![[Feedback]](/icons/banner/feedbackACT.gif){kind=icon}
![[For Subscribers]](/icons/banner/subscriberACT.gif){kind=icon}
![[Archive]](/icons/banner/archiveACT.gif){kind=icon}
![[Search]](/icons/banner/searchACT.gif){kind=icon}
![[Contents]](/icons/banner/tocACT.gif){kind=icon}
|
|
|
|
|
||
Vol. 285, Issue 1, 285-292, April 1998
Research Triangle Institute, Research Triangle Park, North Carolina
To further characterize neuronal cannabinoid receptors, we compared the
ability of known and novel cannabinoid analogs to compete for receptor
sites labeled with either [3H]SR141716A or
[3H]CP-55,940. These efforts were also directed toward
extending the structure-activity relationships for cannabinoid agonists and antagonists. A series of alternatively halogenated analogs of
SR141716A were synthesized and tested in rat brain membrane binding
assays along with the classical cannabinoids,
9-tetrahydrocannabinol, cannabinol, cannabidiol, the
nonclassical cannabinoid CP-55,940, the aminoalkylindole WIN55212-2
and the endogenous fatty acid ethanolamide, anandamide. Saturation
binding isotherms were performed with both radioligands, as were
displacement studies, allowing an accurate comparison to be made
between the binding of these various compounds. Competition studies
demonstrated that all of the compounds were able to displace the
binding of [3H]CP-55,940 with rank order potencies that
agreed with previous studies. However, the rank order potencies of
these compounds in competition studies with [3H]SR141716A
differed significantly from those determined with [3H]CP-55,940. These results suggest that CP-55,940,
WIN55212-2 and other agonists interact with cannabinoid binding sites
within the brain which are distinguishable from the population of
binding sites for SR141716A, its analogs and cannabidiol. Structural
modification of SR141716A significantly altered the affinity of the
compound and its relative ability to displace either
[3H]CP-55,940 or [3H]SR141716A
preferentially within the rat brain receptor membrane preparation.
This article has been cited by other articles:
|
|
 |
|
  H. Pan, P. Mukhopadhyay, M. Rajesh, V. Patel, B. Mukhopadhyay, B. Gao, G. Hasko, and P. Pacher Cannabidiol Attenuates Cisplatin-Induced Nephrotoxicity by Decreasing Oxidative/Nitrosative Stress, Inflammation, and Cell Death J. Pharmacol. Exp. Ther., March 1, 2009; 328(3): 708 - 714. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 P. Fusar-Poli, J. A. Crippa, S. Bhattacharyya, S. J. Borgwardt, P. Allen, R. Martin-Santos, M. Seal, S. A. Surguladze, C. O'Carrol, Z. Atakan, et al. Distinct Effects of {Delta}9-Tetrahydrocannabinol and Cannabidiol on Neural Activation During Emotional Processing Arch Gen Psychiatry, January 1, 2009; 66(1): 95 - 105. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 J.-K. Chen, J. Chen, J. D. Imig, S. Wei, D. L. Hachey, J. S. Guthi, J. R. Falck, J. H. Capdevila, and R. C. Harris Identification of Novel Endogenous Cytochrome P450 Arachidonate Metabolites with High Affinity for Cannabinoid Receptors J. Biol. Chem., September 5, 2008; 283(36): 24514 - 24524. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
K. E. Hutchison, H. Haughey, M. Niculescu, J. Schacht, A. Kaiser, J. Stitzel, W. J. Horton, and F. Filbey The Incentive Salience of Alcohol: Translating the Effects of Genetic Variant in CNR1 Arch Gen Psychiatry, July 1, 2008; 65(7): 841 - 850. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 D. McHugh, C. Tanner, R. Mechoulam, R. G. Pertwee, and R. A. Ross Inhibition of Human Neutrophil Chemotaxis by Endogenous Cannabinoids and Phytocannabinoids: Evidence for a Site Distinct from CB1 and CB2 Mol. Pharmacol., February 1, 2008; 73(2): 441 - 450. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 M. Rajesh, P. Mukhopadhyay, S. Batkai, G. Hasko, L. Liaudet, V. R. Drel, I. G. Obrosova, and P. Pacher Cannabidiol attenuates high glucose-induced endothelial cell inflammatory response and barrier disruption Am J Physiol Heart Circ Physiol, July 1, 2007; 293(1): H610 - H619. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 G. A. Cabral and F. Marciano-Cabral Cannabinoid receptors in microglia of the central nervous system: immune functional relevance J. Leukoc. Biol., December 1, 2005; 78(6): 1192 - 1197. [Abstract] [Full Text] [PDF]
|
|
|
|
 |
|
 A. C. Howlett, F. Barth, T. I. Bonner, G. Cabral, P. Casellas, W. A. Devane, C. C. Felder, M. Herkenham, K. Mackie, B. R. Martin, et al. International Union of Pharmacology. XXVII. Classification of Cannabinoid Receptors Pharmacol. Rev., June 1, 2002; 54(2): 161 - 202. [Abstract] [Full Text] [PDF]
|
|
|
|
|
|
T.-R. Jan and N. E. Kaminski Role of mitogen-activated protein kinases in the differential regulation of interleukin-2 by cannabinol J. Leukoc. Biol., May 1, 2001; 69(5): 841 - 849. [Abstract] [Full Text]
|
|
|
|
|
|
J. L. Wiley, R. G. Jefferson, M. C. Grier, A. Mahadevan, R. K. Razdan, and B. R. Martin Novel Pyrazole Cannabinoids: Insights into CB1 Receptor Recognition and Activation J. Pharmacol. Exp. Ther., March 1, 2001; 296(3): 1013 - 1022. [Abstract] [Full Text]
|
|
|
|
 |
|
 A. M. Malfait, R. Gallily, P. F. Sumariwalla, A. S. Malik, E. Andreakos, R. Mechoulam, and M. Feldmann The nonpsychoactive cannabis-constituent cannabidiol is an oral anti-arthritic therapeutic in murine collagen-induced arthritis PNAS, July 30, 2000; (2000) 160105897. [Abstract] [Full Text]
|
|
|
|
|
|
A. M. Malfait, R. Gallily, P. F. Sumariwalla, A. S. Malik, E. Andreakos, R. Mechoulam, and M. Feldmann From the Cover: The nonpsychoactive cannabis constituent cannabidiol is an oral anti-arthritic therapeutic in murine collagen-induced arthritis PNAS, August 15, 2000; 97(17): 9561 - 9566. [Abstract] [Full Text] [PDF]
|
|
 |
 |
 |
|
 |
 |
 |
