A 5-HT2B receptor antagonist
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LY266097 (hydrochloride)

Item No. 11935

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(2-chloro-3,4-dimethoxyphenyl)methyl]-2,3,4,9-tetrahydro-6-methyl-1H-pyrido[3,4-b]indole, monohydrochloride
CAS Number
172895-39-5
Molecular Formula
C21H23ClN2O2 • HCl
Formula Weight
407.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Chloroform: 30mg/mL
λmax
211, 228, 231, 242, 275 nm
SMILES
ClC1=C(OC)C(OC)=CC=C1CC(NCC2)C3=C2C4=CC(C)=CC=C4N3.Cl
InChi Code
InChI=1S/C21H23ClN2O2.ClH/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;1H
InChi Key
KPXKZZURYAXZQE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    500 µg

    $36

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    1 mg

    $55

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    5 mg

    $153

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    10 mg

    $236

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    Product Description

    LY266097 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B (Ki = 0.5 nM).1 It is selective for 5-HT2B over 5-HT2A and 5-HT2C receptors (Kis = 19.5 and 24.55 nM, respectively).2 LY266097 (100 nmol, intrathecal) reduces hind paw tactile allodynia induced by L5/L6 spinal nerve ligation in a rat model of neuropathic pain.3 It also reduces hyperlocomotion induced by cocaine in rats when administered at a dose of 0.63 mg/kg without reducing cocaine-induced dopamine outflow in the nucleus accumbens shell.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Auclair, A.L., Cathala, A., Sarrazin, F., et al. The central serotonin2B receptor: A new pharmacological target to modulate the mesoaccumbens dopaminergic pathway activity. J. Neurochem. 115(5), 1323-1332 (2010).

    2. Audia, J.E., Evrard, D.A., Murdoch, G.R., et al. Potent, selective tetrahydro-β-carboline antagonists of the serotonin 2B (5HT2B) contractile receptor in the rat stomach fundus. J. Med. Chem. 39(14), 2773-2780 (1996).

    3. Pineda-Farias, J.B., Velázquez-Lagunas, I., Barragán-Iglesias, P., et al. 5-HT2B receptor antagonists reduce nerve injury-induced tactile allodynia and expression of 5-HT2B receptors. Drug Dev. Res. 76(1), 31-39 (2015).

    4. Devroye, C., Cathala, A., Di Marco, B., et al. Central serotonin2B receptor blockade inhibits cocaine-induced hyperlocomotion independently of changes of subcortical dopamine outflow. Neuropharmacology 97, 329-337 (2015).