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Capsazepine, what can you tell me about it?

I am curious about this chemical and its effects. I like chillis and capsaicin is the chemical that gives chillis thier heat. Capsazepine is a synthetic anologue of capsaicin as well as an antagonist of it. I havn't found much information on it (I'm on my school wifi and most stuff is blocked) apart from this article (http://www.ncbi.nlm....les/PMC3176404/) that suggests it has the opposite effect as capsaicin.

So, I was wondering if someone were to have a little bit diluted in ethanol (this is what you must do to make capsaicin hot) would it make your mouth feel cold?
 
 
does this stuff have any commercial uses? if so you should pursue a commercial supply rout first.
do NOT approach any chemical supply houses like sigma or who ever is in Au. do not try any fake letterhead bullshit.

im guessing this stuff is made in insanely small quantities. it could even be just synthesized in situ, within w/e research lab is studying it. idk. you will have to evaulate this yourself.

personally i would not even waste my time with this, its almost certainly not accessible to anyone but... department heads at some university or w/e research lab has grants to study crap like this.

idk tho, maby theres some wide use for it im not aware of.
 
In answer to your question, No. However, it may switch off activated receptors for Capsaicin, depending on the kinetics of the reaction, association and dissociation constants, binding affinity etc. The paper suggests that this is the case in the insects studied.
 
As you probably know, a receptor agonist is a substance that activates the receptor and you get whatever effects that receptor mediates. In this case the sense of heat. An antagonist blocks the effects of an agonist, so Capsazepine will bind to the receptor and not allow any agonists to activate it. So, if your mouth was on fire after eating the next worlds hottest chili, having some Capsazepine might switch off the pain and heat, so in that sense it would cool you down. On it`s own it would not give you a cool feeling, as the capsaicin receptors do not mediate the sensing of cold. 
 
Make sense? 

So I just read a few papers and Capsazepine can also act as an antagonist to receptors that mediate the feeling of cold, so it can block both the feeling of heat and the feeling of cold. 
 
I don't think it does but it if it were to become popular i assume chilli lovers would use it as a chaser. Thanks nigel, but what about this Capsazepine in low concentration (10−7 M) affected the insects’ thermoregulation in an opposite way to capsaicin in low concentration. The mealworms intoxicated with capsazepine preferred staying at warmer parts of the gradient (22.47 ± 1.27°C) (Fig. 1), especially in the first 24 h of the experiment (23.55 ± 0.78°C; P = 0.001) (Fig. 3). On the other hand, the insects intoxicated with capsazepine in high concentration (10−4 M) stayed at the lowest temperatures (18.25 ± 0.77°C) (Fig. 2).
and this
Here, we report that capsazepine in a concentration of 10−7 M affects insect behavioral thermoregulation, inducing selection of warm temperatures. The observed opposite effect of capsaicin and capsazepine in the same concentration on the mealworms’ thermoregulation may suggest that the tested substances act as agonist–antagonist presumably on the same structure. We suppose that this may be a receptor functionally similar to mammalian TRPV1.
So it could one day be used in cooking to create a cool sensation. What do you think?

Quee, yeah , I'll keep my wits about me and try and talk to some guys on another forum i know (longecity) see if they can get some for me.
 
ThePurpleWiggle said:
I don't think it does but it if it were to become popular i assume chilli lovers would use it as a chaser. Thanks nigel, but what about this Capsazepine in low concentration (10−7 M) affected the insects’ thermoregulation in an opposite way to capsaicin in low concentration. The mealworms intoxicated with capsazepine preferred staying at warmer parts of the gradient (22.47 ± 1.27°C) (Fig. 1), especially in the first 24 h of the experiment (23.55 ± 0.78°C; P = 0.001) (Fig. 3). On the other hand, the insects intoxicated with capsazepine in high concentration (10−4 M) stayed at the lowest temperatures (18.25 ± 0.77°C) (Fig. 2).
and this
Here, we report that capsazepine in a concentration of 10−7 M affects insect behavioral thermoregulation, inducing selection of warm temperatures. The observed opposite effect of capsaicin and capsazepine in the same concentration on the mealworms’ thermoregulation may suggest that the tested substances act as agonist–antagonist presumably on the same structure. We suppose that this may be a receptor functionally similar to mammalian TRPV1.
So it could one day be used in cooking to create a cool sensation. What do you think?


Quee, yeah , I'll keep my wits about me and try and talk to some guys on another forum i know (longecity) see if they can get some for me.
 
Sure, it could be used to chase away the effects of capsaicin if all the reaction kinetics played along, and assuming it was safe for humans to take, obviously. 
 
Many pharmacological papers highlights a typical problem with taking in vitro data (Capsazepine binding to various heat/cold receptors in the lab or in cell lines) and then putting the compound into whole animals, i.e. in vivo. This sort of thing happens all the time in pharmacology and is very often dose-dependent. The problem is specificity, or lack thereof and it is something you cannot predict. That`s why everything is tested in vivo (usually mice, rats, dogs, worms, then eventually, humans) before being made available for the general public and why, as much as the scientists would like, you can`t duplicate effects on whole animals with the use of cultured cells. 
 
However, in this case, the data seem fairly clear for low concentrations. If you partially block heat receptors, the worms can`t sense heat as well, whether it be from capsaicin or the environment. So they go and seek out someplace where there`s more heat. Conversely, if you partially stimulate the heat receptors (with capsaicin), the worms seek out a cooler environment because they sense the extra heat caused by capsaicin. For the case of high concentrations, it`s harder to assess because as the concentration gets higher all sorts of non-specific effects come into play. One of those is the reported ability of Capsazepine to block cold-receptors as well as heat-receptors. It may be that the high doses are required to act on the cold-receptors in addition to the heat-receptors, thereby resulting in a mixed effect or one that favours blocking the cold-receptors. With in vivo data like this it`s impossible to know.
 
I don`t know for sure whether Capsazepine would cause a cool sensation in the mouth, but I doubt it. It could block the feeling of heat, but that isn`t necessarily the same thing. To get a feeling of cold, you`d probably want to activate the cold-receptors, not block the heat-receptors.
 
An excellent idea Aussie. I suppose I'll scrap this idea for now at least. The reason for my interest in this chemical is that in my life I want to have as many interesting/awesome experiences (not necessarily pleasant) as I can and this seems interesting.
 
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