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Old 11-22-2011, 04:22 AM #1
mofeta
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Excellent Paper on Cannabinoid Pharmacology

Here is a link to an excellent paper on cannabinoid pharmacology:

The diverse CB1 and CB2 receptor pharmacology of
three plant cannabinoids: D9-tetrahydrocannabinol,
cannabidiol and D9-tetrahydrocannabivarin


thaistix's binned thread inspired me to post this, it is very interesting.
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Old 11-22-2011, 04:41 AM #2
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Once you read the above paper, you would never make a comment like this:

Quote:
Originally Posted by noob
CBD is old news
CBD is hardly "old news", I know Chimera has pointed this out somewhere before. Our understanding of it's effects on various receptors (known and undiscovered), is primitive, and the study of it is bleeding edge science. To refer to it as "old news" shows a lack of understanding at the most basic level.

Or like this:

Quote:
Originally Posted by noob
CBD is a great cannabinoid because it activates the CB2 receptor without getting you high.
This is simplistic (and incorrect) to the point of being meaningless. The term "activate", in the context of neurochemistry, refers to agonism. Although we can't totally rule it out, any agonism of the CB2 receptor by CBD is miniscule. The important effects of CBD on CB2 (and CB1, as Chimera has pointed out) is the antagonistic effect on CB1 AND CB2 receptor agonists. So, CBD has very low affinity for CB1 and CB2 receptors, but has a fairly powerful indirectly antagonistic effect, not agonism (activation) on BOTH receptors. It also has a inverse agonism on CB2, that is thought to be part of the mechinism behind it's anti-inflammatory properties. For your edification:

agonist: binds to receptor and activates it
antagonist: binds to receptor and does not activate it
inverse agonist: binds to receptor and has "opposite" effect as activation

terms/concepts for you to look up: binding affinity, efficacy, half maximal effective concentration (EC50), constitutive activity. Remember to find the definitions specifically intended for discussing receptors, all these terms have a very exact definition in this context, and discussing these concepts is impossible without employing a very strict terminology.

And, once again, as Chimera has pointed out before, the really interesting recent developments with CBD have to do with it binding other receptors, like 5HT, GPR55 and GPR18 to name a few. Old news, eh?

More incorrectness:

Quote:
Originally Posted by noob
CBG activates both the CB1 AND the CB2 receptor without getting you high !!!!!!
This is inaccurate in a similar way to the above about CBD. CBG has only weak affinity for CB1 and CB2, it is antagonistic, not "activating" at these receptors, and its most interesting properties are those that deal with its effects on other receptors, namely it's alpha adrenergic agonism and 5HT1A antagonism.

So, read the paper linked above, look for and read similar papers. Most of all, study the fundemental concepts/terminology necessary for understanding this stuff, and to allow you to have proper discourse on the subject.
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