Cannabinoid receptors hybrid cannabinoids

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... 

Di Marzo, V., Bisogno, T., De Petrocellis, L., et al. (2001) Highly selective CBl cannabinoid receptor ligands and novel CBl/VRl vanilloid receptor hybrid Ug-ands. Biochem. Biophys. Res. Cotrmm. 281,444-451. 

The first identified cannabinoid receptor subtype, CB was cloned and demonstrated to have an amino acid sequence consistent with a tertiary structure typical of the seven transmembrane-spanning proteins that are coupled to G proteins. In addition to being found in the central nervous system, mRNA for CB has also been identified in testes. The central nervous system responses to cannabinoid compounds are believed to be mediated exclusively by CB, inasmuch as CB2 transcripts could not be found in brain tissue by either Northern analysis or in situ hybridization studies. CBj transduces signals in response to central-nervous-system-active constituents of C. sativa as well as synthetic bicyclic and tricyclic cannabinoid analogs, aminoalkylindole, and eicosanoid cannabimimetic compounds. CB is coupled to G, to inhibit adenylate cyclase activity and to a pertussis-sensitive G protein to regulate Ca2+ currents. 

Westlake TM, Howlett AC, Bonner II, Matsuda LA, Herkenham M. 1994. Cannabinoid receptor binding and messenger RNA expression in human brain An in vitro receptor autoradiography and in situ hybridization histochemistry study of normal aged and Alzheimer s brains. Neuroscience 63 637-652. 

Boring DL, Betgjund BA, Howlett AC (1996) Cerebtodiene, arachidonylethanolamide, and hybrid structures potential for interaction with brain cannabinoid receptors. Prostaglandins Leukot Essent Fatty Adds 55 207—210... 

Blount, B.K. Robinson, R. Derivatives of 1-Methyltropane 1933 Boger, L. R. Inhibitors of Fatty Acid Amide Hydrolase 2002 US 6,462,054 Boring D.L, Berglund, B.A, Howlett A.C. Cerebrodiene, Arachidonyl-ethanolamide, and Hybrid Structures Potential for Interaction with Brain Cannabinoid Receptors Prostaglandins Leukot Essent Fatty Acids. (1996) 55(3) 207-10. 

Mailleux, P., and Vanderhaeghen, J.J. Distribution of neuronal cannabinoid receptor in the adult rat brain A comparative receptor binding radioautography and in situ hybridization histochemistry. Neuroscience 48(3) 655-668, 1992. 

Sugiura T, Kodaka T, Kondo S, Tonegawa T, Nakane S, Kishimoto S, Yamashita A, Waku K (1996) 2-Arachidonoylglycerol, a putative endogenous cannabinoid receptor ligand, induces rapid, transient elevation of intracellular free Ca2+ in neuroblastoma x glioma hybrid NG108-15 cells. Biochem Biophys Res Commun 229 58-64... 

Rubino T, Massi P, Patrini G, Venier I, Giagnoni G, Parolaro D (1994) Chronic CP-55,940 alters cannabinoid receptor mRNA in the rat brain an in situ hybridization study. Neuroreport 5 2493-2496... 

Mailleux P, Parmentier M, Vanderhaeghen JJ (1992) Distribution of cannabinoid receptor messenger RNA in the human brain an in situ hybridization histochemistry with oligonucleotides. Neurosci Lett 143 200-204... 

The distribution of cannabinoid receptors has been extensively mapped by quantitative autoradiography, in situ hybridization, and immunocytochemistry. Each of these techniques has its strengths and weaknesses. Properly calibrated, quantitative autoradiography provides the best measure of absolute receptor density. Nonetheless, its spatial resolution is limited and specificity depends on the ligand used. In situ hybridization identifies the cells synthesizing CB i mRNA. However, mRNA levels and protein levels may not necessarily correlate. Immunocytochemistry provides outstanding spatial resolution however, fixation artifacts and unanticipated antibody crossreactivity must be assiduously avoided. For the most... 

Hohmann AG, Herkenham M (1999b) Localization of central cannabinoid CBI receptor messenger RNA in neuronal subpopulations of rat dorsal root ganglia a double-label in situ hybridization study. Neuroscience 90 923-931... 

In 1992, Kaminski and colleagues (Kaminski et al. 1992) demonstrated through an equilibrium binding assay that membranes from mouse spleen had specific binding sites for cannabinoids. In addition, using specific primers for the cannabinoid receptor identified in brain, they amplified from splenic RNA using RNA transcriptase-polymerase chain reaction (RT-PCR), an 854-kb product that hybridized with brain cannabinoid receptor cDNA. These studies demonstrated that... 

Mailleux P, Vanderhaeghen JJ (1993) Dopaminergic regulation of cannabinoid receptor mRNA levels in the rat caudate-putamen an in situ hybridization study. J Neurochem 61 1705-1712... 

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