Page last updated: 2024-08-07 16:32:01
Cannabinoid receptor 2
A cannabinoid receptor 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P34972]
Synonyms
CB-2;
CB2;
hCB2;
CX5
Research
Bioassay Publications (257)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (0.78) | 18.2507 |
| 2000's | 90 (35.02) | 29.6817 |
| 2010's | 142 (55.25) | 24.3611 |
| 2020's | 23 (8.95) | 2.80 |
Compounds (88)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| tacrine | Homo sapiens (human) | Ki | 1.0000 | 1 | 1 |
| am 251 | Homo sapiens (human) | Ki | 0.3703 | 7 | 8 |
| cannabinol | Homo sapiens (human) | Ki | 0.1217 | 5 | 5 |
| palmidrol | Homo sapiens (human) | Ki | 5.0000 | 2 | 3 |
| indopan | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| dronabinol | Homo sapiens (human) | IC50 | 0.0095 | 1 | 1 |
| dronabinol | Homo sapiens (human) | Ki | 0.0366 | 22 | 22 |
| cannabichromene | Homo sapiens (human) | Ki | 0.2570 | 1 | 1 |
| epigallocatechin gallate | Homo sapiens (human) | Ki | 42.8000 | 1 | 1 |
| gallocatechol | Homo sapiens (human) | Ki | 361.3000 | 1 | 1 |
| magnolol | Homo sapiens (human) | Ki | 1.7200 | 2 | 2 |
| honokiol | Homo sapiens (human) | Ki | 2.4595 | 3 | 3 |
| (6ar-trans)-isomer of tetrahydrocannabivarin 9 | Homo sapiens (human) | IC50 | 0.0176 | 1 | 1 |
| (6ar-trans)-isomer of tetrahydrocannabivarin 9 | Homo sapiens (human) | Ki | 0.0429 | 3 | 3 |
| delta(9)-tetrahydrocannabinolic acid | Homo sapiens (human) | Ki | 0.0560 | 1 | 1 |
| rimonabant | Homo sapiens (human) | IC50 | 9.8000 | 1 | 1 |
| rimonabant | Homo sapiens (human) | Ki | 1.5800 | 1 | 1 |
| sr141716 | Homo sapiens (human) | IC50 | 2.3894 | 19 | 19 |
| sr141716 | Homo sapiens (human) | Ki | 1.7507 | 46 | 49 |
| cp-55,940 | Homo sapiens (human) | IC50 | 0.0028 | 4 | 4 |
| cp-55,940 | Homo sapiens (human) | Ki | 0.0050 | 27 | 29 |
| 1,1-dimethylheptyl-11-hydroxytetrahydrocannabinol | Homo sapiens (human) | Ki | 0.0751 | 2 | 2 |
| epicatechin gallate | Homo sapiens (human) | Ki | 95.6000 | 1 | 1 |
| 4-methoxyhonokiol | Homo sapiens (human) | Ki | 0.6832 | 2 | 5 |
| 8-hydroxy-delta(9)-tetrahydrocannabinol | Homo sapiens (human) | Ki | 0.0880 | 1 | 1 |
| delta-8-tetrahydrocannabinol | Homo sapiens (human) | Ki | 0.0275 | 5 | 6 |
| cannabidiol | Homo sapiens (human) | Ki | 4.0230 | 4 | 4 |
| capsaicin | Homo sapiens (human) | Ki | 10.0000 | 2 | 3 |
| orlistat | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| sr 144528 | Homo sapiens (human) | IC50 | 2.0090 | 4 | 4 |
| sr 144528 | Homo sapiens (human) | Ki | 0.1296 | 15 | 16 |
| 11-hydroxycannabinol | Homo sapiens (human) | Ki | 0.0266 | 1 | 1 |
| lenabasum | Homo sapiens (human) | Ki | 0.1705 | 1 | 1 |
| jhw 015 | Homo sapiens (human) | Ki | 0.1337 | 8 | 11 |
| am 281 | Homo sapiens (human) | Ki | 4.2000 | 1 | 1 |
| am 630 | Homo sapiens (human) | IC50 | 7.2000 | 1 | 1 |
| am 630 | Homo sapiens (human) | Ki | 0.3350 | 9 | 10 |
| caryophyllene | Homo sapiens (human) | Ki | 0.1500 | 1 | 1 |
| anandamide | Homo sapiens (human) | Ki | 0.2699 | 10 | 11 |
| glyceryl 2-arachidonate | Homo sapiens (human) | Ki | 1.3750 | 4 | 4 |
| n-oleoylethanolamine | Homo sapiens (human) | Ki | 7.7750 | 3 | 4 |
| nabilone | Homo sapiens (human) | Ki | 0.0097 | 2 | 2 |
| arachidonyl-2-chloroethylamide | Homo sapiens (human) | Ki | 0.0950 | 1 | 1 |
| hu 243 | Homo sapiens (human) | Ki | 0.0021 | 1 | 1 |
| l 759633 | Homo sapiens (human) | Ki | 0.0132 | 2 | 2 |
| ly 320135 | Homo sapiens (human) | Ki | 12.3956 | 2 | 2 |
| (3r)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone | Homo sapiens (human) | IC50 | 0.0064 | 5 | 5 |
| (3r)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone | Homo sapiens (human) | Ki | 0.0047 | 66 | 70 |
| cannabigerol | Homo sapiens (human) | IC50 | 3.4600 | 1 | 1 |
| cannabigerol | Homo sapiens (human) | Ki | 1.2382 | 4 | 4 |
| am-356 | Homo sapiens (human) | Ki | 0.2200 | 1 | 1 |
| guineensine | Homo sapiens (human) | Ki | 38.3000 | 1 | 1 |
| (2E,4E)-N-isobutyl-2,4-dodecadienamide | Homo sapiens (human) | Ki | 0.0560 | 2 | 2 |
| noladin ether | Homo sapiens (human) | Ki | 2.3333 | 3 | 3 |
| am 404 | Homo sapiens (human) | Ki | 1.1000 | 3 | 3 |
| jwh-133 | Homo sapiens (human) | IC50 | 0.0818 | 1 | 1 |
| jwh-133 | Homo sapiens (human) | Ki | 0.0048 | 17 | 17 |
| CB-13 | Homo sapiens (human) | IC50 | 2.6990 | 2 | 2 |
| CB-13 | Homo sapiens (human) | Ki | 0.0190 | 2 | 2 |
| am-411 | Homo sapiens (human) | Ki | 0.0522 | 3 | 3 |
| hu 210 | Homo sapiens (human) | Ki | 0.0039 | 10 | 10 |
| slv 319 | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| slv 319 | Homo sapiens (human) | Ki | 6.8767 | 6 | 6 |
| sr 147778 | Homo sapiens (human) | Ki | 0.4420 | 1 | 1 |
| jte 907 | Homo sapiens (human) | IC50 | 0.3346 | 2 | 2 |
| jte 907 | Homo sapiens (human) | Ki | 0.0340 | 4 | 6 |
| emindole SB | Homo sapiens (human) | Ki | 2.2400 | 1 | 1 |
| 1-(2,3-dichlorobenzoyl)-5-methoxy-2-methyl-(2-(mopholin-4-yl)ethyl)-1h-indole | Homo sapiens (human) | Ki | 0.0097 | 7 | 7 |
| amg 3 | Homo sapiens (human) | Ki | 0.0005 | 2 | 3 |
| cp 945598 | Homo sapiens (human) | Ki | 7.7000 | 1 | 1 |
| 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-3-hexyl-1h-1,2,4-triazole | Homo sapiens (human) | Ki | 3.0820 | 1 | 1 |
| am 1241 | Homo sapiens (human) | IC50 | 0.0034 | 1 | 1 |
| am 1241 | Homo sapiens (human) | Ki | 0.1259 | 8 | 11 |
| km-233 | Homo sapiens (human) | Ki | 0.0009 | 5 | 5 |
| 1-(2,4-dichlorophenyl)-6-methyl-N-(1-piperidinyl)-4H-indeno[1,2-c]pyrazole-3-carboxamide | Homo sapiens (human) | Ki | 0.0000 | 3 | 3 |
| gw 842166x | Homo sapiens (human) | Ki | 7.5000 | 2 | 2 |
| jwh 018 | Homo sapiens (human) | Ki | 0.0057 | 5 | 6 |
| jwh-073 | Homo sapiens (human) | Ki | 0.0098 | 1 | 1 |
| n-arachidonoyl l-serine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| n-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamide | Homo sapiens (human) | IC50 | 0.5087 | 4 | 4 |
| n-(3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl)-2-methyl-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)propanamide | Homo sapiens (human) | Ki | 0.2900 | 1 | 1 |
| pf 514273 | Homo sapiens (human) | Ki | 7.5002 | 3 | 4 |
| mk-9470 | Homo sapiens (human) | IC50 | 0.0440 | 2 | 2 |
| hu 308 | Homo sapiens (human) | Ki | 0.0204 | 6 | 6 |
| 1-(4-chlorophenyl)-3-(3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl)urea | Homo sapiens (human) | IC50 | 10.0000 | 4 | 4 |
| 1-(4-chlorophenyl)-3-(3-(6-pyrrolidin-1-ylpyridin-2-yl)phenyl)urea | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| a-796260 | Homo sapiens (human) | IC50 | 0.0008 | 2 | 2 |
| a-796260 | Homo sapiens (human) | Ki | 0.1095 | 5 | 8 |
| cannabidivarin | Homo sapiens (human) | Ki | 0.5740 | 1 | 1 |
| omdm 169 | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| a 803467 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| a-836339 | Homo sapiens (human) | Ki | 0.0006 | 3 | 3 |
| smm-189 | Homo sapiens (human) | Ki | 0.0818 | 3 | 3 |
| n-(adamantan-1-yl)-4-oxo-1-pentyl-6-phenyl-1,4-dihydroquinoline-3-carboxamide | Homo sapiens (human) | Ki | 0.0038 | 2 | 2 |
| jwh 250 | Homo sapiens (human) | Ki | 0.0330 | 2 | 2 |
| jwh-122 | Homo sapiens (human) | Ki | 0.0012 | 1 | 1 |
| ur-144 | Homo sapiens (human) | Ki | 0.0018 | 1 | 2 |
| misoprostol | Homo sapiens (human) | IC50 | 10.0000 | 2 | 2 |
| jwh-210 | Homo sapiens (human) | Ki | 0.0007 | 1 | 1 |
| n,n-diallyl-5-methoxytryptamine | Homo sapiens (human) | Ki | 10.0000 | 1 | 1 |
| s-777469 | Homo sapiens (human) | IC50 | 0.0240 | 1 | 1 |
| s-777469 | Homo sapiens (human) | Ki | 0.0360 | 3 | 3 |
| jd5037 | Homo sapiens (human) | IC50 | 1.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| cannabinol | Homo sapiens (human) | EC50 | 0.1671 | 2 | 2 |
| dronabinol | Homo sapiens (human) | EC50 | 0.0086 | 3 | 3 |
| magnolol | Homo sapiens (human) | EC50 | 3.2800 | 1 | 1 |
| (6ar-trans)-isomer of tetrahydrocannabivarin 9 | Homo sapiens (human) | EC50 | 0.0680 | 2 | 2 |
| sr141716 | Homo sapiens (human) | EC50 | 20.6050 | 2 | 2 |
| cp-55,940 | Homo sapiens (human) | EC50 | 0.0302 | 48 | 52 |
| cp-55,940 | Homo sapiens (human) | Kd | 0.0006 | 1 | 1 |
| 1,1-dimethylheptyl-11-hydroxytetrahydrocannabinol | Homo sapiens (human) | EC50 | 0.0003 | 1 | 1 |
| cannabidiol | Homo sapiens (human) | EC50 | 0.1791 | 23 | 23 |
| 3-[[4-(2,3-dimethylphenyl)-1-piperazinyl]-oxomethyl]-N,N-dimethyl-4-(1-pyrrolidinyl)benzenesulfonamide | Homo sapiens (human) | EC50 | 30.0000 | 1 | 1 |
| sr 144528 | Homo sapiens (human) | EC50 | 5.8578 | 5 | 5 |
| jhw 015 | Homo sapiens (human) | EC50 | 0.6340 | 2 | 2 |
| am 630 | Homo sapiens (human) | EC50 | 0.9990 | 4 | 4 |
| caryophyllene | Homo sapiens (human) | EC50 | 1.9000 | 1 | 1 |
| glyceryl 2-arachidonate | Homo sapiens (human) | EC50 | 0.0170 | 1 | 1 |
| (3r)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone | Homo sapiens (human) | EC50 | 0.0288 | 17 | 17 |
| jwh-133 | Homo sapiens (human) | EC50 | 0.1802 | 3 | 3 |
| CB-13 | Homo sapiens (human) | EC50 | 0.0279 | 1 | 1 |
| hu 210 | Homo sapiens (human) | EC50 | 0.0026 | 5 | 5 |
| jte 907 | Homo sapiens (human) | EC50 | 0.3162 | 1 | 1 |
| jte 907 | Homo sapiens (human) | Kd | 0.1585 | 1 | 1 |
| 1-(2,3-dichlorobenzoyl)-5-methoxy-2-methyl-(2-(mopholin-4-yl)ethyl)-1h-indole | Homo sapiens (human) | EC50 | 0.0257 | 2 | 2 |
| am 1241 | Homo sapiens (human) | EC50 | 6.6721 | 3 | 3 |
| gw 842166x | Homo sapiens (human) | EC50 | 0.2193 | 10 | 10 |
| jwh 018 | Homo sapiens (human) | EC50 | 0.0127 | 3 | 5 |
| hu 308 | Homo sapiens (human) | EC50 | 0.0983 | 4 | 4 |
| a-796260 | Homo sapiens (human) | EC50 | 0.0102 | 3 | 3 |
| cannabidivarin | Homo sapiens (human) | EC50 | 0.0126 | 1 | 1 |
| smm-189 | Homo sapiens (human) | EC50 | 0.1543 | 3 | 3 |
| ur-144 | Homo sapiens (human) | EC50 | 0.0290 | 1 | 1 |
| AKB48 | Homo sapiens (human) | EC50 | 0.0920 | 1 | 1 |
