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*  AM-630
... is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2, with a Ki of 32.1 nM at CB2 and ... May 2010). "Brain cannabinoid CB2 receptor in schizophrenia". Biological Psychiatry. 67 (10): 974-82. doi:10.1016/j.biopsych. ... February 1999). "Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656, and AM630 ... It is used in the study of CB2 mediated responses and has been used to investigate the possible role of CB2 receptors in the ...
*  JWH-015
Ghosh S, Preet A, Groopman JE, Ganju RK (July 2006). "Cannabinoid receptor CB2 modulates the CXCL12/CXCR4-mediated chemotaxis ... Montecucco F, Burger F, Mach F, Steffens S (March 2008). "CB2 cannabinoid receptor agonist JWH-015 modulates human monocyte ... an aminoalkylindole agonist for the peripheral cannabinoid receptor (CB2) by HPLC-MS/MS". Analytical and Bioanalytical ... Its affinity for CB2 receptors is 13.8 nM, while its affinity for CB1 is 383 nM, meaning that it binds almost 28x more strongly ...
*  QMPSB
"Sulfamoyl benzamides as novel CB2 cannabinoid receptor ligands". Bioorganic & Medicinal Chemistry Letters. 18 (9): 2830-2835. ... It acts as a full agonist of the CB1 receptor and CB2 receptor with Ki values of 3 nM and 4 nM, respectively. A large number of ... "Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity". Bioorganic & Medicinal Chemistry Letters. 18 ( ... with the main focus of this work being to increase selectivity for the non-psychoactive CB2 receptor. This work led on from an ...
*  NAGly receptor
endoCANNABINOIDS: actions at non-CB1/CB2 cannabinoid receptors. New York: Springer. ISBN 978-1-4614-4668-2. Chiang N, Dalli J, ... N-Arachidonyl glycine receptor (NAGly receptor), also known as G protein-coupled receptor 18 (GPR18), is a protein that in ... Along with the other previously "orphan" receptors GPR55 and GPR119, GPR18 has been found to be a receptor for endogenous lipid ... several of which also bind to cannabinoid receptors. Research supports the hypothesis that GPR18 is the abnormal cannabidiol ...
*  Cannabinoid
... a CB2 receptor antagonist WIN 55,212-2, a potent cannabinoid receptor agonist JWH-133, a potent selective CB2 receptor agonist ... It acts as an α2-adrenergic receptor agonist, 5-HT1A receptor antagonist, and CB1 receptor antagonist. It also binds to the CB2 ... The human brain has more cannabinoid receptors than any other G protein-coupled receptor (GPCR) type. CB1 receptors are found ... a potent cannabinoid receptor agonist Cannabinoid receptor antagonist Endocannabinoid enhancer Endocannabinoid reuptake ...
*  Cannabinol
... and preferentially binds to the cannabinoid G-protein coupled receptor CB2, which is mainly expressed on a variety of immune ... "Novel cannabinol probes for CB1 and CB2 cannabinoid receptors". Journal of Medicinal Chemistry. 43 (20): 3778-85. doi:10.1021/ ... CBN acts as a partial agonist at the CB1 receptors, but has a higher affinity to CB2 receptors; however, it has lower ... Stimulation of CB2 receptors by cannabinol may both trigger apoptosis in these cells and inhibit the production of a variety of ...
*  Islands of Calleja
Cannabinoid receptor CB2: The cannabinoid receptors are a class of G protein-coupled receptors that bind either internally or ... Cannabinoid CB2 receptors: Immunohistochemical localization in rat brain. Brain Research 1071:10-23 Hargreaves GA, Hunt GE, ... While the CB1 variant of the receptor has a pre-synaptic localization, it is thought that the CB2 receptors may possess a post- ... Muscarinic acetylcholine receptor M4: The muscarinic acetylcholine receptors are types of G protein-coupled receptors that ...
*  GW-405,833
CB1 and CB2 cannabinoid receptors are implicated in inflammatory pain. Pain. 2002 Apr;96(3):253-60. PMID 11972997 Valenzano KJ ... GW-405,833 (L-768,242) is a drug that acts as a potent and selective partial agonist for the cannabinoid receptor subtype CB2, ... PMID 15814101 Beltramo M, Bernardini N, Bertorelli R, Campanella M, Nicolussi E, Fredduzzi S, Reggiani A. CB2 receptor-mediated ... The search for selective ligands for the CB2 receptor. Current Pharmaceutical Design. 2000 Sep;6(13):1323-37. doi:10.2174/ ...
*  AM-1241
"Activation of CB2 cannabinoid receptors by AM1241 inhibits experimental neuropathic pain: pain inhibition by receptors not ... February 2005). "CB2 cannabinoid receptor activation produces antinociception by stimulating peripheral release of endogenous ... Kim K, Moore DH, Makriyannis A, Abood ME (August 2006). "AM1241, a cannabinoid CB2 receptor selective compound, delays disease ... August 2007). "Species-specific in vitro pharmacological effects of the cannabinoid receptor 2 (CB2) selective ligand AM1241 ...
