R-96544 hydrochloride

Catalog #: 1742
3 Citations Datasheet / COA / SDS

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R-96544 hydrochloride | CAS No. 167144-80-1 | 5-HT2A Receptor Antagonists

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Description: Potent, selective 5-HT2A antagonist

Chemical Name: (2R,4R)-5-[2-[2-[2-(3-Methoxyphenyl)ethyl]phenoxy]ethyl]-1-methyl-3-pyrrolidinol hydrochloride

Purity: ≥99%

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Product Details

Citations (3)

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Biological Activity

R-96544 hydrochloride is a potent, selective 5-HT₂ receptor antagonist; displays some selectivity for 5-HT_2A receptors (K_i = 1.6 nM). IC₅₀ values are 2.2, 310, 2400, 3700, > 5000 and > 5000 nM for 5-HT₂, α₁-adrenergic, D₂ dopamine, 5-HT₁, 5-HT₃ and β-adrenergic receptors respectively. Inhibits 5-HT-induced platelet aggregation and pressor responses in vivo.

Technical Data

M.Wt:

391.94

Formula:

C₂₂H₂₉NO₃.HCl

Solubility:

Soluble to 100 mM in water and to 100 mM in DMSO

Purity:

≥99%

Storage:

Store at RT

CAS No:

167144-80-1

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.

Background References

[2-(ω-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding.
Tanaka et al.
Chem.Pharm.Bull., 2000;48:1729
Pharmacological profiles of R-96544, the active form of a novel 5-HT_2A receptor antagonist R-102444.
Ogawa et al.
Eur.J.Pharmacol., 2002;457:107
Effects of R-102444 and its active metabolite R-96544, selective 5-HT2A receptor antagonists, on experimental acute and chronic pancreatitis: additional evidence for possible involvement of 5-HT2A receptors in the development of expe
Ogawa et al.
Eur.J.Pharmacol., 2005;521:156

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Citations for R-96544 hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for R-96544 hydrochloride include:

3 Citations: Showing 1 - 3

5-hydroxytryptamine has an endothelium-derived hyperpolarizing factor-like effect on coronary flow in isolated rat hearts.
Authors: Chien and Su
PLoS One 2015;22:42
Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells.
Authors: Tanaka Et al.
J Biol Chem 2014;289:10466
Deficits in LTP induction by 5-HT2A receptor antagonist in a mouse model for fragile X syndrome.
Authors: Xu Et al.
J Pharmacol Exp Ther 2012;7:e48741

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