A 5-HT2B receptor antagonist
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LY272015

Item No. 31471

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(3,4-dimethoxyphenyl)methyl]-2,3,4,9-tetrahydro-6-methyl-1H-pyrido[3,4-b]indole, monohydrochloride
CAS Number
172895-15-7
Molecular Formula
C21H24N2O2 • HCl
Formula Weight
372.9
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mM
SMILES
COC1=CC(CC2NCCC3=C2NC4=C3C=C(C)C=C4)=CC=C1OC.Cl
InChi Code
InChI=1S/C21H24N2O2.ClH/c1-13-4-6-17-16(10-13)15-8-9-22-18(21(15)23-17)11-14-5-7-19(24-2)20(12-14)25-3;/h4-7,10,12,18,22-23H,8-9,11H2,1-3H3;1H
InChi Key
BKAZOTIBKRWLQA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $190

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    Product Description

    LY272015 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B.1 It binds to 5-HT2B receptors in isolated rat fundus (Kb = 0.177 nM). LY272015 is selective for 5-HT2B receptors over 5-HT2A and 5-HT2C receptors (Kis = 3.54 and 2.1 nM, respectively), as well as α1-adrenergic receptors.1,2 It reduces 5-HT-induced migration of isolated mouse aortic smooth muscle cells when used at a concentration of 100 nM.3 LY272015 (1 and 3 mg/kg) decreases mean arterial pressure in DOCA-salt hypertensive rats.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. 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).

    2. Cohen, M.L., Schenck, K.W., Mabry, T.E., et al. LY272015, a potent selective and orally active 5-HT2B receptor antagonist. J. Med. Chem. 39(14), 2773-2780 (1996).

    3. Liu, Y., Wang, Z., Li, J., et al. Inhibition of 5-hydroxytryptamine receptor 2B reduced vascular restenosis and mitigated the β-arrestin2–mammalian target of rapamycin/p70S6K pathway. J. Am. Heart Assoc. 7(3), e006810 (2017).

    4. Watts, S.W., and Fink, G.D. 5-HT2B-receptor antagonist LY-272015 is antihypertensive in DOCA-salt-hypertensive rats. Am. J. Physiol. 276(3), H944-H952 (1999).