| sdb-001 | Homo sapiens (human) | EC50 | 0.0617 | 4 | 5 |
Drugs with Other Measurements
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Emerging targets in osteoporosis disease modification.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
Synthesis, cannabinoid receptor affinity, molecular modeling studies and in vivo pharmacological evaluation of new substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides. 2. Effect of the 3-carboxamide substituent on the affinity and selectivityBioorganic & medicinal chemistry, , Aug-01, Volume: 17, Issue:15, 2009
Novel sterically hindered cannabinoid CB1 receptor ligands.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Synthesis, cannabinoid receptor affinity, and molecular modeling studies of substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Phytocannabinoid Pharmacology: Medicinal Properties of Journal of natural products, , 01-22, Volume: 84, Issue:1, 2021
Plant-Based Modulators of Endocannabinoid Signaling.Journal of natural products, , 03-22, Volume: 82, Issue:3, 2019
Iodine-Promoted Aromatization of p-Menthane-Type Phytocannabinoids.Journal of natural products, , 03-23, Volume: 81, Issue:3, 2018
Novel cannabinol probes for CB1 and CB2 cannabinoid receptors.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Cannabinol derivatives: binding to cannabinoid receptors and inhibition of adenylylcyclase.Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
[no title available]Journal of natural products, , Sep-24, Volume: 84, Issue:9, 2021
Oxa-adamantyl cannabinoids.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 38, 2021
The Essential Medicinal Chemistry of Cannabidiol (CBD).Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
[no title available]Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Isolation and Pharmacological Evaluation of Minor Cannabinoids from High-Potency Cannabis sativa.Journal of natural products, , Jun-26, Volume: 78, Issue:6, 2015
One-pot heterogeneous synthesis of Δ(3)-tetrahydrocannabinol analogues and xanthenes showing differential binding to CB(1) and CB(2) receptors.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Antagonists for the orphan G-protein-coupled receptor GPR55 based on a coumarin scaffold.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
γ-Carbolines: a novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 22, Issue:4, 2012
Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents.Bioorganic & medicinal chemistry, , Mar-15, Volume: 20, Issue:6, 2012
Cannabinomimetic lipid from a marine cyanobacterium.Journal of natural products, , Oct-28, Volume: 74, Issue:10, 2011
1-Bromo-3-(1',1'-dimethylalkyl)-1-deoxy-Δ(8)-tetrahydrocannabinols: New selective ligands for the cannabinoid CB(2) receptor.Bioorganic & medicinal chemistry, , Nov-15, Volume: 18, Issue:22, 2010
Synthesis and structure-activity relationship of substitutions at the C-1 position of Delta9-tetrahydrocannabinol.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
Synthesis and pharmacology of 1-methoxy analogs of CP-47,497.Bioorganic & medicinal chemistry, , Aug-01, Volume: 18, Issue:15, 2010
Synthesis and pharmacology of 1-deoxy analogs of CP-47,497 and CP-55,940.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
Novel benzimidazole derivatives as selective CB2 agonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 18, Issue:13, 2008
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 2: orally bioavailable compounds.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 17, Issue:14, 2007
1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 15, Issue:18, 2005
Synthesis and testing of novel phenyl substituted side-chain analogues of classical cannabinoids.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 13, Issue:20, 2003
Novel cannabinol probes for CB1 and CB2 cannabinoid receptors.Journal of medicinal chemistry, , Oct-05, Volume: 43, Issue:20, 2000
A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Cannabinol derivatives: binding to cannabinoid receptors and inhibition of adenylylcyclase.Journal of medicinal chemistry, , Sep-26, Volume: 40, Issue:20, 1997
Synthesis and pharmacology of a very potent cannabinoid lacking a phenolic hydroxyl with high affinity for the CB2 receptor.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
Magnolia Extract, Magnolol, and Metabolites: Activation of Cannabinoid CB2 Receptors and Blockade of the Related GPR55.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 2013
Mechanisms of osteoclastogenesis inhibition by a novel class of biphenyl-type cannabinoid CB(2) receptor inverse agonists.Chemistry & biology, , Aug-26, Volume: 18, Issue:8, 2011
Synthesis and pharmacological evaluation of new biphenylic derivatives as CB2 receptor ligands.European journal of medicinal chemistry, , Jun-30, Volume: 116, 2016
Magnolia Extract, Magnolol, and Metabolites: Activation of Cannabinoid CB2 Receptors and Blockade of the Related GPR55.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 2013
Mechanisms of osteoclastogenesis inhibition by a novel class of biphenyl-type cannabinoid CB(2) receptor inverse agonists.Chemistry & biology, , Aug-26, Volume: 18, Issue:8, 2011
Phytocannabinoid Pharmacology: Medicinal Properties of Journal of natural products, , 01-22, Volume: 84, Issue:1, 2021
Synthesis of the Major Mammalian Metabolites of THCV.Journal of natural products, , 07-24, Volume: 83, Issue:7, 2020
Plant-Based Modulators of Endocannabinoid Signaling.Journal of natural products, , 03-22, Volume: 82, Issue:3, 2019
Design, syntheses, structure-activity relationships and docking studies of coumarin derivatives as novel selective ligands for the CB2 receptor.European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Design, synthesis, biological properties, and molecular modeling investigations of novel tacrine derivatives with a combination of acetylcholinesterase inhibition and cannabinoid CB1 receptor antagonism.Journal of medicinal chemistry, , Feb-11, Volume: 53, Issue:3, 2010
Synthesis, Biological Evaluation, and Molecular Modeling Studies of 3,4-Diarylpyrazoline Series of Compounds as Potent, Nonbrain Penetrant Antagonists of Cannabinoid-1 (CBJournal of medicinal chemistry, , 02-10, Volume: 65, Issue:3, 2022
Synthesis and pharmacological characterization of functionalized 6-piperazin-1-yl-purines as cannabinoid receptor 1 (CB1) inverse agonists.Bioorganic & medicinal chemistry, , 08-15, Volume: 26, Issue:15, 2018
[no title available]Journal of medicinal chemistry, , 11-21, Volume: 61, Issue:22, 2018
Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Pyrazole antagonists of the CB1 receptor with reduced brain penetration.Bioorganic & medicinal chemistry, , Mar-01, Volume: 24, Issue:5, 2016
Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 7. Synthesis and Pharmacological Evaluation of 4-Quinolone-3-carboxamides and 4-Hydroxy-2-quinolone-3-carboxamides as High Affinity Cannabinoid Receptor 2 (CB2R) Ligands with Improved Aqueous SoluJournal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
A critical review of both the synthesis approach and the receptor profile of the 8-chloro-1-(2',4'-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide and analogue derivatives.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
Design, synthesis, biological evaluation, and comparative docking study of 1,2,4-triazolones as CB1 receptor selective antagonists.European journal of medicinal chemistry, , Mar-03, Volume: 74, 2014
Ultrapure ajulemic acid has improved CB2 selectivity with reduced CB1 activity.Bioorganic & medicinal chemistry, , Jul-01, Volume: 22, Issue:13, 2014
Magnolia Extract, Magnolol, and Metabolites: Activation of Cannabinoid CB2 Receptors and Blockade of the Related GPR55.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 2013
7-Alkyl-3-benzylcoumarins: a versatile scaffold for the development of potent and selective cannabinoid receptor agonists and antagonists.Journal of medicinal chemistry, , Sep-27, Volume: 55, Issue:18, 2012
Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents.ACS medicinal chemistry letters, , May-10, Volume: 3, Issue:5, 2012
Design and synthesis of cannabinoid receptor 1 antagonists for peripheral selectivity.Journal of medicinal chemistry, , Mar-22, Volume: 55, Issue:6, 2012
Investigations on the 4-quinolone-3-carboxylic acid motif. 6. Synthesis and pharmacological evaluation of 7-substituted quinolone-3-carboxamide derivatives as high affinity ligands for cannabinoid receptors.European journal of medicinal chemistry, , Volume: 58, 2012
Design, synthesis, and pharmacological characterization of indol-3-ylacetamides, indol-3-yloxoacetamides, and indol-3-ylcarboxamides: potent and selective CB2 cannabinoid receptor inverse agonists.Journal of medicinal chemistry, , Jun-14, Volume: 55, Issue:11, 2012
Investigations on the 4-quinolone-3-carboxylic acid motif. 4. Identification of new potent and selective ligands for the cannabinoid type 2 receptor with diverse substitution patterns and antihyperalgesic effects in mice.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
Structure-activity relationship studies of novel pyrazole and imidazole carboxamides as cannabinoid-1 (CB1) antagonists.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 21, Issue:16, 2011
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 21, Issue:7, 2011
Investigations on the 4-quinolone-3-carboxylic acid motif. 3. Synthesis, structure-affinity relationships, and pharmacological characterization of 6-substituted 4-quinolone-3-carboxamides as highly selective cannabinoid-2 receptor ligands.Journal of medicinal chemistry, , Aug-26, Volume: 53, Issue:16, 2010
Discovery of benzhydrylpiperazine derivatives as CB1 receptor inverse agonists via privileged structure-based approach.European journal of medicinal chemistry, , Volume: 45, Issue:3, 2010
