LY-266,097

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LY-266,097
LY-266097 structure.png
Legal status
Legal status
  • In general: uncontrolled
Identifiers
IUPAC name
  • 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)
SMILES
  • CC1=CC2=C(C=C1)NC3=C2CCNC3CC4=C(C(=C(C=C4)OC)OC)Cl
InChI
  • 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-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] It has been used to study the role of the 5-HT2B receptor in modulating dopamine release in the brain,[2][3] as well as its involvement in other processes such as allodynia.[4]

References[]

  1. ^ McCorvy JD, Wacker D, Wang S, et al. Structural determinants of 5-HT2B receptor activation and biased agonism. Nat Struct Mol Biol. 2018;25(9):787-796. doi:10.1038/s41594-018-0116-7
  2. ^ 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): 1323–32. doi:10.1111/j.1471-4159.2010.06848.x. PMID 20534001. S2CID 45607832.
  3. ^ Devroye C, Cathala A, Haddjeri N, Rovera R, Vallée M, Drago F, Piazza PV, Spampinato U (October 2016). "Differential control of dopamine ascending pathways by serotonin2B receptor antagonists: New opportunities for the treatment of schizophrenia". Neuropharmacology. 109: 59–68. doi:10.1016/j.neuropharm.2016.05.024. PMID 27260325. S2CID 46847094.
  4. ^ 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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