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Submit ReviewR-96544 hydrochloride
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)
Biological Activity for R-96544 hydrochloride
R-96544 hydrochloride is a 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 for R-96544 hydrochloride
R-96544 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for R-96544 hydrochloride
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for R-96544 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 39.19 | 100 | |
| DMSO | 39.19 | 100 |
Preparing Stock Solutions for R-96544 hydrochloride
The following data is based on the product molecular weight 391.94. 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 | 2.55 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 for R-96544 hydrochloride
References for R-96544 hydrochloride
References are publications that support the biological activity of the product.
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, R-96544 hydrochloride supplier, Potent, selective, 5-HT2A, antagonists, serotonin, receptors, 5-HT2, antagonist, Receptors, 1742, 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
Tanaka et al (2014) Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells. J Biol Chem 289 10466 PMID: 24570000
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
Do you know of a great paper that uses R-96544 hydrochloride from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.
Depression Poster
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.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.