Synthesis and biological evaluation of bivalent ligands for the cannabinoid 1 receptor.Journal of medicinal chemistry, , Oct-14, Volume: 53, Issue:19, 2010
Probing the cannabinoid CB1/CB2 receptor subtype selectivity limits of 1,2-diarylimidazole-4-carboxamides by fine-tuning their 5-substitution pattern.Bioorganic & medicinal chemistry letters, , May-01, Volume: 20, Issue:9, 2010
Diaryl piperidines as CB1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Synthesis and biological evaluation of new N-alkyl 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides as cannabinoid receptor ligands.European journal of medicinal chemistry, , Volume: 45, Issue:12, 2010
Discovery of 2-(4-((1H-1,2,4-triazol-1-yl)methyl)-5-(4-bromophenyl)-1-(2-chlorophenyl)-1H-pyrazol-3-yl)-5-tert-butyl-1,3,4-thiadiazole (GCC2680) as a potent, selective and orally efficacious cannabinoid-1 receptor antagonist.Bioorganic & medicinal chemistry, , Sep-01, Volume: 18, Issue:17, 2010
Synthesis and structure-activity relationship of 1,2,4-triazole-containing diarylpyrazolyl carboxamide as CB1 cannabinoid receptor-ligand.Bioorganic & medicinal chemistry, , Volume: 18, Issue:3, 2010
Synthesis and in vitro autoradiographic evaluation of a novel high-affinity radioiodinated ligand for imaging brain cannabinoid subtype-1 receptors.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 19, Issue:21, 2009
Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Oxadiazole-diarylpyrazole 4-carboxamides as cannabinoid CB1 receptor ligands.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 19, Issue:7, 2009
Diarylimidazolyl oxadiazole and thiadiazole derivatives as cannabinoid CB1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
Synthesis, cannabinoid receptor affinity, molecular modeling studies and in vivo pharmacological evaluation of new substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides. 2. Effect of the 3-carboxamide substituent on the affinity and selectivityBioorganic & medicinal chemistry, , Aug-01, Volume: 17, Issue:15, 2009
Discovery and functional evaluation of diverse novel human CB(1) receptor ligands.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Discovery of 2-[5-(4-chloro-phenyl)-1-(2,4-dichloro-phenyl)-4-ethyl-1H-pyrazol-3-yl]-1,5,5-trimethyl-1,5-dihydro-imidazol-4-thione (BPR-890) via an active metabolite. A novel, potent and selective cannabinoid-1 receptor inverse agonist with high antiobesiJournal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
1,2,3-Triazole derivatives as new cannabinoid CB1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 2009
Pentacycle derivatives as cannabinoid CB1 receptor ligands.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 19, Issue:23, 2009
Synthesis and characterization of a peripherally restricted CB1 cannabinoid antagonist, URB447, that reduces feeding and body-weight gain in mice.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 19, Issue:3, 2009
Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a CB1 receptor antagonist with in vivo antiobesity effect.Bioorganic & medicinal chemistry letters, , May-01, Volume: 19, Issue:9, 2009
Investigations on the 4-quinolone-3-carboxylic acid motif. 2. Synthesis and structure-activity relationship of potent and selective cannabinoid-2 receptor agonists endowed with analgesic activity in vivo.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Novel sterically hindered cannabinoid CB1 receptor ligands.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
Synthesis, ex vivo evaluation, and radiolabeling of potent 1,5-diphenylpyrrolidin-2-one cannabinoid subtype-1 receptor ligands as candidates for in vivo imaging.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
Discovery and labeling of high-affinity 3,4-diarylpyrazolines as candidate radioligands for in vivo imaging of cannabinoid subtype-1 (CB1) receptors.Journal of medicinal chemistry, , Sep-25, Volume: 51, Issue:18, 2008
Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Design, synthesis and biological evaluation of piperazine analogues as CB1 cannabinoid receptor ligands.Bioorganic & medicinal chemistry, , Apr-01, Volume: 16, Issue:7, 2008
Synthesis, cannabinoid receptor affinity, and molecular modeling studies of substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Bioisosteric replacement of the pyrazole 5-aryl moiety of N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716A). A novel series of alkynylthiophenes as potent and selective cannabinoid-1 receptor antagJournal of medicinal chemistry, , Sep-11, Volume: 51, Issue:17, 2008
Tetrazole-biarylpyrazole derivatives as cannabinoid CB1 receptor antagonists.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 18, Issue:7, 2008
Aminopyrazine CB1 receptor inverse agonists.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 18, Issue:11, 2008
Rational design, synthesis and biological evaluation of new 1,5-diarylpyrazole derivatives as CB1 receptor antagonists, structurally related to rimonabant.European journal of medicinal chemistry, , Volume: 43, Issue:12, 2008
Identification of novel cannabinoid CB1 receptor antagonists by using virtual screening with a pharmacophore model.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Conformationally constrained analogues of N-(piperidinyl)-5-(4-chlorophenyl)-1-(2,4- dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716): design, synthesis, computational analysis, and biological evaluations.Journal of medicinal chemistry, , Jun-26, Volume: 51, Issue:12, 2008
Discovery of a novel class of selective human CB1 inverse agonists.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 18, Issue:3, 2008
Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 17, Issue:8, 2007
Diaryl dihydropyrazole-3-carboxamides with significant in vivo antiobesity activity related to CB1 receptor antagonism: synthesis, biological evaluation, and molecular modeling in the homology model.Journal of medicinal chemistry, , Nov-29, Volume: 50, Issue:24, 2007
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 17, Issue:23, 2007
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.Journal of medicinal chemistry, , Dec-28, Volume: 49, Issue:26, 2006
Bioisosteric replacements of the pyrazole moiety of rimonabant: synthesis, biological properties, and molecular modeling investigations of thiazoles, triazoles, and imidazoles as potent and selective CB1 cannabinoid receptor antagonists.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Synthesis and structure-activity relationships of amide and hydrazide analogues of the cannabinoid CB(1) receptor antagonist N-(piperidinyl)- 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide (SR141716).Journal of medicinal chemistry, , Jun-20, Volume: 45, Issue:13, 2002
A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Pyrazolidine Carboxamide Analogs as Selective Agonists of the Cannabinoid 2 Receptor.ACS medicinal chemistry letters, , Dec-08, Volume: 13, Issue:12, 2022
Design, Synthesis, and Biological Activity of New CB2 Receptor Ligands: from Orthosteric and Allosteric Modulators to Dualsteric/Bitopic Ligands.Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
[no title available]RSC medicinal chemistry, , Feb-23, Volume: 13, Issue:2, 2022
Carbon-silicon switch led to the discovery of novel synthetic cannabinoids with therapeutic effects in a mouse model of multiple sclerosis.European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
Phytocannabinoid Pharmacology: Medicinal Properties of Journal of natural products, , 01-22, Volume: 84, Issue:1, 2021
Novel Functionalized Cannabinoid Receptor Probes: Development of Exceptionally Potent Agonists.Journal of medicinal chemistry, , 04-08, Volume: 64, Issue:7, 2021
Synthesis and SAR evaluation of coumarin derivatives as potent cannabinoid receptor agonists.European journal of medicinal chemistry, , Aug-05, Volume: 220, 2021
The discovery of a potent and selective pyrazolo-[2,3-e]-[1,2,4]-triazine cannabinoid type 2 receptor agonist.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Oxa-adamantyl cannabinoids.Bioorganic & medicinal chemistry letters, , 04-15, Volume: 38, 2021
Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.Bioorganic & medicinal chemistry, , 03-01, Volume: 33, 2021
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Introducing nitrogen atoms to amidoalkylindoles: potent and selective cannabinoid type 2 receptor agonists with improved aqueous solubility.MedChemComm, , Dec-01, Volume: 10, Issue:12, 2019
Strategies to develop selective CBEuropean journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Oximes short-acting CB1 receptor agonists.Bioorganic & medicinal chemistry, , 10-01, Volume: 26, Issue:18, 2018
Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Bioactive products from singlet oxygen photooxygenation of cannabinoids.European journal of medicinal chemistry, , Jan-01, Volume: 143, 2018
Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system.European journal of medicinal chemistry, , Jun-25, Volume: 154, 2018
Antitumorigenic Properties of Omega-3 Endocannabinoid Epoxides.Journal of medicinal chemistry, , 07-12, Volume: 61, Issue:13, 2018
[no title available]ACS medicinal chemistry letters, , Jun-08, Volume: 8, Issue:6, 2017
Biological evaluation of pyridone alkaloids on the endocannabinoid system.Bioorganic & medicinal chemistry, , 11-15, Volume: 25, Issue:22, 2017
Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CBMedChemComm, , Aug-01, Volume: 8, Issue:8, 2017
Developing pyridazine-3-carboxamides to be CB2 agonists: The design, synthesis, structure-activity relationships and docking studies.European journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
