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Alexandros Makriyannis is the director of the Center for Drug Discovery, which is a research group at the University of Connecticut who have synthesized many new compounds with cannabinoid activity. Some of those are: AM-087 — an analgesic CB1 agonist derived from Δ8THC substituted with a side chain on the 3-position, it has a Ki of 0.43nM making it roughly 100x as potent as THC. AM-251 — an inverse agonist at the CB1 cannabinoid receptor that is structurally related to SR141716A (rimonabant), but has a higher binding affinity with a Ki value of 7.5nM.[1] AM-281 — N-(morpholin-4-yl)-1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-1H-pyrazole-3-carboxamide[1] AM-356 — a synthetically-created stable chiral analog of anandamide, it acts on the cannabinoid receptors with a Ki of 17.9nM at CB1 and 868nM at CB2.[2] AM-374 — palmitylsulfonyl fluoride[3] AM-381 — stearylsulfonyl fluoride AM-404 — an active metabolite of paracetamol (acetaminophen) and a likely inhibitor of fatty acid amide hydrolase (FAAH) AM-411 — an adamantyl-substituted derivative of Δ8THC, it is a potent and fairly selective CB1 full agonist with a Ki of 6.80nM. It is also a moderately potent CB2 agonist with a Ki of 52.0nM. AM-630 — a potent and selective inverse agonist for the cannabinoid receptor CB2, with a Ki of 32.1nM at CB2 and 165x selectivity over CB1, at which it acts as a weak partial agonist. AM-661 — 1-(N-methyl-2-piperidine)methyl-2-methyl-3-(2-iodo)benzoylindole[4] AM-678 — another name for JWH-018, it is a full agonist at both cannabinoid receptors with some selectivity for CB2. AM-679 — an iodobenzoylindole which acts as a moderately potent agonist for the cannabinoid receptors, with a Ki of 13.5nM at CB1 and 49.5nM at CB2. AM-694 — an iodobenzoylindole which acts as a potent and selective agonist for the CB1 cannabinoid receptor, with a Ki of 0.08nM at CB1 and 18x selectivity over the related CB2 receptor (1.44nM).[5] AM-855 — an analgesic derivative of Δ8tetrahydrocannabinol, it is an agonist at both CB1 and CB2 with moderate selectivity for CB1, with a Ki of 22.3nM at CB1 and 58.6nM at CB2. AM-881 — a chlorine-substituted stereoisomer of anandamide whose Ki = 5.3nM at CB1 and 95nM at CB2.[2] AM-883 — an allyl-substituted stereoisomer of anandamide whose Ki = 9.9nM at CB1 and 226nM at CB2.[2] AM-905 — a potent and reasonably selective agonist for the CB1 cannabinoid receptor, with a Ki of 1.2nM at CB1 and 5.3nM at CB2. AM-906 — a potent and dodecally selective agonist for the CB1 cannabinoid receptor, with a Ki of 0.8nM at CB1 and 9.5nM at CB2. AM-919 — a potent agonist at both CB1 and CB2 with moderate selectivity for CB1, with a Ki of 2.2nM at CB1 and 3.4nM at CB2. It is a derivative of HU-210 and represents a hybrid structure between the classical and nonclassical cannabinoid families. AM-926 — a potent agonist at both CB1 and CB2 with moderate selectivity for CB1, with a Ki of 2.2nM at CB1 and 4.3nM at CB2. It is a derivative of HU-210 and represents a hybrid structure between the classical and nonclassical cannabinoid families. AM-938 — a potent agonist at both CB1 and CB2 with quadruple selectivity for CB2, with a Ki of 1.2nM at CB1 and 0.3nM at CB2. It is a derivative of HU-210 and represents a hybrid structure between the classical and nonclassical cannabinoid families. AM-1116 — a dimethylated stereoisomer of anandamide whose Ki = 7.4nM at CB1.[2] AM-1172 — an endocannabinoid analog specifically designed to be a potent and selective inhibitor of AEA uptake that is resistant to FAAH hydrolysis. AM-1220 — a potent and selective analgesic CB1 agonist (as racemate) with a Ki of 3.88nM at CB1 and 73.4nM at CB2, giving it 19x selectivity for CB1. (R) enantiomer has around 1000x higher affinity for CB1 than (S) enantiomer.[6][7] AM-1221 — a potent and selective CB2 agonist with a Ki of 0.28nM at CB2 and 52.3nM at CB1, giving it a selectivity of almost 187x. AM-1235 — a moderately CB1 selective agonist, with a Ki of 1.5nM at CB1 and 20.4nM at CB2, giving it a selectivity of around 13x.[8] AM-1241 — a potent and selective analgesic CB2 agonist with a Ki of 3.4nM at CB2 and 80x selectivity over CB1.[9] AM-1248 — a moderately potent agonist with some selectivity for CB1, containing an unusual 3-(adamant-1-oyl) substitution on the indole ring. AM-2201 — a potent agonist at both CB1 and CB2 with moderate selectivity for CB1, with a Ki of 1.0nM at CB1 and 2.6nM at CB2. AM-2212 — a potent agonist at both CB1 and CB2 with dodecal selectivity for CB1, with a Ki of 1.4nM at CB1 and 18.9nM at CB2.