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3. Umbruch 4.4..2005 - Online Pot

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Cannabidiol as a potential medicine 51<br />

Table 2. Some actions of CBD expected to affect neurotransmission<br />

Action Tissue Effective concentration Reference<br />

Antagonism of cannabinoid CB1 receptor agonists Mouse vas deferens 120 nM (KB value) [47]<br />

Inhibition of Ca 2+ uptake Rat brainstem synaptosomes 100 nM [45]<br />

Inhibition of Ca 2+ uptake Mouse brain synaptosomes 1 µM [45]<br />

Inhibition of 5-HT uptake Rat hypothalamic synaptosomes 1 µM [41]<br />

Inhibition of dopamine and noradrenaline uptake Rat striatal or hypothalamic 1 µM [41, 49]<br />

synaptosomes<br />

Displacement of [ 3 H]SR-141716A from CB1 receptors CB1-containing membranes 1.26 µM (Ki value) [51]<br />

Displacement of 3 H-CP-55,940 from CB1 receptors CB1-containing membranes 2.28 µM (Ki value) [50, 51]<br />

4.35 µM (Ki value)<br />

Enhancement of evoked neuronal release of noradrenaline and ATP Mouse vas deferens <strong>3.</strong>2 µM [47]<br />

Inhibition of dopamine and noradrenaline uptake Mouse whole-brain synaptosomes 5 µM [46]<br />

Inhibition of 5-HT and GABA uptake Mouse whole-brain synaptosomes 10 µM [46]<br />

Enhancement of basal release of dopamine and noradrenaline Rat striatal and hypothalamic 10 µM [49]<br />

synaptosomes<br />

Antagonism of the cannabinoid CB1 receptor agonist CP-55,940 Rat cerebellar membranes 10 µM [48]<br />

Inhibition of choline uptake Rat hippocampal crude synaptosomal 16 µM (EC50) [28]<br />

fraction<br />

Inhibition of anandamide uptake RBL-2H3 cells 22 µM (EC50) [42]<br />

Inhibition of anandamide metabolism N18TG2 cell membranes 27.5 µM (EC50) [42]<br />

Attenuation of the affinity of dopamine D2 receptor ligands for D2 Mouse striatal membranes 30 µM [43, 44]<br />

receptors<br />

GABA, γ-aminobutyric acid; 5-HT, 5-hydroxytryptamine.

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