Probably part of the reason for the all carnivore diet, a big contrast to the all veggie diet trend a few years ago. Many foods are/can become poisonous if not stored or prepared correctly.

I think you are bordering on fearmongering without presenting the facts yourself, requiring others to prove that there isn't enough bioavailable to not have major effects. There are enough case studies of people eating carrots without any noticeable health concerns, although too much is definitely known to be bad, as I've had a vegetarian friend who was told by her doctor she needs to eat meat(not sure of her specific condition).
 
yeah, good you posted this link, but i already have researched all this and i knew of all those problems regarding vegetables.
anyway, carrots are not on the list and are highly underestimated. im surprised that nobody who has been eating them reported any ill effects. perhaps because hardly anyone eats too much of them to report problems? in that case, i should ask the bunnies!?
anyway, i have always been noticing some dissociative weird effects from eating carrots even in normal doses and i never thought much of it until i started researching them better and it was difficult at first. google keeps posting POSITIVE TOPICS REGARDING ALL VEGETABLES so i was never fully able to get any good reliable information on them until recently! they contain several interesting, requiring further analyses chemicals out of aforementioned falcarinol. something to research further, and discuss deeper. i even posted seperated thread about falcarinol that nobody yet has responded. it speaks in volumes of people's ignorance of serious shit we consume on daily basis without acknowledging the impact. please, if anyone reads this, try to take a bit of time to research and comeback to me please, thanks!
 
i already have researched all this and i knew of all those problems regarding vegetables.
anyway, carrots are not on the list and are highly underestimated. im surprised that nobody who has been eating them reported any ill effects. perhaps because hardly anyone eats too much of them to report problems? in that case, i should ask the bunnies!?
If you've already done the research, why don't you share that research? Here, let me do a little bit for you maybe to lessen your worries in my boredom.
"In carrots, it occurs in a concentration of approximately 2 mg/kg.[1][2].
As a toxin, it protects roots from fungal diseases, such as liquorice rot that causes black spots on the roots during storage. The compound requires the freezing condition to maintain well because it is sensitive to light and heat.

Falcarinol was also credited for helping to prevent colon cancer.[3]"

All in the first lines of wiki, and if you follow the links, especially the last one:

"One of these groups of compounds is aliphatic C17-polyacetylenes of the falcarinol-type (Figure (Figure1)1) (713), which are common in carrots and related vegetables such as parsley, celery, parsnip, and fennel (10,11,14) as well as in medicinal plants such as ginseng (15,16). Polyacetylenes of the falcarinol-type have shown many interesting bioactivities including anti-inflammatory (11,13,16), antiplatelet-aggregatory11,1618, cytotoxic (10,11,16,19,20), and antitumor activity (9,22) as well as activity against bacteria and mycoplasma (21). Falcarinol appears to be the most bioactive among polyacetylenes of the falcarinol-type. The bioactivity of falcarinol is probably associated with its hydrophobicity and its ability to form an extremely stable carbocation with the loss of water, thereby acting as a very reactive alkylating agent toward various biomolecules (9,11). This is supported by the fact that falcarinol is a strong contact allergen (23). A similar mode of action is expected for other falcarinol-type polyacetylenes with a hydroxyl group at C-3 (9,11).

The beneficial effects of polyacetylenes of the falcarinol-type occur at nontoxic concentrations and thus represent pharmacologically useful properties indicating that polyacetylenes may be important nutraceuticals of vegetables. In the human diet, carrots are the major dietary source of falcarinol-type polyacetylenes, in particular falcarinol and falcarindiol (8,13,14). It has been demonstrated that falcarinol but not β-carotene could stimulate differentiation of primary mammalian cells of mammary origin in concentrations between 1 ng/mL and 10 ng/mL falcarinol. Toxic effects were found >50 ng/mL falcarinol."

So there's the info you need to determine the safe amount of carrots for you, based on your body weight. And believe it or not, many health benefits are found from falcarinol in non-toxic doses. Even anti-tumor properties have been found.

