Cannabinoid receptors ligands

CB, was identified by radioligand binding techniques and subsequently cloned. A second receptor subclass, CB2, has been identified in human spleen and also has been cloned (34). Table 5 Hsts cannabinoid receptor ligands. 

Pertwee RG. Cannabinoid receptor ligands clinical and neuropharmaco-logical considerations, relevant to future drug discovery and development. Exp Opin Invest Drugs 2000 9 1-19. 

Pertwee RG (1999). Pharmacology of cannabinoid receptor ligands. Current Medical Chemistry, 6, 635-664. 

Goparaju SK, Ueda N, Yamaguchi H, Yamamoto S. (1998). Anandamide amidohydrolase reacting with 2-arachidonoylglycerol, another cannabinoid receptor ligand. FEBS Letters. 422(1) 69-73. 

Romero J, de Miguel R, Garcia-Palomero E, Fernandez-Ruiz JJ, Ramos JA. (1995). Time-course of the effects of anandamide, the putative endogenous cannabinoid receptor ligand, on extrapyramidal function. Brain Res. 694(1-2) 223-32. 

Later, we described the isolation of a second type of cannabinoid receptor ligand, 2-arachidonoyl glycerol (2-AG) (K = 5-85 0.12 xM), an ester isolated from canine gut. " This was the first putative endogenous cannabinoid receptor ligand isolated from a peripheral tissue. Later, Sugiura et al isolated independently this compound from brain. 

SugiuraT, Kondo S, Sukagawa A, Nakane S, Shinoda A, Itoh K, Yamashita A, Waku K, 2-Arachidonoylglycerol A possible endogenous cannabinoid receptor ligand in brain, Biochem Biophys Res Commun 215 89—97, 1995. 

Makriannis, A, Deng, H. (University of Conneticut) Retro-anandamides, high affinity and stability cannabinoid receptor ligands, WO0128498 (2001). 

Straiker A, Mackie K (2005) Depolarization-induced suppression of excitation in murine autaptic hippocampal neurones. J Physiol 569(Pt 2) 501—17 Sullivan JM (2000) Cellular and molecular mechanisms underlying learning and memory impairments produced by cannabinoids. Learn Mem 7(3) 132-9 Sugiura T, Kondo S, Sukagawa A, Nakane S, Shinoda A, Itoh K, Yamashita A, Waku K (1995) 2-Arachidonoylglycerol a possible endogenous cannabinoid receptor ligand in brain. Biochem Biophys Res Commun 215(1) 89—97... 

Nakane, S., Oka, S., Arai, S., Waku, K., Ishima, Y., Tokumura, A., and Sugiura, T. (2002). 2-Arachidonoyl-sn-glycero-3-phosphate, an arachidonic acid-containing lysophosphatidic acid Occurrence and rapid enzymatic conversion to 2-arachidonoyl-sn-glycerol, a cannabinoid receptor ligand, in rat brain. Arch. Biochem. Biophys. 402, 51-58. 

Patel, S., and Hillard, C.J. (2006). Pharmacological evaluation of cannabinoid receptor ligands in a mouse model of anxiety Further evidence for an anxiolytic role for endogenous cannabinoid signaling.. Pharmacol. Exp. Ther. 318, 304-311. 

Bisogno T (2008) Endogenous cannabinoids structure and metabohsm. J Neuroendociinol 20 1-9 Bisogno T, Melck D, Bobrov MY, Gretskaya NM, Bezuglov VV, De Petrocellis L, Di Marzo V (2000) N-acyl-dopamines novel synthetic CBl cannabinoid-receptor ligands and inhibitors of anandamide inactivation with cannabimemetic activity in vitro and in vivo. Biochem J 351 817-824... 

Sugiura, T., Kondo, S., Kishimoto, S., Miyashita, T., Nakan, S., Kodaka, T., et al. (2000). Evidence that 2-arachidonoylglycerol but no N-palmitoylethanolamine or anandamide is the physiological ligand for the cannabinoid CB2 receptor. Comparison of the agonistic activities of various cannabinoid receptor ligands in HL-60 cells. Journal of Biological Chemistry, 275, 605-612. 

Arachidonoylglycerol a possible endogenous cannabinoid receptor ligand in brain. Biochem Biophys Res Commun 215 89-97... 

Ooms, F., Wouters, J., Oscari, O., Happaerts, T., Bouchard, G., Carrupt, R A., Testa, B., Lambert, D. M. Exploration of the pharmacophore of 3-alkyl-5-arylimidazoUdinediones as new CB(1) cannabinoid receptor ligands and potential antagonists synthesis, lipophihcity, affinity, and molecular modelUng. J. Med. Chem. 2002, 45(9), 1748-1756. 

Several cannabinoid receptor ligands have been radiolabelled with tritium, and these have been used both to determine the CB 1 and CB2 receptor affinities of unlabelled cannabinoids in displacement assays and to establish the tissue distribution patterns of these receptors (reviewed in Howlett et al. 2002 Pertwee 1999a). As indicated in Tables 1,2 and 3, some of these compounds bind more readily to CBi or to CB2 receptors, whilst the others bind more or less equally well to both these... 

Di Marzo V, Melck D, Bisogno T, De Petrocellis L (1998) Endocannabinoids endogenous cannabinoid receptor ligands with neuromodulatory action. Trends Neurosci 21 521— 528... 

Di Marzo V, Bisogno T, De Petrocellis L, Brandi I, Jefferson RG, Winckler RL, Davis JB, Dasse O, Mahadevan A, Razdan RK, Martin BR (2001) Highly selective CBI cannabinoid receptor ligands and novel CB 1/VR1 vanilloid receptor hybrid ligands. Biochem Biophys Res Commun 281 444-451... 

Suhara Y, Takayama H, Nakane S, Miyashita T, Waku K, Sugiura T (2000) Synthesis and biological activities of 2-arachidonoylglycerol, an endogenous cannabinoid receptor ligand, and its metabolicaUy stable ether-linked analogues. Chem Pharm Bull (Tokyo) 48 903-907... 

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