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Pharmacological Characterization of Minor Cannabinoid Constituents
Author(s) -
ElAlfy Abir,
Ross Samir,
Childress Suzanne,
Wilson Lisa,
Xu Yan Tong,
Viard Eddy,
Viard Eddy,
Radwan Mohamed,
Ahmed Safwat,
Slade Desmond,
ElSohly Mahmoud,
Matsumoto Rae
Publication year - 2008
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.22.2_supplement.622
Subject(s) - cannabinoid receptor , cannabinoid , catalepsy , pharmacology , chemistry , radioligand , receptor , cannabinoid receptor type 2 , analgesic , cannabinoid receptor antagonist , cannabis , medicine , biochemistry , antagonist , dopamine , haloperidol , psychiatry
The goal of this study was to evaluate the pharmacological actions of several poorly characterized cannabinoid constituents isolated from Cannabis. Sixteen hydroxylated cannabinoids were isolated from Cannabis extract and identified using standard NMR techniques. The identified compounds were then evaluated in CB1 receptor binding assays using rat brain homogenates and [ 3 H]CP55,940 as the radioligand. The CB1 receptor binding assay showed that a few of the isolated compounds exhibited moderate affinities to the CB1 receptors with Ki values ranging from 200 to 800 nM. These compounds were evaluated using male Swiss Webster mice in the established tetrad assay. In this assay, the cannabinoid receptor agonists Δ 9 ‐THC and CP55,940 caused a dose dependent reduction in locomotor activity, catalepsy, hypothermia, as well as antinociception. Four compounds showed significant cannabinoid‐like activity comparable to that of Δ 9 ‐THC. The Δ 9 ‐THC analog SAA‐52‐38 demonstrated significant analgesic, cataleptic, as well as hypothermic actions at 10 and 20 mg/kg doses ( p<0.001 ). Similarly, the Δ 8 ‐THC analogs MRRoss‐01‐45‐28‐46 and SAA‐53‐20 showed significant cannabinoid‐like activity ( p<0.001 and p<0.01 respectively). Current studies are underway to further characterize the therapeutic potential of these as well as other cannabinoids. Grant Number P20RR021929 from the National Center for Research Resources.