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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.
R-96544 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
|Storage||Store at RT|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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|
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
If you know of a relevant reference for R-96544 hydrochloride, please let us know.
Keywords: R-96544 hydrochloride, R-96544 hydrochloride supplier, Potent, selective, 5-HT2A, antagonists, serotonin, receptors, 5-HT2, antagonist, Receptors, 1742, Tocris Bioscience
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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