Skip to main page content
Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
, 30 (8), 1037-43

Agonistic Properties of Cannabidiol at 5-HT1a Receptors


Agonistic Properties of Cannabidiol at 5-HT1a Receptors

Ethan B Russo et al. Neurochem Res.


Cannabidiol (CBD) is a major, biologically active, but psycho-inactive component of cannabis. In this cell culture-based report, CBD is shown to displace the agonist, [3H]8-OH-DPAT from the cloned human 5-HT1a receptor in a concentration-dependent manner. In contrast, the major psychoactive component of cannabis, tetrahydrocannabinol (THC) does not displace agonist from the receptor in the same micromolar concentration range. In signal transduction studies, CBD acts as an agonist at the human 5-HT1a receptor as demonstrated in two related approaches. First, CBD increases [35S]GTPgammaS binding in this G protein coupled receptor system, as does the known agonist serotonin. Second, in this GPCR system, that is negatively coupled to cAMP production, both CBD and 5-HT decrease cAMP concentration at similar apparent levels of receptor occupancy, based upon displacement data. Preliminary comparative data is also presented from the cloned rat 5-HT2a receptor suggesting that CBD is active, but less so, relative to the human 5-HT1a receptor, in binding analyses. Overall, these studies demonstrate that CBD is a modest affinity agonist at the human 5-HT1a receptor. Additional work is required to compare CBD's potential at other serotonin receptors and in other species. Finally, the results indicate that cannabidiol may have interesting and useful potential beyond the realm of cannabinoid receptors.

Similar articles

See all similar articles

Cited by 136 PubMed Central articles

See all "Cited by" articles


    1. Neuro Endocrinol Lett. 2004 Feb-Apr;25(1-2):31-9 - PubMed
    1. Pain. 2004 Dec;112(3):299-306 - PubMed
    1. Pharmacol Ther. 1997;74(2):129-80 - PubMed
    1. Mult Scler. 2004 Aug;10(4):434-41 - PubMed
    1. Life Sci. 1998;63(1):PL1-6 - PubMed

Publication types


LinkOut - more resources