Anandamide (endocannabinoid), CB1-receptors and TRPV1-receptors

[Function]

Hello everyone

 

It is known that anandamide, an endocannabinoid, binds to CB1-receptors, thus taking part in pain relief.

 

However, it also binds to the TRPV1-nociceptor, inducing a burning pain as is experienced with temperatures above 43°C (or so).

 

So ... Imagine I inject some anadamide (1) intradermal and (2) intravenous.

 

Will you get high and sedated or will you curse me to death?

 

Thanks!

 

F

[The_Platypus]

It will certainly lead to euphoria/ dysphoria in either of the two routes of administration . We can only guess that intradermal route would be more painful. Also , TRPV1 regulates temp , sweating would definitely follow .

 

I believe one would have an unpleasant experience if it were to be given by that route .

[Function]

I asked a professor (neurologist) specialized in pain systems who taught us these pain principles; and he told me after the class that indeed the mechanism of anandamide is not fully understood yet, that it is very dependent from person to person what will happen

[Xalatan]

You may have to look at the distribution of the receptors in the body, and the route of your drug administration. TRPV1 is typically a heat/acid/capsaicin receptor, so you'd think they occur peripherally in the first order neurons rather than in the CNS. CB1 may be more CNS-distributed given its psychotropic effects.

 

So if you injected intradermally, you may elicit a stronger TRPV1 response relative to the CB1 response. If you gave the drug systemically, if it crosses the blood brain barrier you may get more of a CB1 response.