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The Endogenous Cannabinoids and the Control of Drug Craving Alexandros Makriyannis, Director
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9 / 8 -THC 9 -THC / 8 -THC 9 -tetrahydrocannabinol 8 -tetrahydrocannabinol
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Medicinal Uses for Cannabinoids AnalgesicAnticonvulsiveSedativeAntidepressiveHypnoticAntiasthmaticImmunomodulation Memory Enhancing Anesthetic Birth Control Appetite Stimulation Antipyretic Neuropathic Pain AntiemeticAntirheumaticAntimigraineAntineuralgic Reduction of Fatigue
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Two Cannabinoid Receptors: CB1 & CB2 174 179 CB2 e1 e2 e3 i1 i2 i3 Extracellular 472 amino acids 360 amino acids
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Endogenous Cannabinoid Receptor Ligands Anandamide2-Arachidonylglycerol Palmitylethanolamide CB2 72279 CB1CB2CB1 K i (nM) 58 145
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Cannabinoid Targets for Drug Discovery
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Nature Neuroscience, Vol. 2, 4, 304-5 (1999)
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Retrograde Signaling & the Cannabinergic System
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Purification of FAAH MW: 63 kDaMW: 63 kDa pI: 6.2pI: 6.2208144 87 44.1 32.7
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Inhibition of [ 3 H]anandamide accumulation by AM 404 and AM403 Science, Vol. 277, 1094-97 (1997) AM404 AM403
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Pharmacological Tools
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Cannabinergic Ligands O N H OH AM 251 Anandamides (AEA’s) AM356 1,5-Biarylpyrazoles 8 -THC Aminoalkylindoles(AAI’s) Non-Classical (NCC’s) AM630 OH OH O H Classical (CC’s) CP55,940
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