*  SR-144,528
"CB2 cannabinoid receptor antagonist SR144528 decreases μ-opioid receptor expression and activation in mouse brainstem: Role of ... SR144528 is a drug that acts as a potent and highly selective CB2 receptor inverse agonist, with a Ki of 0.6 nM at CB2 and 400 ... Nackley, A. G; Makriyannis, A; Hohmann, A. G (4 July 2003). "Selective activation of cannabinoid CB2 receptors suppresses ... "Mutational analysis and molecular modelling of the antagonist SR 144528 binding site on the human cannabinoid CB2 receptor". ...
*  UR-144
"Targeting the cannabinoid CB2 receptor: modelling and structural determinants of CB2 selective ligands". Br. J. Pharmacol. 153 ... UR-144 has high affinity for the CB2 receptor with a Ki of 1.8 nM but 83x lower affinity for the CB1 receptor with a Ki of 150 ... 2010). "Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB2 Cannabinoid Receptor ... UR-144 was found to possess an EC50 of 421 nM for human CB1 receptors, and 72 nM for human CB2 receptors. UR-144 produces ...
*  HU-308
... is a drug that acts as a cannabinoid agonist. It is highly selective for the CB2 receptor subtype, with a selectivity of ... Labuda, C.; Koblish, M.; Little, P. (2005). "Cannabinoid CB2 receptor agonist activity in the hindpaw incision model of ... 2007). "CB2-receptor stimulation attenuates TNF-α-induced human endothelial cell activation, transendothelial migration of ... 2006). "Non-psychoactive CB2 cannabinoid agonists stimulate neural progenitor proliferation". The FASEB Journal. 20 (13): 2405- ...
*  A-834,735
Poso, A.; Huffman, J. W. (2008). "Targeting the cannabinoid CB2 receptor: modelling and structural determinants of CB2 ... 2010). "Indol-3-ylcycloalkyl Ketones: Effects of N1 Substituted Indole Side Chain Variations on CB2 Cannabinoid Receptor ... 2008). "Indol-3-yl-tetramethylcyclopropyl Ketones: Effects of Indole Ring Substitution on CB2 Cannabinoid Receptor Activity". ... drug developed by Abbott Laboratories that acts as a potent cannabinoid receptor full agonist at both the CB1 and CB2 receptors ...
*  JWH-019
Poso A, Huffman JW (January 2008). "Targeting the cannabinoid CB2 receptor: modelling and structural determinants of CB2 ... "Cannabinoid CB1 and CB2 receptor ligand specificity and the development of CB2-selective agonists". Current Medicinal Chemistry ... is an analgesic chemical from the naphthoylindole family that acts as a cannabinoid agonist at both the CB1 and CB2 receptors. ... and may be useful in characterising the active site of the CB1 and CB2 receptors. As of October 2015 JWH-019 is a controlled ...
*  CBS-0550
... which acts as a potent and selective cannabinoid CB2 receptor agonist, with 1400x selectivity for CB2 over the related CB1 ... Imine derivatives as new potent and selective CB2 cannabinoid receptor agonists with an analgesic action. Bioorganic and ... "N-Alkylidenearylcarboxamides as new potent and selective CB2 cannabinoid receptor agonists with good oral bioavailability". ... receptor. Unlike most cannabinoid agonists, CBS-0550 has good solubility in water, and in animal studies it was found to ...
*  Abnormal cannabidiol
Jarai, Z. (1999). "Cannabinoid-induced mesenteric vasodilation through an endothelial site distinct from CB1 or CB2 receptors ... McCollum, L; Howlett, AC; Mukhopadhyay, S (2007). "Anandamide-mediated CB1/CB2 cannabinoid receptor-independent nitric oxide ... Cannabinoids Cannabinoid receptors Cannabidiol O-1918 Rimonabant Adams, MD; Earnhardt, JT; Martin, BR; Harris, LS; Dewey, WL; ... "The orphan receptor GPR55 is a novel cannabinoid receptor". British Journal of Pharmacology. 152 (7): 1092-1101. doi:10.1038/sj ...
*  2-Arachidonyl glyceryl ether
"The endocannabinoid noladin ether acts as a full agonist at human CB2 cannabinoid receptors". J. Pharmacol. Exp. Ther. 314 (2 ... 3 µM at the Cannabinoid receptor type 1 and the peripheral cannabinoid receptors. The presence of 2-AGE in body tissue is ... 2-AGE binds with a Ki of 21 nM to the CB1 receptor and 480 nM to the CB2 receptor. It shows agonistic behaviour on both ... After binding to CB2 receptors it inhibits adenylate cyclase and stimulates ERK-MAPK and regulates calcium transients. In ...
