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(Redirected from LY-266,097)
Chemical compound
Pharmaceutical compound
LY-266097
Clinical data
Other namesLY266097; LY-266,097
Legal status
Legal status
  • In general: uncontrolled
Identifiers
  • 1-[(2-chloro-3,4-dimethoxyphenyl)methyl]-6-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC21H23ClN2O2
Molar mass370.88 g·mol−1
3D model (JSmol)
  • CC1=CC2=C(C=C1)NC3=C2CCNC3CC4=C(C(=C(C=C4)OC)OC)Cl
  • InChI=1S/C21H23ClN2O2/c1-12-4-6-16-15(10-12)14-8-9-23-17(20(14)24-16)11-13-5-7-18(25-2)21(26-3)19(13)22/h4-7,10,17,23-24H,8-9,11H2,1-3H3
  • Key:NJLHHCITDFZZSE-UHFFFAOYSA-N

LY-266097 is a synthetic β-carboline 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-266097 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]

See also

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References

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  1. ↑ Krempaska K, Barnowski S, Gavini J, Hobi N, Ebener S, Simillion C, et al. (January 2020). "Azithromycin has enhanced effects on lung fibroblasts from idiopathic pulmonary fibrosis (IPF) patients compared to controls [corrected]". Respiratory Research. 21 (1): 25. doi:10.1186/s12931-020-1275-8. PMC 6964061. PMID 31941499.
  2. ↑ McCorvy JD, Wacker D, Wang S, Agegnehu B, Liu J, Lansu K, Tribo AR, Olsen RH, Che T, Jin J, Roth BL (August 2018). "Structural determinants of 5-HT2B receptor activation and biased agonism". Nature Structural & Molecular Biology. 25 (9): 787–796. doi:10.1038/s41594-018-0116-7. PMC 6237183. PMID 30127358.
  3. ↑ Auclair AL, Cathala A, Sarrazin F, Depoortère R, Piazza PV, Newman-Tancredi A, Spampinato U (September 2010). "The central serotonin 2B receptor: a new pharmacological target to modulate the mesoaccumbens dopaminergic pathway activity". Journal of Neurochemistry. 114 (5): 1323–1332. doi:10.1111/j.1471-4159.2010.06848.x. PMID 20534001. S2CID 45607832.
  4. ↑
  5. ↑ Pineda-Farias JB, Velázquez-Lagunas I, Barragán-Iglesias P, Cervantes-Durán C, Granados-Soto V (February 2015). "5-HT2B Receptor Antagonists Reduce Nerve Injury-Induced Tactile Allodynia and Expression of 5-HT2B Receptors". Drug Development Research. 76 (1): 31–39. doi:10.1002/ddr.21238. PMID 25620128. S2CID 26049138.
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