Also, maybe look into antinutrients(from wiki):
"
Antinutrients are found at some level in almost all foods for a variety of reasons. However, their levels are reduced in modern crops, probably as an outcome of the process of domestication.[24] The possibility now exists to eliminate antinutrients entirely using genetic engineering; but, since these compounds may also have beneficial effects, such genetic modifications could make the foods more nutritious but not improve people's health.[25]

Many traditional methods of food preparation such as fermentation, cooking, and malting increase the nutritive quality of plant foods through reducing certain antinutrients such as phytic acid, polyphenols, and oxalic acid.[26] Such processing methods are widely used in societies where cereals and legumes form a major part of the diet.[27][28] An important example of such processing is the fermentation of cassava to produce cassava flour: this fermentation reduces the levels of both toxins and antinutrients in the tuber.[29]"

As with all chemicals, the poison is in the dose, and often the difference between poison and medicine is the dose.
 
*sigh* a bit off topic here posting all this, but yes, i have already seen the wiki article on falcarinol. BUT since its not being researched enough yet, thats why im posting here for more information beyond just having you or someone paste whatever is already available about it. i wish we can go into detail about it a bit more on its own thread that i made https://www.bluelight.org/xf/threads/falcarinol-id-this-chemical-better-please.879679/ but here im more concerned with the cannabinoid type 1 inverse agonism and the effects from that.
To be continued this in the falcarinol thread; "It was shown that falcarinol acts as a covalent cannabinoid receptor type 1 inverse agonist and blocks the effect of anandamide in keratinocytes, leading to pro-allergic effects in human skin" i wish there is further explanation about this somewhere... but there isnt.
Also, very important to note "It is structurally related to the oenanthotoxin and cicutoxin" Now thats fucked up if you check what those toxins actually DO. They are; noncompetitive gamma-aminobutyric acid (GABA) antagonists! So, how close is it to being like them in that regard, its not explained at all. I wish people research this better and report. Its quite vital to know this! And yet, nobody has researched it any further and knows anything besides pasting the wiki article.
ALSO not well explained is what does 'normal' consumption constitutes of? one, two, three or ten carrots? i would think cooking them is a good idea since it destroys the falcarinol. so at least that is something interesting i have learned thus far into researching this chemical. And it seems so far to be best way to avoid it. But I am still striving on understanding better how detrimental is it actually to human health and at what amount exactly?? Nowhere has it been researched yet to be explained...
anyway, can we try to gather NEW important information about it regarding its cannabinoid receptor type 1 inverse agonist effect most specifically? Thats all i wish for in this specific thread.
 
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We don't need two threads for falcarinol. I'm sure this thread can handle the range of discussion on the topic.
 
uhm yeah turning orange. thats not important at all.

I don't know if this is sarcastic or not, but it surely isn't normal, suffice to say. But you'd need a heck of a lot of carrot.

how do you know they dont have enough thats bioavailable?

I've been around the block, never a whisper about this sort of thing.

from what i read, they have a decent amount and this chemical is potent, very bioavailable. perhaps the dietary fiber might slow down its bioavailability a bit but i cannot see anything else stopping it from completely entering our blood stream. as far as i know, im the first person ever to notice carrots arent some innocent little vegetable for the kids.

Enlighten us with your convincing sources, then. But then again you couldn't be the first person to have this idea, otherworldly as it seems. Bupropion is structurally similar to methcathinone. Different ballgames.

this stuff harbours some serious chemicals in there which might be detrimental to health. as i mentioned in the other thread about falcarinol, i would get really shakey and uncomfortable especially when consumed while withdrawing from drugs and alcohol

And you attribute this to carrots, not drug withdrawal? This is a subjective case study with heavy conflict of interest. Where was the scientifically rigorous literature you promised us?
 
