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. 2020 Dec 24;22(1):134. doi: 10.3390/ijms22010134

Table 1.

Cannabidiol (CBD) binding profiles in in vitro binding assays for the receptors or functional molecules involved in drug abuse and addiction.

Target Function CBD Action References
CB1 Antagonist Low affinity to CB1Rs in [3H]CP55940 binding assay (Ki = 3.3~4.9 μM);
↓ CP55940-enhanced GTPγS binding (KB = 79 nM);
↓ CP55940-induced inhibition of cAMP formation (KB = 545 nM);
↓ CP55940-induced β-arrestin recruitmrnt in CB1-expressing
HEK-CRE cells (KB = 547 nM)		 [41,42]
NAM ↓ Δ9-THC- or 2-AG efficacy and potency on arrestin2, PLCβ3 and ERK1/2 signaling in CB1-expressing HEK 293A cells (IC50 = 0.27~0.96 μM) [43]
CB2 Antagonist Low affinity to CB2Rs in [3H]CP55940 or [3H]WIN55212-2 binding assays
(CBD-Ki = 4.2 μM vs. ∆9-THC-Ki = 3.3 μM)
↓ CP55940-enahnced GTPγS binding in CB2-expressing CHO cells
(KB = 65 nM)
↓ CP55940-induced inhibition of cAMP formation (KB = 641 nM);
↓ CP55940-induced β-arrestin recruitmrnt in CB2-expressing HEK-CRE cells (KB = 420 nM);		 [41,42,44,45]
NAM ↓ JWH133-induced reduction in forskolin-stimulated cAMP formation
(IC50 = 3 nM)
↓ JWH133-induced ERK1/2 phosphorylation in HEK cells expressed hCB2 (IC50 = 29 nM)		 [44]
Inverse agonist ↓ GTPγS binding in CB2-expressing CHO cells
(EC50 = 503 nM)		 [41]
Partial agonist Unexpectedly high affinity to CB2Rs in [3H]CP55940 binding assays
(CBD-Ki = 34 nM vs. ∆9-THC-Ki = 15 nM)
↑ BRET response, ↑ intracellular CRE activity in CRE and BRET assays
in CB2-expressing HEK cells		 [42]
GPR55 Antagonist ↓ CP55940-enhanced GTPγS binding in GPR55-expressing cells (IC50 = 445 nM) [45]
TRPV1 Agonist ↑ [Ca++] levels in TRPV1-expressing HEK 293 cells (EC50 = 3.5 μM) [46]
FAAH Inhibitor ↓ [14C] AEA update in N18TG2 cells (IC50 = 27.5 µM)
↓ [14C] AEA update in HeLa cells expressing rat, but not human, FAAH at 50–200 μM		 [46,47]
5-HT1A Agonist ↓ [3H]8-OH-DPAT binding;
↑ GTPγS binding in 5-HT1A-expressing CHO cells 		[48]
D2 Partial agonist ↓ [3H]domperidone binding to D2 receptors (Ki = 11 nM at D2High; Ki = 2800 nm at D2Low) [45]
MOR & DOR Allosteric modulator ↓ [3DNM] binding to MOR (IC50 = 7 μM)
At 100 μM, ↑ [3H]DAMGO dissociation from MOR (pE50 = 4.38 μM)
↑ [3H]-naltrindole dissociation from DOR (pE50 = 4.1 μM)		 [49,50]

CRE, cAMP response element; BRET, bioluminescence resonance energy transfer.

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