[4] AM-2213 — a potent agonist at both CB1 and CB2 with 10x selectivity for CB1, with a Ki of 3.0M at CB1 and 30nM at CB2.[4] AM-2232 — a potent agonist at both CB1 and CB2, with a Ki of 0.28nM at CB1 and 1.48nM at CB2.[8] AM-2233 — (R) enantiomer is potent and selective CB1 agonist used in 131I radiolabelled form to map distribution of CB1 receptors in brain.[10][11][12][13][14][15] AM-3102 — oleoyl ethanolamide, an endogenous agonist for proliferator-activated receptor α (PPARα) that also acts as a weak cannabinoid agonist with Ki values of 33µM at CB1 and 26µM at CB2. AM-4030 — a potent agonist at both CB1 and CB2, it is dodecally selective for CB1, with a Ki of 0.7nM at CB1 and 8.6nM at CB2. It is a derivative of HU-210 and represents a hybrid structure between the classical and nonclassical cannabinoid families. See also List of JWH cannabinoids List of CP cannabinoids List of HU cannabinoids Further reading A more complete list can be found here [1] References ^ a b Lan, Ruoxi; Lu, Qian; Fan, Pusheng; Gatley, John; Volkow, Nora D.; Fernando, Susanthi R.; Pertwee, Roger; Makriyannis, Alexandros (1999). "Design and synthesis of the CB1 selective cannabinoid antagonist AM281: A potential human SPECT ligand". AAPS PharmSci 1 (2): 39–45. doi:10.1208/ps010204.  edit ^ a b c d Selwood, D. (2009). "The Cannabinoid Receptors. Edited by Patricia H. Reggio". ChemMedChem 4: 1949. doi:10.1002/cmdc.200900286.  edit ^ Pacher, P.; Bátkai, S; Kunos, G (2006). "The Endocannabinoid System as an Emerging Target of Pharmacotherapy". Pharmacological Reviews 58 (3): 389–462. doi:10.1124/pr.58.3.2. PMC 2241751. PMID 16968947.  edit ^ a b c Hongfeng Deng. Design and synthesis of selective cannabinoid receptor ligands: Aminoalkylindole and other heterocyclic analogs. PhD Dissertation, University of Connecticut, 2000. ^ WO patent 200128557, Makriyannis A, Deng H, "Cannabimimetic indole derivatives", granted 2001-06-07   ^ D'ambra, T. (1996). "C-Attached aminoalkylindoles: potent cannabinoid mimetics". Bioorganic & Medicinal Chemistry Letters 6: 17–14. doi:10.1016/0960-894X(95)00560-G.  edit ^ Willis, P. G.; Pavlova, O. A.; Chefer, S. I.; Vaupel, D. B.; Mukhin, A. G.; Horti, A. G. (2005). "Synthesis and Structure−Activity Relationship of a Novel Series of Aminoalkylindoles with Potential for Imaging the Neuronal Cannabinoid Receptor by Positron Emission Tomography". Journal of Medicinal Chemistry 48 (18): 5813. doi:10.1021/jm0502743. PMID 16134948.  edit ^ a b US patent 7241799, Makriyannis A, Deng H, "Cannabimimetic indole derivatives", granted 2007-07-10   ^ Poso, A.; Huffman, J. W. (2008). "Targeting the cannabinoid CB2 receptor: modelling and structural determinants of CB2 selective ligands". British Journal of Pharmacology 153 (2): 335. doi:10.1038/sj.bjp.0707567. PMC 2219524. PMID 17982473.  edit ^ Deng H, Gifford AN, Zvonok AM, Cui G, Li X, Fan P, Deschamps JR, Flippen-Anderson JL, Gatley SJ, Makriyannis A (October 2005). "Potent cannabinergic indole analogues as radioiodinatable brain imaging agents for the CB1 cannabinoid receptor". Journal of Medicinal Chemistry 48 (20): 6386–92. doi:10.1021/jm050135l. PMID 16190764.  ^ Hanu�, L. �R. O.; Mechoulam, R. (2005). Cannabinoid chemistry: an overview. pp. 23. doi:10.1007/3-7643-7358-X_2.  edit ^ Shen CP, Xiao JC, Armstrong H, Hagmann W, Fong TM (February 2006). "F200A substitution in the third transmembrane helix of human cannabinoid CB1 receptor converts AM2233 from receptor agonist to inverse agonist". European Journal of Pharmacology 531 (1–3): 41–6. doi:10.1016/j.ejphar.2005.12.026. PMID 16438957.  ^ Dhawan, J.; Deng, H.; Gatley, S. J.; Makriyannis, A.; Akinfeleye, T.; Bruneus, M.; Dimaio, A. A.; Gifford, A. N. (2006). "Evaluation of the in vivo receptor occupancy for the behavioral effects of cannabinoids using a radiolabeled cannabinoid receptor agonist, R-[125/131I]AM2233". Synapse 60 (2): 93. doi:10.1002/syn.20277. PMID 16715483.  edit ^ Leung K (2006 Dec 12). "R-2-[131I]Iodophenyl-(1-(1-methylpiperidin-2-ylmethyl)-1H-indol-3-yl)methanone". Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. PMID 20641836.  ^ Pei, Y.; Mercier, R.; Anday, J.; Thakur, G.; Zvonok, A.; Hurst, D.; Reggio, P.; Janero, D. et al. (2008). "Ligand-Binding Architecture of Human CB2 Cannabinoid Receptor: Evidence for Receptor Subtype-Specific Binding Motif and Modeling GPCR Activation". Chemistry & Biology 15: 1207. doi:10.1016/j.chembiol.2008.10.011.  edit