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Next, the binding kinetics of all compounds were determined using the high throughput dual-point competition association assay, yielding Kinetic Rate Index (KRI) values that

Black arrowheads: excitatory synapses; white arrow- heads: inhibitory synapses; black thin arrows: neuronal CB 1 receptor immunoparticles; black thick arrows: astrocytic CB 1

The data in Table 2 indicate that an exchange of the amide moiety (NHC(=O)) of 7a by an aminomethylene (NHCH 2 ) moiety (23a) only slightly increased the metabolic stability

The resulting mixture was extracted with Et 2 O ( ×2), and the combined organic phases were washed with brine, dried (MgSO 4 ), filtered, and concentrated in vacuo to yield the

Water (5 mL) was added, the reaction mixture was concentrated in vacuo and the residue was dissolved in ethyl acetate (300 mL)... The reaction mixture was heated at reflux for

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However, by adjusting the cooperativity parameters  and , an allosteric ligand may increase the basal activity of the receptor as well as the potency of the endogenous ligand

Subsequently, the short RT antagonists (6 and rimonabant) and long RT antagonist (9) were functionally characterized in hCB1 receptor agonist-induced [ 35 S]GTP c S binding and