LY 266097 hydrochloride

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Cat.No. 4081 - LY 266097 hydrochloride | C21H23ClN2O2.HCl | CAS No. 172895-39-5
Description: Selective 5-HT2B antagonist
Chemical Name: 1-[(2-Chloro-3,4-dimethoxyphenyl)methyl]-2,3,4,9-tetrahydro-6-methyl-1H-pyrido[3,4-b]indole hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (3)

Biological Activity

Selective 5-HT2B receptor antagonist (pKi = 9.3). More than 100-fold selective over 5-HT2A and 5-HT2C. Attenuates amphetamine-induced locomotion in the rat.

Compound Libraries

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Technical Data

M. Wt 407.33
Formula C21H23ClN2O2.HCl
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 172895-39-5
PubChem ID 9953184
InChI Key KPXKZZURYAXZQE-UHFFFAOYSA-N
Smiles CC1=CC=C(NC3=C2CCNC3CC4=CC=C(OC)C(OC)=C4Cl)C2=C1.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 40.73 100
ethanol 40.73 100

Preparing Stock Solutions

The following data is based on the product molecular weight 407.33. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.46 mL 12.28 mL 24.55 mL
5 mM 0.49 mL 2.46 mL 4.91 mL
10 mM 0.25 mL 1.23 mL 2.46 mL
50 mM 0.05 mL 0.25 mL 0.49 mL

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References

References are publications that support the biological activity of the product.

Audia et al (1996) Potent, selective tetrahydro-β-carboline antagonists of the serotonin 2B (5-HT2B) contractile receptor in the rat stomach fundus. J.Med.Chem. 39 2773 PMID: 8709108

Auclair et al (2010) The central serotonin2B receptor: a new pharmacological target to modulate the mesoaccumbens DArgic pathway activity. J.Neurochem. 114 1323 PMID: 20534001


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1 Citation for LY 266097 hydrochloride

Citations are publications that use Tocris products. Selected citations for LY 266097 hydrochloride include:

McCorvy et al (2018) Structural determinants of 5-HT2B receptor activation and biased agonism. Nat Struct Mol Biol 25 787 PMID: 30127358


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Literature in this Area

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5-HT Receptors Scientific Review

Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.

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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.