LY-266,097

LY-266,097
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	208591-60-0 ;
PubChem CID	9953185;
ChemSpider	8128795;
UNII	2Z9TC7YMY4;
ChEMBL	ChEMBL95121;
Chemical and physical data
Formula	C21H23ClN2O2
Molar mass	370.88 g·mol−1
3D model (JSmol)	Interactive image;
	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-HT_2B receptor, with more than 100x selectivity over the related 5-HT_2A and 5-HT_2C receptor subtypes.^[1] It has been used to study the role of the 5-HT_2B receptor in modulating dopamine release in the brain,^[2]^[3] as well as its involvement in other processes such as allodynia.^[4]

References

^ 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.
^ 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.
^ Devroye C, Cathala A, Haddjeri N, Rovera R, Vallée M, Drago F, et al. (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.
^ Pineda-Farias JB, Velázquez-Lagunas I, Barragán-Iglesias P, Cervantes-Durán C, Granados-Soto V (February 2015). "5-HT_2B Receptor Antagonists Reduce Nerve Injury-Induced Tactile Allodynia and Expression of 5-HT_2B Receptors". Drug Development Research. 76 (1): 31–39. doi:10.1002/ddr.21238. PMID 25620128. S2CID 26049138.

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[pmid31941499-1] 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.

[pmid20534001-2] 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): 1323–1332. doi:10.1111/j.1471-4159.2010.06848.x. PMID 20534001. S2CID 45607832.

[pmid27260325-3] Devroye C, Cathala A, Haddjeri N, Rovera R, Vallée M, Drago F, et al. (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.

[pmid25620128-4] Pineda-Farias JB, Velázquez-Lagunas I, Barragán-Iglesias P, Cervantes-Durán C, Granados-Soto V (February 2015). "5-HT_2B Receptor Antagonists Reduce Nerve Injury-Induced Tactile Allodynia and Expression of 5-HT_2B Receptors". Drug Development Research. 76 (1): 31–39. doi:10.1002/ddr.21238. PMID 25620128. S2CID 26049138.

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