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EMD-281014 hydrochloride

Chemical Structure : EMD-281014 hydrochloride

CAS No.: 443144-27-2

EMD-281014 hydrochloride (Pruvanserin;LSN2411347;LY-2422347)

Catalog No.: PC-35384Not For Human Use, Lab Use Only.

EMD-281014 hydrochloride ((Pruvanserin, LSN2411347, LY-2422347)) is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

EMD-281014 hydrochloride ((Pruvanserin, LSN2411347, LY-2422347)) is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels; significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test; reduces dyskinesia and psychosis in the l-DOPA-treated parkinsonian marmoset.

Sleep Disorder

Discontinued

Physicochemical Properties

M.Wt 412.893
Formula C22H22ClFN4O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

7-[[4-[2-(4-Fluorophenyl)ethyl]-1-piperazinyl]carbonyl]-1H-indole-3-carbonitrile hydrochloride

References

1. Hamadjida A, et al. Neuropharmacology. 2018 Jun 30;139:61-67.

2. Lauffer L, et al. J Pharmacol Exp Ther. 2016 Jul;358(1):39-49.

3. Patel JG, et al. Synapse. 2004 Apr;52(1):73-5.

4. Ladduwahetty T, et al. Bioorg Med Chem Lett. 2006 Jun 15;16(12):3201-4.

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