Chemical Name: 5-(4-Chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamide
Biological ActivityHigh affinity and selective CB2 inverse agonist (Ki = 0.6 nM). Exhibits >700-fold selectivity for CB2 over CB1 receptors. Blocks the effects of CP 55,940 (Cat. No. 0949) on forskolin-sensitive adenylyl cyclase activity and MAPK in CHO cells expressing CB2 receptors. Also blocks CP 55,940-induced B-cell activation. Orally bioavailable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.
Rinaldi-Carmona et al.
The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimeth
Kotsikorou et al.
Gi protein modulation induced by a selective inverse agonist for the peripheral cannabinoid receptor CB2: implication for intracellular signalization cross-regulation.
Bouaboula et al.
Citations for SR 144528
The citations listed below are publications that use Tocris products. Selected citations for SR 144528 include:
3 Citations: Showing 1 - 3
Activation of cannabinoid receptor type 2 by JWH133 alleviates bleomycin-induced pulmonary fibrosis in mice.
Δ 9-Tetrahydrocannabinol Reverses TNFα-induced Increase in Airway Epithelial Cell Permeability through CB 2 Receptors
Authors: Shang Et al.
Biochemical Pharmacology 2016;
Preclinical evaluation of SMM-189, a cannabinoid receptor 2-specific inverse agonist.
Authors: Presley Et al.
J Neurosci 2015;3:e00159
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