R-96544 hydrochloride

Cat. No. 1742

R-96544 hydrochloride C22H29NO3.HCl [167144-80-1]

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

Biological Activity

Potent, selective 5-HT2 receptor antagonist; displays some selectivity for 5-HT2A receptors (Ki = 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

Soluble to 100 mM in water and to 100 mM in DMSO
>99 %
Store at RT

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Ogawa et al (2005) 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 experimental pancreatitis. Eur.J.Pharmacol. 521 156. PMID: 16183055.

Ogawa et al (2002) Pharmacological profiles of R-96544, the active form of a novel 5-HT2A receptor antagonist R-102444. Eur.J.Pharmacol. 457 107. PMID: 12464356.

Tanaka et al (2000) [2-(ω-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding. Chem.Pharm.Bull. 48 1729. PMID: 11086903.

If you know of a relevant reference for R-96544 hydrochloride please let us know.

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

Chien and Su (2015) 5-hydroxytryptamine has an endothelium-derived hyperpolarizing factor-like effect on coronary flow in isolated rat hearts. PLoS One 22 42. PMID: 26076928.

Tanaka et al (2014) Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells. J Biol Chem 289 10466. PMID: 24570000.

Xu et al (2012) Deficits in LTP induction by 5-HT2A receptor antagonist in a mouse model for fragile X syndrome. J Pharmacol Exp Ther 7 e48741. PMID: 23119095.

Do you know of a great paper that uses R-96544 hydrochloride from Tocris? If so please let us know.

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Keywords: R-96544 hydrochloride, supplier, Potent, selective, 5-HT2A, antagonists, serotonin, receptors, 5-HT2, antagonist, Tocris Bioscience, 5-HT2A Receptor Antagonist products

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