A critical review of both the synthesis approach and the receptor profile of the 8-chloro-1-(2',4'-dichlorophenyl)-N-piperidin-1-yl-1,4,5,6-tetrahydrobenzo[6,7]cyclohepta[1,2-c]pyrazole-3-carboxamide and analogue derivatives.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Design, syntheses, structure-activity relationships and docking studies of coumarin derivatives as novel selective ligands for the CB2 receptor.European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Distinct Temporal Fingerprint for Cyclic Adenosine Monophosphate (cAMP) Signaling of Indole-2-carboxamides as Allosteric Modulators of the Cannabinoid Receptors.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
One-pot heterogeneous synthesis of Δ(3)-tetrahydrocannabinol analogues and xanthenes showing differential binding to CB(1) and CB(2) receptors.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Structure-affinity relationships and pharmacological characterization of new alkyl-resorcinol cannabinoid receptor ligands: Identification of a dual cannabinoid receptor/TRPA1 channel agonist.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
Synthesis and biological evaluation of bivalent cannabinoid receptor ligands based on hCB₂R selective benzimidazoles reveal unexpected intrinsic properties.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 2014
Development of fluorinated CB(2) receptor agonists for PET studies.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
Trisubstituted Sulfonamides: a New Chemotype for Development of Potent and Selective CBACS medicinal chemistry letters, , Apr-11, Volume: 4, Issue:4, 2013
The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxJournal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
3-Carboxamido-5-aryl-isoxazoles as new CB2 agonists for the treatment of colitis.Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
Magnolia Extract, Magnolol, and Metabolites: Activation of Cannabinoid CB2 Receptors and Blockade of the Related GPR55.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 2013
Novel triaryl sulfonamide derivatives as selective cannabinoid receptor 2 inverse agonists and osteoclast inhibitors: discovery, optimization, and biological evaluation.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Mastering tricyclic ring systems for desirable functional cannabinoid activity.European journal of medicinal chemistry, , Volume: 69, 2013
7-Alkyl-3-benzylcoumarins: a versatile scaffold for the development of potent and selective cannabinoid receptor agonists and antagonists.Journal of medicinal chemistry, , Sep-27, Volume: 55, Issue:18, 2012
Lead discovery, chemistry optimization, and biological evaluation studies of novel biamide derivatives as CB2 receptor inverse agonists and osteoclast inhibitors.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Investigations on the 4-quinolone-3-carboxylic acid motif. 6. Synthesis and pharmacological evaluation of 7-substituted quinolone-3-carboxamide derivatives as high affinity ligands for cannabinoid receptors.European journal of medicinal chemistry, , Volume: 58, 2012
Mechanisms of osteoclastogenesis inhibition by a novel class of biphenyl-type cannabinoid CB(2) receptor inverse agonists.Chemistry & biology, , Aug-26, Volume: 18, Issue:8, 2011
Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity.European journal of medicinal chemistry, , Volume: 46, Issue:10, 2011
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Emerging targets in osteoporosis disease modification.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands: structural insights into the design of a novel inverse agonist series.Journal of medicinal chemistry, , Nov-25, Volume: 53, Issue:22, 2010
6-Methoxy-N-alkyl isatin acylhydrazone derivatives as a novel series of potent selective cannabinoid receptor 2 inverse agonists: design, synthesis, and binding mode prediction.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists.Bioorganic & medicinal chemistry, , Apr-01, Volume: 17, Issue:7, 2009
Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Synthesis and pharmacology of 1-deoxy analogs of CP-47,497 and CP-55,940.Bioorganic & medicinal chemistry, , Jan-01, Volume: 16, Issue:1, 2008
Design and synthesis of a novel series of N-alkyl isatin acylhydrazone derivatives that act as selective cannabinoid receptor 2 agonists for the treatment of neuropathic pain.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Imine derivatives as new potent and selective CB2 cannabinoid receptor agonists with an analgesic action.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
N-Alkylidenearylcarboxamides as new potent and selective CB(2) cannabinoid receptor agonists with good oral bioavailability.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 2007
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.Journal of medicinal chemistry, , Aug-09, Volume: 50, Issue:16, 2007
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
New metabolically stable fatty acid amide ligands of cannabinoid receptors: Synthesis and receptor affinity studies.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 2006
Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors.Journal of medicinal chemistry, , Dec-20, Volume: 44, Issue:26, 2001
Design, synthesis, binding, and molecular modeling studies of new potent ligands of cannabinoid receptors.Bioorganic & medicinal chemistry, , Aug-15, Volume: 15, Issue:16, 2007
Virtual screening of novel CB2 ligands using a comparative model of the human cannabinoid CB2 receptor.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Magnolia Extract, Magnolol, and Metabolites: Activation of Cannabinoid CB2 Receptors and Blockade of the Related GPR55.ACS medicinal chemistry letters, , Jan-10, Volume: 4, Issue:1, 2013
Mechanisms of osteoclastogenesis inhibition by a novel class of biphenyl-type cannabinoid CB(2) receptor inverse agonists.Chemistry & biology, , Aug-26, Volume: 18, Issue:8, 2011
Isolation and Pharmacological Evaluation of Minor Cannabinoids from High-Potency Cannabis sativa.Journal of natural products, , Jun-26, Volume: 78, Issue:6, 2015
Design and synthesis of novel tri-aryl CB2 selective cannabinoid ligands.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 19, Issue:6, 2009
Quantitative structure-activity relationship (QSAR) for a series of novel cannabinoid derivatives using descriptors derived from semi-empirical quantum-chemical calculations.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Exploring the substituent effects on a novel series of C1'-dimethyl-aryl Delta8-tetrahydrocannabinol analogs.Bioorganic & medicinal chemistry, , Jul-01, Volume: 16, Issue:13, 2008
The application of 3D-QSAR studies for novel cannabinoid ligands substituted at the C1' position of the alkyl side chain on the structural requirements for binding to cannabinoid receptors CB1 and CB2.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
Design of Negative and Positive Allosteric Modulators of the Cannabinoid CBJournal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
The Essential Medicinal Chemistry of Cannabidiol (CBD).Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Plant-Based Modulators of Endocannabinoid Signaling.Journal of natural products, , 03-22, Volume: 82, Issue:3, 2019
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Emerging targets in osteoporosis disease modification.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.Bioorganic & medicinal chemistry, , 03-01, Volume: 33, 2021
[no title available]Journal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Discovery of novel benzofuran-based compounds with neuroprotective and immunomodulatory properties for Alzheimer's disease treatment.European journal of medicinal chemistry, , Sep-15, Volume: 178, 2019
Dual-Acting Cholinesterase-Human Cannabinoid Receptor 2 Ligands Show Pronounced Neuroprotection in Vitro and Overadditive and Disease-Modifying Neuroprotective Effects in Vivo.Journal of medicinal chemistry, , 10-24, Volume: 62, Issue:20, 2019
[no title available]European journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
[no title available]Journal of medicinal chemistry, , 02-22, Volume: 61, Issue:4, 2018
Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
[no title available]European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Discovery of novel Tetrahydrobenzo[b]thiophene and pyrrole based scaffolds as potent and selective CB2 receptor ligands: The structural elements controlling binding affinity, selectivity and functionality.European journal of medicinal chemistry, , Oct-21, Volume: 122, 2016
Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 7. Synthesis and Pharmacological Evaluation of 4-Quinolone-3-carboxamides and 4-Hydroxy-2-quinolone-3-carboxamides as High Affinity Cannabinoid Receptor 2 (CB2R) Ligands with Improved Aqueous SoluJournal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Synthesis, pharmacological evaluation and docking studies of pyrrole structure-based CB2 receptor antagonists.European journal of medicinal chemistry, , Aug-28, Volume: 101, 2015
The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxJournal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Rational design, synthesis and anti-proliferative properties of new CB2 selective cannabinoid receptor ligands: an investigation of the 1,8-naphthyridin-2(1H)-one scaffold.European journal of medicinal chemistry, , Volume: 52, 2012
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Contributions of academic laboratories to the discovery and development of chemical biology tools.Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Development of CoMFA and CoMSIA models of affinity and selectivity for indole ligands of cannabinoid CB1 and CB2 receptors.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 15, Issue:16, 2005
A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