*  SDB-005
It is presumed to be an agonist of the CB1 and CB2 cannabinoid receptors. SDB-005 is the indazole core analogue of PB-22 where ... This compound is a potent agonist of the CB1 receptor (Ki = 21 nM) and CB2 receptor (Ki = 140 nM). However SDB-005 was ... Consequently, there are now two distinct, yet fairly closely related cannabinoid compounds, which may both be referred to under ... SDB-005 is an indazole-based synthetic cannabinoid that has been sold online as a designer drug. ...
*  JTE-907
2001). "In vitro and in vivo pharmacological characterization of JTE-907, a novel selective ligand for cannabinoid CB2 receptor ... 2005). "Involvement of cannabinoid CB(2) receptor-mediated response and efficacy of cannabinoid CB(2) receptor inverse agonist ... Ueda, Y; Miyagawa, N; Wakitani, K (2007). "Involvement of cannabinoid CB2 receptors in the IgE-mediated triphasic cutaneous ... It has antiinflammatory effects in animal studies, thought to be mediated by an interaction between the CB2 receptor and IgE. ...
*  Canbisol
"Functional role of serine residues of transmembrane dopamin VII in signal transduction of CB2 cannabinoid receptor". Journal of ... It is a potent agonist at both the CB1 and CB2 receptors, with a binding affinity of 0.1nM at CB1 and 0.2nM at CB2. It is ... in receptor binding studies to determine the structure and function of the cannabinoid receptors, but has been made illegal in ... July 2005). "Cysteine 2.59(89) in the second transmembrane domain of human CB2 receptor is accessible within the ligand binding ...
*  Honokiol
... is a weak cannabinoid CB2 receptor ligand but the naturally occurring derivative 4-O-methylhonokiol was shown to be a ... "Mechanisms of Osteoclastogenesis Inhibition by a Novel Class of Biphenyl-Type Cannabinoid CB2 Receptor Inverse Agonists". ... potent and selective cannabinoid CB2 receptor inverse agonist and to possess antiosteoclastic effects. Honokiol inhibits ... GABAA receptors control ligand-gated Cl− channels that can help increase seizure thresholds through the influx of chloride ...
*  N-Acylamides
Anandamide activates the cannabinoid receptors CB1 and CB2. FAAH knockout mice show increased anandamide levels in vivo and ... "Opportunistic activation of TRP receptors by endogenous lipids: Exploiting lipidomics to understand TRP receptor cellular ... an orthologue of vertebrate cannabinoid receptors in the urochordate Ciona intestinalis. Gene, 302(1), 95-101. Fezza, F., ... cannabinoid-receptor dependent behaviors including antinociception and anxiolysis. GPR18, GPR55, GPR92 have also been proposed ...
*  L-759,633
... is an analgesic drug that is a cannabinoid agonist. It is a fairly selective agonist for the CB2 receptor, with ... "Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630". British Journal ... Huffman JW (2005). "CB2 receptor ligands". Mini reviews in medicinal chemistry. 5 (7): 641-9. doi:10.2174/1389557054368844. ... Huffman JW (2000). "The search for selective ligands for the CB2 receptor". Current pharmaceutical design. 6 (13): 1323-37. doi ...
*  L-759,656
... is an analgesic drug that is a cannabinoid agonist. It is a highly selective agonist for the CB2 receptor, with ... "Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656, and AM630". British Journal ... Huffman, J. W. (2000). "The search for selective ligands for the CB2 receptor". Current pharmaceutical design. 6 (13): 1323- ... Huffman, J. W. (2005). "CB2 receptor ligands". Mini reviews in medicinal chemistry. 5 (7): 641-649. doi:10.2174/ ...
*  WIN 54,461
... (6-Bromopravadoline) is a drug that acts as a potent and selective inverse agonist for the cannabinoid receptor CB2 ... "Cannabinoid Receptor Agonists and Antagonists". Current Pharmaceutical Design. 1 (3): 343-352. ...
*  JWH-424
... which acts as a cannabinoid agonist at both the CB1 and CB2 receptors, but with moderate selectivity for CB2, having a Ki of ... EFFECTS OF HALOGEN SUBSTITUENTS UPON CB1 AND CB2 RECEPTOR AFFINITIES IN THE SERIES OF N-ALKYL-3-(8-HALO-1-NAPTHOYL)INDOLES. ( ... STRUCTURE-ACTIVITY RELATIONSHIPS AT THE CB1 AND CB2 RECEPTORS FOR 1-ALKYL-3-(1-NAPHTHOYL-4 AND 8-HALOGEN SUBSTITUTED) INDOLES ( ... The heavier 8-iodo analogue is even more CB2 selective, with its 2-methyl derivative having 40x selectivity for CB2. However ...