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The Endogenous Cannabinoids and the Control of Drug Craving

The Endogenous Cannabinoids and the Control of Drug Craving. Alexandros Makriyannis, Director. D 9 - THC / D 8 -THC. (-)D 9 -tetrahydrocannabinol. (-)D 8 -tetrahydrocannabinol. Medicinal Uses for Cannabinoids. Analgesic Anticonvulsive Sedative Antidepressive Hypnotic Antiasthmatic.

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The Endogenous Cannabinoids and the Control of Drug Craving

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  1. The Endogenous Cannabinoids and the Control of Drug Craving Alexandros Makriyannis, Director

  2. D9-THC / D8-THC (-)D9-tetrahydrocannabinol (-)D8-tetrahydrocannabinol

  3. Medicinal Uses for Cannabinoids Analgesic Anticonvulsive Sedative Antidepressive Hypnotic Antiasthmatic Immunomodulation Memory Enhancing Anesthetic Birth Control Appetite Stimulation Antipyretic Neuropathic Pain Antiemetic Antirheumatic Antimigraine Antineuralgic Reduction of Fatigue

  4. 264 e2 e3 e1 257 i1 i2 i3 CB1 Two Cannabinoid Receptors: CB1 & CB2 Extracellular 179 e2 e3 174 e1 i1 i2 i3 CB2 472 amino acids 360 amino acids

  5. Endogenous Cannabinoid Receptor Ligands Anandamide 2-Arachidonylglycerol CB1 CB2 CB1 CB2 Ki (nM) 58 145 72 279 Palmitylethanolamide

  6. CB1/CB2 DAG biological AEA 2 - AG actions DAG - L AEA 2 - AG AEA AEA AT AEA PLD AEA NAPE AEA NAT AEA FAAH DPPE AA + extracellular space ethanolamine

  7. Cannabinoid Targets for Drug Discovery

  8. Nature Neuroscience, Vol. 2, 4, 304-5 (1999)

  9. Retrograde Signaling & the Cannabinergic System

  10. 208 144 87 44.1 Purification of FAAH • MW: 63 kDa • pI: 6.2 32.7

  11. AM404 AM403 Inhibition of [3H]anandamide accumulation by AM 404 and AM403 Science, Vol. 277, 1094-97 (1997)

  12. Pharmacological Tools

  13. O O H N H O H O H H O Cannabinergic Ligands D8-THC AM356 Anandamides (AEA’s) Classical (CC’s) CP55,940 Non-Classical (NCC’s) AM630 AM 251 Aminoalkylindoles(AAI’s) 1,5-Biarylpyrazoles

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