[no title available]Journal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Synthesis of novel 2-(1-adamantanylcarboxamido)thiophene derivatives. Selective cannabinoid type 2 (CB2) receptor agonists as potential agents for the treatment of skin inflammatory disease.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Alkyl indole-based cannabinoid type 2 receptor tools: Exploration of linker and fluorophore attachment.European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
[no title available]European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system.European journal of medicinal chemistry, , Jun-25, Volume: 154, 2018
Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Synthesis and biological evaluation of bivalent cannabinoid receptor ligands based on hCB₂R selective benzimidazoles reveal unexpected intrinsic properties.Bioorganic & medicinal chemistry, , Aug-01, Volume: 22, Issue:15, 2014
Mechanisms of osteoclastogenesis inhibition by a novel class of biphenyl-type cannabinoid CB(2) receptor inverse agonists.Chemistry & biology, , Aug-26, Volume: 18, Issue:8, 2011
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Emerging targets in osteoporosis disease modification.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
6-Methoxy-N-alkyl isatin acylhydrazone derivatives as a novel series of potent selective cannabinoid receptor 2 inverse agonists: design, synthesis, and binding mode prediction.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 17, Issue:23, 2007
Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 2005
( R)- N-(1-Methyl-2-hydroxyethyl)-13-( S)-methyl-arachidonamide (AMG315): A Novel Chiral Potent Endocannabinoid Ligand with Stability to Metabolizing Enzymes.Journal of medicinal chemistry, , 10-11, Volume: 61, Issue:19, 2018
[no title available]Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Total synthesis of photoactivatable or fluorescent anandamide probes: novel bioactive compounds with angiogenic activity.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Oxyhomologues of anandamide and related endolipids: chemoselective synthesis and biological activity.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Synthesis of a potential photoactivatable anandamide analog.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 16, Issue:14, 2006
New metabolically stable fatty acid amide ligands of cannabinoid receptors: Synthesis and receptor affinity studies.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 2006
Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors.Journal of medicinal chemistry, , Dec-20, Volume: 44, Issue:26, 2001
A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
[no title available]Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Development of endocannabinoid-based chemical probes for the study of cannabinoid receptors.Journal of medicinal chemistry, , Jul-28, Volume: 54, Issue:14, 2011
Resorcinol-sn-glycerol derivatives: novel 2-arachidonoylglycerol mimetics endowed with high affinity and selectivity for cannabinoid type 1 receptor.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Synthesis and biological evaluation of several structural analogs of 2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand.Bioorganic & medicinal chemistry, , Jan-15, Volume: 15, Issue:2, 2007
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Oxyhomologues of anandamide and related endolipids: chemoselective synthesis and biological activity.Journal of medicinal chemistry, , Apr-06, Volume: 49, Issue:7, 2006
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
Carbon-silicon switch led to the discovery of novel synthetic cannabinoids with therapeutic effects in a mouse model of multiple sclerosis.European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
The endocannabinoid system dual-target ligand N-cycloheptyl-1,2-dihydro-5-bromo-1-(4-fluorobenzyl)-6-methyl-2-oxo-pyridine-3-carboxamide improves disease severity in a mouse model of multiple sclerosis.European journal of medicinal chemistry, , Dec-15, Volume: 208, 2020
Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity.Bioorganic & medicinal chemistry, , 06-01, Volume: 28, Issue:11, 2020
New cannabinoid receptor antagonists as pharmacological tool.Bioorganic & medicinal chemistry, , 10-01, Volume: 28, Issue:19, 2020
Isolation of a High-Affinity Cannabinoid for the Human CB1 Receptor from a Medicinal Journal of natural products, , 01-24, Volume: 83, Issue:1, 2020
Benzo[d]thiazol-2(3H)-ones as new potent selective CBEuropean journal of medicinal chemistry, , Mar-01, Volume: 165, 2019
Polypharmacological profile of 1,2-dihydro-2-oxo-pyridine-3-carboxamides in the endocannabinoid system.European journal of medicinal chemistry, , Jun-25, Volume: 154, 2018
[no title available]European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
[no title available]Bioorganic & medicinal chemistry, , 01-01, Volume: 26, Issue:1, 2018
[no title available]European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CBMedChemComm, , Aug-01, Volume: 8, Issue:8, 2017
Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Identification of Novel GPR55 Modulators Using Cell-Impedance-Based Label-Free Technology.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Synthesis, binding assays, cytotoxic activity and docking studies of benzimidazole and benzothiophene derivatives with selective affinity for the CB2 cannabinoid receptor.European journal of medicinal chemistry, , Nov-29, Volume: 124, 2016
Synthesis and structure activity relationship investigation of triazolo[1,5-a]pyrimidines as CB2 cannabinoid receptor inverse agonists.European journal of medicinal chemistry, , May-04, Volume: 113, 2016
Synthesis, pharmacological evaluation and docking studies of pyrrole structure-based CB2 receptor antagonists.European journal of medicinal chemistry, , Aug-28, Volume: 101, 2015
Combining Mass Spectrometric Metabolic Profiling with Genomic Analysis: A Powerful Approach for Discovering Natural Products from Cyanobacteria.Journal of natural products, , Jul-24, Volume: 78, Issue:7, 2015
Conformational Restriction Leading to a Selective CB2 Cannabinoid Receptor Agonist Orally Active Against Colitis.ACS medicinal chemistry letters, , Feb-12, Volume: 6, Issue:2, 2015
Functionalization of β-caryophyllene generates novel polypharmacology in the endocannabinoid system.ACS chemical biology, , Jul-18, Volume: 9, Issue:7, 2014
One-pot heterogeneous synthesis of Δ(3)-tetrahydrocannabinol analogues and xanthenes showing differential binding to CB(1) and CB(2) receptors.European journal of medicinal chemistry, , Oct-06, Volume: 85, 2014
Structure-affinity relationships and pharmacological characterization of new alkyl-resorcinol cannabinoid receptor ligands: Identification of a dual cannabinoid receptor/TRPA1 channel agonist.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease.European journal of medicinal chemistry, , Feb-12, Volume: 73, 2014
Switching cannabinoid response from CB(2) agonists to FAAH inhibitors.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 24, Issue:5, 2014
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Synthetic cannabinoid quinones: preparation, in vitro antiproliferative effects and in vivo prostate antitumor activity.European journal of medicinal chemistry, , Volume: 70, 2013
Development of fluorinated CB(2) receptor agonists for PET studies.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
Discovery of agonists of cannabinoid receptor 1 with restricted central nervous system penetration aimed for treatment of gastroesophageal reflux disease.Journal of medicinal chemistry, , Jan-10, Volume: 56, Issue:1, 2013
Mastering tricyclic ring systems for desirable functional cannabinoid activity.European journal of medicinal chemistry, , Volume: 69, 2013
Evaluation of (Z)-2-((1-benzyl-1H-indol-3-yl)methylene)-quinuclidin-3-one analogues as novel, high affinity ligands for CB1 and CB2 cannabinoid receptors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 23, Issue:7, 2013
Contributions of academic laboratories to the discovery and development of chemical biology tools.Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
3-Carboxamido-5-aryl-isoxazoles as new CB2 agonists for the treatment of colitis.Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
Novel antiobesity agents: synthesis and pharmacological evaluation of analogues of Rimonabant and of LH21.Bioorganic & medicinal chemistry, , Apr-01, Volume: 21, Issue:7, 2013
Design, synthesis, and pharmacological properties of new heteroarylpyridine/heteroarylpyrimidine derivatives as CB(2) cannabinoid receptor partial agonists.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Synthesis and pharmacology of 1-alkyl-3-(1-naphthoyl)indoles: steric and electronic effects of 4- and 8-halogenated naphthoyl substituents.Bioorganic & medicinal chemistry, , Mar-15, Volume: 20, Issue:6, 2012
Scaffold hopping strategy toward original pyrazolines as selective CB₂ receptor ligands.European journal of medicinal chemistry, , Volume: 58, 2012
4-Oxo-1,4-dihydropyridines as selective CB₂ cannabinoid receptor ligands. Part 2: discovery of new agonists endowed with protective effect against experimental colitis.Journal of medicinal chemistry, , Oct-25, Volume: 55, Issue:20, 2012
7-Oxo-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxamides as selective CB(2) cannabinoid receptor ligands: structural investigations around a novel class of full agonists.Journal of medicinal chemistry, , Jul-26, Volume: 55, Issue:14, 2012
N-Methyl-3-(tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamides as a novel class of cannabinoid receptors agonists with low CNS penetration.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Resorcinol-sn-glycerol derivatives: novel 2-arachidonoylglycerol mimetics endowed with high affinity and selectivity for cannabinoid type 1 receptor.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity.European journal of medicinal chemistry, , Volume: 46, Issue:10, 2011
