LY-266,097 explained

LY-266,097 is a research ligand which acts as a potent and selective antagonist for the 5-HT2B receptor, with more than 100x selectivity over the related 5-HT2A and 5-HT2C receptor subtypes.[1] However, other sources have stated that LY-266,097 is actually a biased agonist of the receptor, selective for Gq signaling but not β-arrestin2.[2] The drug has been used to study the role of the 5-HT2B receptor in modulating dopamine release in the brain,[3] [4] as well as its involvement in other processes such as allodynia.[5]

Notes and References

  1. Krempaska K, Barnowski S, Gavini J, Hobi N, Ebener S, Simillion C, Stokes A, Schliep R, Knudsen L, Geiser TK, Funke-Chambour M . 6 . Azithromycin has enhanced effects on lung fibroblasts from idiopathic pulmonary fibrosis (IPF) patients compared to controls [corrected] . Respiratory Research . 21 . 1 . 25 . January 2020 . 31941499 . 6964061 . 10.1186/s12931-020-1275-8 . free .
  2. McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RH, Che T, Jin J, Roth BL . Structural determinants of 5-HT2B receptor activation and biased agonism . Nature Structural & Molecular Biology . 25. 9. 787–796 . August 2018 . 30127358 . 6237183 . 10.1038/s41594-018-0116-7 .
  3. Auclair AL, Cathala A, Sarrazin F, Depoortère R, Piazza PV, Newman-Tancredi A, Spampinato U . The central serotonin 2B receptor: a new pharmacological target to modulate the mesoaccumbens dopaminergic pathway activity . Journal of Neurochemistry . 114 . 5 . 1323–1332 . September 2010 . 20534001 . 10.1111/j.1471-4159.2010.06848.x . 45607832 .
  4. Devroye C, Cathala A, Haddjeri N, Rovera R, Vallée M, Drago F, Piazza PV, Spampinato U . 6 . Differential control of dopamine ascending pathways by serotonin2B receptor antagonists: New opportunities for the treatment of schizophrenia . Neuropharmacology . 109 . 59–68 . October 2016 . 27260325 . 10.1016/j.neuropharm.2016.05.024 . 46847094 .
  5. Pineda-Farias JB, Velázquez-Lagunas I, Barragán-Iglesias P, Cervantes-Durán C, Granados-Soto V . 5-HT2B Receptor Antagonists Reduce Nerve Injury-Induced Tactile Allodynia and Expression of 5-HT2B Receptors . Drug Development Research . 76 . 1 . 31–39 . February 2015 . 25620128 . 10.1002/ddr.21238 . 26049138 .

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