R-96544 hydrochloride

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Cat.No. 1742 - R-96544 hydrochloride | C22H29NO3.HCl | CAS No. 167144-80-1
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% (HPLC)
Datasheet
Citations (3)
Literature

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.

Compound Libraries

R-96544 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 391.94
Formula C22H29NO3.HCl
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 167144-80-1
PubChem ID 10668210
InChI Key OUKRSTJUAQEATQ-GZJHNZOKSA-N
Smiles Cl[H].COC1=CC=CC(CCC2=C(OCC[C@@H]3C[C@@H](O)CN3C)C=CC=C2)=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.19 100
water 39.19 100

Preparing Stock Solutions

The following data is based on the product molecular weight 391.94. Batch specific molecular weights may vary from batch to batch due to solvent 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 2.55 mL 12.76 mL 25.51 mL
5 mM 0.51 mL 2.55 mL 5.1 mL
10 mM 0.26 mL 1.28 mL 2.55 mL
50 mM 0.05 mL 0.26 mL 0.51 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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 expe Eur.J.Pharmacol. 521 156 PMID: 16183055


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

3 Citations for R-96544 hydrochloride

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

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

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


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