Bioactive prenylogous cannabinoid from fiber hemp (Cannabis sativa).Journal of natural products, , Sep-23, Volume: 74, Issue:9, 2011
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Cannabinomimetic lipid from a marine cyanobacterium.Journal of natural products, , Oct-28, Volume: 74, Issue:10, 2011
Two distinct classes of novel pyrazolinecarboxamides as potent cannabinoid CB1 receptor agonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 20, Issue:17, 2010
Synthesis and biological evaluation of new potential inhibitors of N-acylethanolamine hydrolyzing acid amidase.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 20, Issue:24, 2010
4-Oxo-1,4-dihydropyridines as selective CB2 cannabinoid receptor ligands: structural insights into the design of a novel inverse agonist series.Journal of medicinal chemistry, , Nov-25, Volume: 53, Issue:22, 2010
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Synthesis and pharmacological evaluation of coumarin derivatives as cannabinoid receptor antagonists and inverse agonists.Bioorganic & medicinal chemistry, , Apr-01, Volume: 17, Issue:7, 2009
New resorcinol-anandamide "hybrids" as potent cannabinoid receptor ligands endowed with antinociceptive activity in vivo.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Discovery and optimization of a novel series of N-arylamide oxadiazoles as potent, highly selective and orally bioavailable cannabinoid receptor 2 (CB2) agonists.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Novel benzimidazole derivatives as selective CB2 agonists.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 18, Issue:13, 2008
Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Design, synthesis, binding, and molecular modeling studies of new potent ligands of cannabinoid receptors.Bioorganic & medicinal chemistry, , Aug-15, Volume: 15, Issue:16, 2007
New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 17, Issue:22, 2007
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 17, Issue:23, 2007
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: discovery of CB2 receptor selective compounds.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 17, Issue:14, 2007
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.Journal of medicinal chemistry, , Aug-09, Volume: 50, Issue:16, 2007
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
New metabolically stable fatty acid amide ligands of cannabinoid receptors: Synthesis and receptor affinity studies.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 16, Issue:1, 2006
1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 15, Issue:18, 2005
Design, synthesis, and binding studies of new potent ligands of cannabinoid receptors.Journal of medicinal chemistry, , Nov-17, Volume: 48, Issue:23, 2005
Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.Journal of medicinal chemistry, , May-22, Volume: 46, Issue:11, 2003
C-3 Amido-indole cannabinoid receptor modulators.Bioorganic & medicinal chemistry letters, , Sep-02, Volume: 12, Issue:17, 2002
Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors.Journal of medicinal chemistry, , Dec-20, Volume: 44, Issue:26, 2001
A 3D-QSAR study on the structural requirements for binding to CB(1) and CB(2) cannabinoid receptors.Journal of medicinal chemistry, , Jun-15, Volume: 43, Issue:12, 2000
Phytocannabinoid Pharmacology: Medicinal Properties of Journal of natural products, , 01-22, Volume: 84, Issue:1, 2021
Plant-Based Modulators of Endocannabinoid Signaling.Journal of natural products, , 03-22, Volume: 82, Issue:3, 2019
Bioactive prenylogous cannabinoid from fiber hemp (Cannabis sativa).Journal of natural products, , Sep-23, Volume: 74, Issue:9, 2011
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Development of endocannabinoid-based chemical probes for the study of cannabinoid receptors.Journal of medicinal chemistry, , Jul-28, Volume: 54, Issue:14, 2011
Resorcinol-sn-glycerol derivatives: novel 2-arachidonoylglycerol mimetics endowed with high affinity and selectivity for cannabinoid type 1 receptor.Journal of medicinal chemistry, , Dec-22, Volume: 54, Issue:24, 2011
New analgesics synthetically derived from the paracetamol metabolite N-(4-hydroxyphenyl)-(5Z,8Z,11Z,14Z)-icosatetra-5,8,11,14-enamide.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Design, synthesis, and biological evaluation of new inhibitors of the endocannabinoid uptake: comparison with effects on fatty acid amidohydrolase.Journal of medicinal chemistry, , Apr-10, Volume: 46, Issue:8, 2003
Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors.Journal of medicinal chemistry, , Dec-20, Volume: 44, Issue:26, 2001
[no title available]Journal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Benzo[d]thiazol-2(3H)-ones as new potent selective CBEuropean journal of medicinal chemistry, , Mar-01, Volume: 165, 2019
Chromenopyrazole, a Versatile Cannabinoid Scaffold with in Vivo Activity in a Model of Multiple Sclerosis.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
Synthesis, biological activity and molecular modeling of new biphenylic carboxamides as potent and selective CB2 receptor ligands.European journal of medicinal chemistry, , Jan-27, Volume: 90, 2015
New quinolone- and 1,8-naphthyridine-3-carboxamides as selective CB2 receptor agonists with anticancer and immuno-modulatory activity.European journal of medicinal chemistry, , Jun-05, Volume: 97, 2015
Functionalization of β-caryophyllene generates novel polypharmacology in the endocannabinoid system.ACS chemical biology, , Jul-18, Volume: 9, Issue:7, 2014
CB2-selective cannabinoid receptor ligands: synthesis, pharmacological evaluation, and molecular modeling investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides.Journal of medicinal chemistry, , Nov-13, Volume: 57, Issue:21, 2014
1,2-Dihydro-2-oxopyridine-3-carboxamides: the C-5 substituent is responsible for functionality switch at CB2 cannabinoid receptor.European journal of medicinal chemistry, , Mar-03, Volume: 74, 2014
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Rational design, synthesis and anti-proliferative properties of new CB2 selective cannabinoid receptor ligands: an investigation of the 1,8-naphthyridin-2(1H)-one scaffold.European journal of medicinal chemistry, , Volume: 52, 2012
Fluorinated cannabinoid CB2 receptor ligands: synthesis and in vitro binding characteristics of 2-oxoquinoline derivatives.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Emerging targets in osteoporosis disease modification.Journal of medicinal chemistry, , Jun-10, Volume: 53, Issue:11, 2010
1-Bromo-3-(1',1'-dimethylalkyl)-1-deoxy-Δ(8)-tetrahydrocannabinols: New selective ligands for the cannabinoid CB(2) receptor.Bioorganic & medicinal chemistry, , Nov-15, Volume: 18, Issue:22, 2010
Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
Rational design, synthesis, and pharmacological properties of new 1,8-naphthyridin-2(1H)-on-3-carboxamide derivatives as highly selective cannabinoid-2 receptor agonists.Journal of medicinal chemistry, , Jun-25, Volume: 52, Issue:12, 2009
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
[no title available]Bioorganic & medicinal chemistry, , 10-01, Volume: 26, Issue:18, 2018
γ-Carbolines: a novel class of cannabinoid agonists with high aqueous solubility and restricted CNS penetration.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 22, Issue:4, 2012
N-Methyl-3-(tetrahydro-2H-pyran-4-yl)-2,3,4,9-tetrahydro-1H-carbazole-6-carboxamides as a novel class of cannabinoid receptors agonists with low CNS penetration.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 22, Issue:12, 2012
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.Journal of medicinal chemistry, , Aug-09, Volume: 50, Issue:16, 2007
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Quantitative structure-activity relationship (QSAR) for a series of novel cannabinoid derivatives using descriptors derived from semi-empirical quantum-chemical calculations.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
The application of 3D-QSAR studies for novel cannabinoid ligands substituted at the C1' position of the alkyl side chain on the structural requirements for binding to cannabinoid receptors CB1 and CB2.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
Synthetic bioactive olivetol-related amides: The influence of the phenolic group in cannabinoid receptor activity.Bioorganic & medicinal chemistry, , 06-01, Volume: 28, Issue:11, 2020
Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CBMedChemComm, , Aug-01, Volume: 8, Issue:8, 2017
Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.Journal of medicinal chemistry, , 07-28, Volume: 59, Issue:14, 2016
New quinolone- and 1,8-naphthyridine-3-carboxamides as selective CB2 receptor agonists with anticancer and immuno-modulatory activity.European journal of medicinal chemistry, , Jun-05, Volume: 97, 2015
Structure-affinity relationships and pharmacological characterization of new alkyl-resorcinol cannabinoid receptor ligands: Identification of a dual cannabinoid receptor/TRPA1 channel agonist.Bioorganic & medicinal chemistry, , Sep-01, Volume: 22, Issue:17, 2014
Development of fluorinated CB(2) receptor agonists for PET studies.Bioorganic & medicinal chemistry, , Dec-01, Volume: 21, Issue:23, 2013
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Design and evaluation of a novel fluorescent CB2 ligand as probe for receptor visualization in immune cells.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 21, Issue:19, 2011
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.Journal of medicinal chemistry, , Oct-08, Volume: 52, Issue:19, 2009
Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 19, Issue:1, 2009
New resorcinol-anandamide "hybrids" as potent cannabinoid receptor ligands endowed with antinociceptive activity in vivo.Journal of medicinal chemistry, , Apr-23, Volume: 52, Issue:8, 2009
Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.Journal of medicinal chemistry, , May-31, Volume: 50, Issue:11, 2007
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.Bioorganic & medicinal chemistry letters, , Dec-01, Volume: 17, Issue:23, 2007
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.Journal of medicinal chemistry, , Jan-12, Volume: 49, Issue:1, 2006
Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB(1) receptor antagonists.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 20, Issue:5, 2010
Discovery and functional evaluation of diverse novel human CB(1) receptor ligands.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Synthesis and evaluation of dibenzothiazepines: a novel class of selective cannabinoid-1 receptor inverse agonists.Journal of medicinal chemistry, , Apr-09, Volume: 52, Issue:7, 2009
Identification of novel cannabinoid CB1 receptor antagonists by using virtual screening with a pharmacophore model.Journal of medicinal chemistry, , Apr-24, Volume: 51, Issue:8, 2008
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.Journal of medicinal chemistry, , Dec-28, Volume: 49, Issue:26, 2006
Novel 3,4-diarylpyrazolines as potent cannabinoid CB1 receptor antagonists with lower lipophilicity.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 15, Issue:21, 2005
Synthesis, biological properties, and molecular modeling investigations of novel 3,4-diarylpyrazolines as potent and selective CB(1) cannabinoid receptor antagonists.Journal of medicinal chemistry, , Jan-29, Volume: 47, Issue:3, 2004
Design, synthesis, biological evaluation, and comparative docking study of 1,2,4-triazolones as CB1 receptor selective antagonists.European journal of medicinal chemistry, , Mar-03, Volume: 74, 2014
Fluorinated cannabinoid CB2 receptor ligands: synthesis and in vitro binding characteristics of 2-oxoquinoline derivatives.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 20, Issue:3, 2010
Synthesis and SAR studies of 2-oxoquinoline derivatives as CB2 receptor inverse agonists.Journal of medicinal chemistry, , Mar-23, Volume: 49, Issue:6, 2006
Triaryl bis-sulfones as a new class of cannabinoid CB2 receptor inhibitors: identification of a lead and initial SAR studies.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 15, Issue:3, 2005
[no title available]MedChemComm, , Nov-01, Volume: 10, Issue:11, 2019
Discovery of a high affinity and selective pyridine analog as a potential positron emission tomography imaging agent for cannabinoid type 2 receptor.Journal of medicinal chemistry, , May-28, Volume: 58, Issue:10, 2015
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Fluorinated cannabinoid CB2 receptor ligands: synthesis and in vitro binding characteristics of 2-oxoquinoline derivatives.Bioorganic & medicinal chemistry, , Sep-15, Volume: 19, Issue:18, 2011
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Imidazopyridine CB2 agonists: optimization of CB2/CB1 selectivity and implications for in vivo analgesic efficacy.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 21, Issue:8, 2011
Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Synthesis and cannabinoid activity of 1-substituted-indole-3-oxadiazole derivatives: novel agonists for the CB1 receptor.European journal of medicinal chemistry, , Volume: 43, Issue:3, 2008
Comparative molecular dynamics simulations of the potent synthetic classical cannabinoid ligand AMG3 in solution and at binding site of the CB1 and CB2 receptors.Bioorganic & medicinal chemistry, , Aug-01, Volume: 16, Issue:15, 2008
The application of 3D-QSAR studies for novel cannabinoid ligands substituted at the C1' position of the alkyl side chain on the structural requirements for binding to cannabinoid receptors CB1 and CB2.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
Novel azoles as potent and selective cannabinoid CB2 receptor agonists.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 25, Issue:1, 2015
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Contributions of academic laboratories to the discovery and development of chemical biology tools.Journal of medicinal chemistry, , Sep-26, Volume: 56, Issue:18, 2013
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
Imine derivatives as new potent and selective CB2 cannabinoid receptor agonists with an analgesic action.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Design and synthesis of novel tri-aryl CB2 selective cannabinoid ligands.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 19, Issue:6, 2009
Quantitative structure-activity relationship (QSAR) for a series of novel cannabinoid derivatives using descriptors derived from semi-empirical quantum-chemical calculations.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Exploring the substituent effects on a novel series of C1'-dimethyl-aryl Delta8-tetrahydrocannabinol analogs.Bioorganic & medicinal chemistry, , Jul-01, Volume: 16, Issue:13, 2008
The application of 3D-QSAR studies for novel cannabinoid ligands substituted at the C1' position of the alkyl side chain on the structural requirements for binding to cannabinoid receptors CB1 and CB2.Journal of medicinal chemistry, , Jun-14, Volume: 50, Issue:12, 2007
Synthesis and testing of novel phenyl substituted side-chain analogues of classical cannabinoids.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 13, Issue:20, 2003
Tricyclic pyrazoles. Part 6. Benzofuro[3,2-c]pyrazole: a versatile architecture for CB2 selective ligands.European journal of medicinal chemistry, , Jul-23, Volume: 82, 2014
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
[no title available]ACS medicinal chemistry letters, , Jun-08, Volume: 8, Issue:6, 2017
Developing pyridazine-3-carboxamides to be CB2 agonists: The design, synthesis, structure-activity relationships and docking studies.European journal of medicinal chemistry, , Sep-08, Volume: 137, 2017
Design, syntheses, structure-activity relationships and docking studies of coumarin derivatives as novel selective ligands for the CB2 receptor.European journal of medicinal chemistry, , Mar-26, Volume: 93, 2015
Development of Quinoline-2,4(1H,3H)-diones as Potent and Selective Ligands of the Cannabinoid Type 2 Receptor.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.Journal of medicinal chemistry, , Oct-08, Volume: 52, Issue:19, 2009
Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
Morpholine containing CB2 selective agonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 19, Issue:6, 2009
Imine derivatives as new potent and selective CB2 cannabinoid receptor agonists with an analgesic action.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 18, Issue:5, 2008
Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.Journal of medicinal chemistry, , May-31, Volume: 50, Issue:11, 2007
[no title available]RSC medicinal chemistry, , Feb-23, Volume: 13, Issue:2, 2022
Synthesis, Molecular Pharmacology, and Structure-Activity Relationships of 3-(Indanoyl)indoles as Selective Cannabinoid Type 2 Receptor Antagonists.Journal of medicinal chemistry, , 05-13, Volume: 64, Issue:9, 2021
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Novel indole and azaindole (pyrrolopyridine) cannabinoid (CB) receptor agonists: design, synthesis, structure-activity relationships, physicochemical properties and biological activity.European journal of medicinal chemistry, , Volume: 46, Issue:10, 2011
Development of CoMFA and CoMSIA models of affinity and selectivity for indole ligands of cannabinoid CB1 and CB2 receptors.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.Journal of medicinal chemistry, , May-27, Volume: 53, Issue:10, 2010
Discovery and functional evaluation of diverse novel human CB(1) receptor ligands.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 19, Issue:15, 2009
Synthesis and evaluation of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-aminopropanamide as human cannabinoid-1 receptor (CB1R) inverse agonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
Biarylpyrazolyl oxadiazole as potent, selective, orally bioavailable cannabinoid-1 receptor antagonists for the treatment of obesity.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Discovery of N-[(1S,2S)-3-(4-Chlorophenyl)-2- (3-cyanophenyl)-1-methylpropyl]-2-methyl-2- {[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist for the treatment of obesity.Journal of medicinal chemistry, , Dec-28, Volume: 49, Issue:26, 2006
Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents.ACS medicinal chemistry letters, , May-10, Volume: 3, Issue:5, 2012
Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
N-(4-cyanotetrahydro-2H-pyran-4-yl) and N-(1-cyanocyclohexyl) derivatives of 1,5-diarylpyrazole-3-carboxamides showing high affinity for 18 kDa translocator protein and/or cannabinoid receptors.Journal of medicinal chemistry, , Apr-28, Volume: 54, Issue:8, 2011
Discovery of N-{(1S,2S)-2-(3-cyanophenyl)- 3-[4-(2-[18F]fluoroethoxy)phenyl]-1-methylpropyl}- 2-methyl-2-[(5-methylpyridin-2-yl)oxy]propanamide, a cannabinoid-1 receptor positron emission tomography tracer suitable for clinical use.Journal of medicinal chemistry, , Jul-26, Volume: 50, Issue:15, 2007
Carbon-silicon switch led to the discovery of novel synthetic cannabinoids with therapeutic effects in a mouse model of multiple sclerosis.European journal of medicinal chemistry, , Dec-15, Volume: 226, 2021
New cannabinoid receptor antagonists as pharmacological tool.Bioorganic & medicinal chemistry, , 10-01, Volume: 28, Issue:19, 2020