alphadude, ill only say this about the effect it has on me when withdrawing from benzos. Yes, it is the withdraw process itself thats causing problems obviously, of course! BUT if you have been through any withdrawal you will know some things for consumption are taboo for your own good if you want to get better that is.
for one, when you withdraw from benzos , you do not consume stimulants or you will get a seizure. its a fact! or consume any type of shit that fucks with your GABA as in case here of carrots containing such compounds. It goes same way with coffee, energy drinks, any stimulants in fact. But also with various drugs, herbals and some foods ive noticed. but most importantly, DO NOT FUCK WITH GABA on benzo wd!!! cannot stress that hard enough!!!!
so anyway, only food ive noticed to cause serious problems with benzo wd, are carrots! and i always thought i just didnt process this right it cannot be. its just a damn fucking vegetable that health guru moms rant about at events and tea parties how high in antioxidants it is and whats the latest dish you can make out of it blah blah. BUT it seems to have much more depth than most of you can so far be any interested in understanding better. And, I didnt either, Until I checked in depth their chemical profile and found out those compounds discussed here.
anyway, i wish you guys work with me here and help me as much as possible please, thanks
 
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carrots are not on the list and are highly underestimated. im surprised that nobody who has been eating them reported any ill effects. perhaps because hardly anyone eats too much of them to report problems?

It may be because it's not a problem, not present in enough volume to produce negative effects, in any ordinary level of carrot consumption. Perhaps if you sat down with 10 pounds of carrots and moshed them down all at once, something would happen, but no one does that.

Consider that benzo withdrawal produces psychiatric disturbances, paranoia and psychosis, all on its own. From what I understand, it's about as bad as withdrawal gets. I've seen loved ones get seriously fucked up in the head from benzo withdrawal.

I mean if you have links to research about controlled experiments with carrot consumption and negative effects resulting from it, I would love to see it. But I think you're fixating on something unrelated to the cause of your suffering. If you're withdrawing from benzos, you don't need another reason to explain your suffering.

I'm not trying to be dismissive or disrespectful. If you have done the research, then please share it here. I'm open to you being right but you saying "trust me I did the research" isn't an argument I can accept, from anyone.
 
well, how am i suppose to prove it? perhaps wait several days for benzos to clear off my system and eat few carrots live on cam and then see how i react? would that be scientific proof? im pretty certain nobody in the world will ever think of testing carrot compounds in inducind seizures in rats or anything. whats their motivation and benefit?
but cant you follow basic biochemistry knowledge here when i post to you the mechanism by which falcarinol works? obviously it screws with the GABA receptors in a bad way. there is literature on what it does, there is no literature on actually proving it. im not sure it will ever be done though
 
just looking at the structure of falcarinol suggests to me it'd be a low BA due to extensive metabolism... note it's not stable to heat and light

and given it's present at 2mg/kg of raw carrot you'd probably have to ingest many pounds of carrot... I don't think there have been any reliable reports of toxicity and indeed wikipedia suggests "no toxicity is observed by the normal consumption of carrots".
 
just looking at its structure, it reminds you of low BA?? whats BA?
yeah, i know its not stable to heat hence while many cuisines incorporate it cooked. same with spaniach, its healthier this way. but lets say you want raw juice from carrots, it will take a pound to make 1-2 glasses of the stuff. so when you prepare juice from it, its very much more likely to get toxic amounts of falcarinol in you, isnt there?
 
BA = bioavailibility.

And given that falcarinol is also very nonpolar, I would think it would not be very water soluble either. So consuminng whole raw carrot, or cold oil/solvent extraction of carrot meal (if you would attempt such a thing) would be routes of concern.
 
well yeah, carotenoids are hardly bioavailable in water. thats why i used to chug at least maybe 10 carrots in juice with oil. so i suppose the possibility for toxicity is real then? shit! i can obviously feel something screwing with me with those carrots when you are hooked on benzos and alcohol. nobody STILL believes me. there should be more awareness of this!
 
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