Chemistry:WOBE437
WOBE437 is a selective endocannabinoid reuptake inhibitor (eCBRI or SERI) which has been used in scientific research.[1][2] It is a highly potent and selective eCBRI, with an IC50 of 10 nM in terms of this action.[1][2][3] The drug produces anxiolytic-like, anti-inflammatory, analgesic, antiallodynic, and muscle relaxant effects in rodents.[1][2][4] These effects are mediated by increased endocannabinoid levels, including of anandamide (AEA) and 2-arachidonylglycerol (2-AG), and are dependent on cannabinoid receptors, for instance the cannabinoid CB1 receptor.[1][2] Conversely, WOBE437 did not produce catalepsy, affect locomotor activity, or produce the typical sedation of cannabinoid CB1 receptor agonists.[2][4] The drug also showed effectiveness in an animal model of multiple sclerosis.[4] Originally believed to be selective, off-target activities of WOBE437 have subsequently been identified and described.[5] WOBE437 is orally bioavailable in rodents.[2] Numerous analogues of WOBE437 have been explored in search of candidates with better drug-like properties, though a series of almost 80 compounds found none that were more potent than WOBE437 itself.[3] WOBE437 was first described in the scientific literature by 2013.[6][1]
See also
References
- ↑ 1.0 1.1 1.2 1.3 1.4 "Chemical probes to potently and selectively inhibit endocannabinoid cellular reuptake". Proceedings of the National Academy of Sciences of the United States of America 114 (25): E5006–E5015. June 2017. doi:10.1073/pnas.1704065114. PMID 28584105. Bibcode: 2017PNAS..114E5006C.
- ↑ 2.0 2.1 2.2 2.3 2.4 2.5 "The Endocannabinoid Reuptake Inhibitor WOBE437 Is Orally Bioavailable and Exerts Indirect Polypharmacological Effects via Different Endocannabinoid Receptors". Frontiers in Molecular Neuroscience 11. 2018. doi:10.3389/fnmol.2018.00180. PMID 29910713.
- ↑ 3.0 3.1 "Synthesis and Biological Evaluation of Endocannabinoid Uptake Inhibitors Derived from WOBE437". ChemMedChem 16 (1): 145–154. January 2021. doi:10.1002/cmdc.202000153. PMID 32369259.
- ↑ 4.0 4.1 4.2 "Selective Endocannabinoid Reuptake Inhibitor WOBE437 Reduces Disease Progression in a Mouse Model of Multiple Sclerosis". ACS Pharmacology & Translational Science 4 (2): 765–779. April 2021. doi:10.1021/acsptsci.0c00214. PMID 33860200.
- ↑ "Chemical Proteomics Reveals Off-Targets of the Anandamide Reuptake Inhibitor WOBE437". ACS Chemical Biology 17 (5): 1174–1183. May 2022. doi:10.1021/acschembio.2c00122. PMID 35482948.
- ↑ "Prototype of a novel class of potent, selective endocannabinoid reuptake inhibitors". 6th European Workshop on Cannabinoid Research. Dublin, Ireland: Trinity College Dublin. 18 April 2013. https://www.researchgate.net/publication/271270897. Retrieved 27 May 2026.
 |  |