[no title available]European journal of medicinal chemistry, , Feb-15, Volume: 127, 2017
Cannabidiol (CBD) and its analogs: a review of their effects on inflammation.Bioorganic & medicinal chemistry, , Apr-01, Volume: 23, Issue:7, 2015
Ligand-based virtual screening identifies a family of selective cannabinoid receptor 2 agonists.Bioorganic & medicinal chemistry, , Jan-01, Volume: 23, Issue:1, 2015
Cannabinoid agonists showing BuChE inhibition as potential therapeutic agents for Alzheimer's disease.European journal of medicinal chemistry, , Feb-12, Volume: 73, 2014
Novel triaryl sulfonamide derivatives as selective cannabinoid receptor 2 inverse agonists and osteoclast inhibitors: discovery, optimization, and biological evaluation.Journal of medicinal chemistry, , Mar-14, Volume: 56, Issue:5, 2013
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Lead discovery, chemistry optimization, and biological evaluation studies of novel biamide derivatives as CB2 receptor inverse agonists and osteoclast inhibitors.Journal of medicinal chemistry, , Nov-26, Volume: 55, Issue:22, 2012
Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids.Bioorganic & medicinal chemistry, , 07-01, Volume: 41, 2021
Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.Journal of medicinal chemistry, , 11-14, Volume: 62, Issue:21, 2019
Novel Diarylurea Based Allosteric Modulators of the Cannabinoid CB1 Receptor: Evaluation of Importance of 6-Pyrrolidinylpyridinyl Substitution.Journal of medicinal chemistry, , 09-14, Volume: 60, Issue:17, 2017
Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.Bioorganic & medicinal chemistry, , 12-15, Volume: 25, Issue:24, 2017
Diarylureas as allosteric modulators of the cannabinoid CB1 receptor: structure-activity relationship studies on 1-(4-chlorophenyl)-3-{3-[6-(pyrrolidin-1-yl)pyridin-2-yl]phenyl}urea (PSNCBAM-1).Journal of medicinal chemistry, , Sep-25, Volume: 57, Issue:18, 2014
Homology modeling in tandem with 3D-QSAR analyses: a computational approach to depict the agonist binding site of the human CB2 receptor.European journal of medicinal chemistry, , Volume: 46, Issue:9, 2011
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Indol-3-ylcycloalkyl ketones: effects of N1 substituted indole side chain variations on CB(2) cannabinoid receptor activity.Journal of medicinal chemistry, , Jan-14, Volume: 53, Issue:1, 2010
Discovery of novel CB2 receptor ligands by a pharmacophore-based virtual screening workflow.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
Imine derivatives as new potent and selective CB2 cannabinoid receptor agonists with an analgesic action.Bioorganic & medicinal chemistry, , Feb-01, Volume: 16, Issue:3, 2008
Indol-3-yl-tetramethylcyclopropyl ketones: effects of indole ring substitution on CB2 cannabinoid receptor activity.Journal of medicinal chemistry, , Mar-27, Volume: 51, Issue:6, 2008
Design of Negative and Positive Allosteric Modulators of the Cannabinoid CBJournal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
Plant-Based Modulators of Endocannabinoid Signaling.Journal of natural products, , 03-22, Volume: 82, Issue:3, 2019
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 22, Issue:8, 2012
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Synthesis and biological evaluation of a ring analogs of the selective CB2 inverse agonist SMM-189.Bioorganic & medicinal chemistry, , 03-01, Volume: 33, 2021
Synthesis and biological evaluation of (3',5'-dichloro-2,6-dihydroxy-biphenyl-4-yl)-aryl/alkyl-methanone selective CB2 inverse agonist.Bioorganic & medicinal chemistry, , Sep-01, Volume: 23, Issue:17, 2015
Design and synthesis of novel tri-aryl CB2 selective cannabinoid ligands.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 19, Issue:6, 2009
Investigations on the 4-Quinolone-3-carboxylic Acid Motif. 7. Synthesis and Pharmacological Evaluation of 4-Quinolone-3-carboxamides and 4-Hydroxy-2-quinolone-3-carboxamides as High Affinity Cannabinoid Receptor 2 (CB2R) Ligands with Improved Aqueous SoluJournal of medicinal chemistry, , Feb-11, Volume: 59, Issue:3, 2016
Three-dimensional quantitative structure-selectivity relationships analysis guided rational design of a highly selective ligand for the cannabinoid receptor 2.European journal of medicinal chemistry, , Volume: 46, Issue:2, 2011
Investigations on the 4-quinolone-3-carboxylic acid motif. 2. Synthesis and structure-activity relationship of potent and selective cannabinoid-2 receptor agonists endowed with analgesic activity in vivo.Journal of medicinal chemistry, , Aug-28, Volume: 51, Issue:16, 2008
Development of CoMFA and CoMSIA models of affinity and selectivity for indole ligands of cannabinoid CB1 and CB2 receptors.European journal of medicinal chemistry, , Volume: 44, Issue:6, 2009
1-Pentyl-3-phenylacetylindoles, a new class of cannabimimetic indoles.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 15, Issue:18, 2005
Benzo[d]thiazol-2(3H)-ones as new potent selective CBEuropean journal of medicinal chemistry, , Mar-01, Volume: 165, 2019
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.Journal of medicinal chemistry, , Nov-14, Volume: 56, Issue:21, 2013
Discovery of S-777469: an orally available CB2 agonist as an antipruritic agent.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 22, Issue:8, 2012
From a Designer Drug to the Discovery of Selective Cannabinoid Type 2 Receptor Agonists with Favorable Pharmacokinetic Profiles for the Treatment of Systemic Sclerosis.Journal of medicinal chemistry, , 01-14, Volume: 64, Issue:1, 2021
Strategies to develop selective CBEuropean journal of medicinal chemistry, , Oct-15, Volume: 180, 2019
Amidoalkylindoles as Potent and Selective Cannabinoid Type 2 Receptor Agonists with in Vivo Efficacy in a Mouse Model of Multiple Sclerosis.Journal of medicinal chemistry, , 08-24, Volume: 60, Issue:16, 2017
Enables
This protein enables 2 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| cannabinoid receptor activity | molecular function | Combining with a cannabinoid to initiate a change in cell activity. Cannabinoids are a class of diverse chemical compounds that include the endocannabinoids and the phytocannabinoids. [GOC:dph, IUPHAR_GPCR:1279, Wikipedia:Cannabinoid] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| extrinsic component of cytoplasmic side of plasma membrane | cellular component | The component of a plasma membrane consisting of gene products and protein complexes that are loosely bound to its cytoplasmic surface, but not integrated into the hydrophobic region. [GOC:mah] |
| perikaryon | cellular component | The portion of the cell soma (neuronal cell body) that excludes the nucleus. [GOC:jl] |
| endoplasmic reticulum | cellular component | The irregular network of unit membranes, visible only by electron microscopy, that occurs in the cytoplasm of many eukaryotic cells. The membranes form a complex meshwork of tubular channels, which are often expanded into slitlike cavities called cisternae. The ER takes two forms, rough (or granular), with ribosomes adhering to the outer surface, and smooth (with no ribosomes attached). [ISBN:0198506732] |
Active In
This protein is active in 2 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| cytoplasm | cellular component | The contents of a cell excluding the plasma membrane and nucleus, but including other subcellular structures. [ISBN:0198547684] |
Involved In
This protein is involved in 12 target(s):
| Target | Category | Definition |
|---|
| response to amphetamine | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an amphetamine stimulus. Amphetamines consist of a group of compounds related to alpha-methylphenethylamine. [GOC:dph, GOC:ef] |
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
| immune response | biological process | Any immune system process that functions in the calibrated response of an organism to a potential internal or invasive threat. [GO_REF:0000022, GOC:add] |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation or inhibition of a nucleotide cyclase activity and a subsequent change in the concentration of a cyclic nucleotide. [GOC:mah, GOC:signaling, ISBN:0815316194] |
| leukocyte chemotaxis | biological process | The movement of a leukocyte in response to an external stimulus. [GOC:add, GOC:jl] |
| negative regulation of synaptic transmission, GABAergic | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of GABAergic synaptic transmission, the process of communication from a neuron to another neuron across a synapse using the neurotransmitter gamma-aminobutyric acid (GABA). [GOC:mah] |
| response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:add, ISBN:0721601464] |
| negative regulation of mast cell activation | biological process | Any process that stops, prevents, or reduces the frequency, rate, or extent of mast cell activation. [GOC:mah] |
| cannabinoid signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a cannabinoid binding to its receptor on the cell surface, and ending with the regulation of a downstream cellular process, e.g. transcription. Cannabinoids are a class of diverse chemical compounds that include the endocannabinoids and the phytocannabinoids. [GOC:bf, GOC:jc, GOC:signaling, Wikipedia:Cannabinoid] |
| negative regulation of action potential | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of action potential creation, propagation or termination. This typically occurs via modulation of the activity or expression of voltage-gated ion channels. [GOC:go_curators] |
| regulation of metabolic process | biological process | Any process that modulates the frequency, rate or extent of the chemical reactions and pathways within a cell or an organism. [GOC:go_curators] |
| adenylate cyclase-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |