Cannabinoid receptor interactions with the antagonists SR 141716A and SR 144528
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Cited by (93)
Common Receptors for Endocannabinoid-Like Mediators and Plant Cannabinoids
2015, The Endocannabinoidome: The World of Endocannabinoids and Related MediatorsExamining the critical roles of human CB2 receptor residues Valine 3.32 (113) and Leucine 5.41 (192) in ligand recognition and downstream signaling activities
2014, Biochemical and Biophysical Research CommunicationsCitation Excerpt :Several CB2 binding pocket residues have been confirmed for their importance in agonist and antagonist binding, such as S112, W172, Y190, W194, F197, W258, and S285 [17–24]. Moreover, since the third and fifth transmembrane regions of CB2 receptor are playing curial roles in the binding of the vast majority of cannabinoid ligands and consequent signal transduction [17,25], we investigated the possible roles of V113 of TM3 (position 3.32) and L192 of TM5 (position 5.41) in binding with three structurally diverse CB2 ligands: CP-55,940, a non-classical cannabinoids agonist; SR144528, a diarylpyrazole inverse agonist; and XIE95-26, a biamide derivative inverse agonist [26] (Supplemental Fig. 1). A CB2 homology model was constructed from the antagonist-bound A2A receptor (3EML.
Effects of endogenous cannabinoid anandamide on excitation-contraction coupling in rat ventricular myocytes
2014, Cell CalciumCitation Excerpt :For this purpose, we have first tested the effects of established antagonists of CB1 and CB2 receptors on the AEA inhibition of shortening amplitudes in cardiomyocytes. Two structurally different CB1 receptor antagonists (AM251 with a Ki of 7.5 nM [26]; Fig. 2A and SR141716 with a Ki of 1.8 nM [27]; Fig. 2B) and two CB2 receptor antagonists (AM630 with a Ki of 32.1 nM [26] and SR144528 with Ki of 0.6 nM [27]) were tested. At 300 nM concentration, these antagonists were not able to reverse the inhibitory effect of AEA on the shortenings amplitudes of cardiomyocytes (n = 8–12, ANOVA, P > 0.05).
Brain PET Imaging in the Cannabinoid System
2014, Imaging of the Human Brain in Health and DiseaseProbing the interaction of SR141716A with the CB1 receptor
2012, Journal of Biological ChemistryCitation Excerpt :Because Phe-3797.35 was identified as a residue critical for SR141716A binding in this study (Table 1), all the receptor residues within 20 Å of Phe-3797.35, whose aromatic ring was positioned toward the TM core, were defined as the binding site. This region adequately covered all the reported SR141716A contact residues (6, 14, 15), including Phe-2003.36, Trp-2795.43, and Trp-3566.48, as well as the TM4-EC2-TM5 segment important for SR141716A binding (16, 17). For the GOLD docking experiment, we used the pre-defined default GOLD generic algorithm settings.
Fluorinated cannabinoid CB2 receptor ligands: Synthesis and in vitro binding characteristics of 2-oxoquinoline derivatives
2011, Bioorganic and Medicinal ChemistryCitation Excerpt :Raitio et al. synthesized a new series of CB2 inverse agonists with responses comparable to SR144528,34,35 based on the structure of 2-oxoquinoline JTE-907 (29, Table 2, Supplementary data) in which the piperonylamide end has been replaced with a variety of aromatic amide structures (32–37, Table 2, Supplementary data).34 Several other classes of compounds, including tricyclic pyrazoles,30–32 sulfamoyl benzamides,36 triarylbis-sulfones,37 and arylsulfonamide,38 have been synthesized and reported to be CB2 receptor ligands. However, among all the classes of CB2 ligands, 2-oxoquinoline derivatives appear to be the most efficient inverse agonists, with high binding affinity and selectivity for CB2 receptor.34,35