RS 127445 hydrochloride
High affinity 5-HT2B receptor antagonist (pKi = 9.5). Displays 1000-fold selectivity for 5-HT2B with good bioavailability.
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 317.79. 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||3.15 mL||15.73 mL||31.47 mL|
|5 mM||0.63 mL||3.15 mL||6.29 mL|
|10 mM||0.31 mL||1.57 mL||3.15 mL|
|50 mM||0.06 mL||0.31 mL||0.63 mL|
References are publications that support the products' biological activity.
Bonhaus et al (1999) RS-127445: a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist. Br.J.Pharmacol. 127 1075 PMID: 10455251
Callebert et al (2006) Evidence for a control of plasma serotonin levels by 5-Hydroxytryptamine2B receptors in mice. J.Pharmacol.Exp.Ther. 317 724 PMID: 16461587
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3 Citations for RS 127445 hydrochloride
Citations are publications that use Tocris products. Selected citations for RS 127445 hydrochloride include:
Söhle et al (2012) Identification of new genes involved in human adipogenesis and fat storage. PLoS One 7 e31193 PMID: 22384002
Tanaka et al (2014) Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells. J Biol Chem 289 10466 PMID: 24570000
Chabbi-Achengli et al (2013) Serotonin 2B receptor (5-HT2B R) signals through prostacyclin and PPAR-β/δ in osteoblasts. PLoS One 8 e75783 PMID: 24069449
Do you know of a great paper that uses RS 127445 hydrochloride from Tocris? If so please let us know.
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Literature in this Area
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.
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.