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Structures and affinity and relative efficacy data for the conformationally restricted anandamide analogs |
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| Compound |
Binding affinity, Ki(nM) |
GTPγS binding |
Adenylyl cyclase |
|
|
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| CP55244 |
0.11 |
Strong stimulation |
Strong inhibition |
| Anandamide |
17 |
Strong stimulation |
Strong inhibition |
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38 |
Strong stimulation |
Strong inhibition |
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59 |
Moderate stimulation |
Weak stimulation |
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305 |
Moderate stimulation |
Weak stimulation |
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335 |
Strong stimulation |
Moderate Inhibition |
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371 |
Moderate stimulation |
Weak stimulation |
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4960 |
No change |
Strong inhibition |
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Anandamide analogs were selected from a series of compounds developed and tested as reported previously [13]. Binding affinity was determined by the ability to compete for [3H]-CP55940 binding in rat brain membranes, G-protein activation was determined by the ability to stimulate [35S]-GTPγS binding to G-proteins in rat brain membranes, and effector activity was determined by the ability to regulate adenylyl cyclase activity (inhibit through Gi or stimulate through Gs) in purified membranes from N18TG2 cells. | |||
Padgett et al. Journal of Molecular Signaling 2008 3:5 doi:10.1186/1750-2187-3-5 |
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