Catalog Number: 1742
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
  • M.Wt:
    391.94
  • Formula:
    C22H29NO3.HCl
  • Solubility:
    Soluble to 100 mM in water and to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    167144-80-1
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.
Background References
  1. Pharmacological profiles of R-96544, the active form of a novel 5-HT2A receptor antagonist R-102444.
    Ogawa et al.
    Eur.J.Pharmacol., 2002;457:107
  2. 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
    Ogawa et al.
    Eur.J.Pharmacol., 2005;521:156
  3. [2-(ω-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding.
    Tanaka et al.
    Chem.Pharm.Bull., 2000;48:1729
Citations:

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

3 Citations: Showing 1 - 3
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  1. 5-hydroxytryptamine has an endothelium-derived hyperpolarizing factor-like effect on coronary flow in isolated rat hearts.
    Authors: Chien and Su
    PLoS One 2015;22:42
  2. Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells.
    Authors: Tanaka Et al.
    J Biol Chem 2014;289:10466
  3. Deficits in LTP induction by 5-HT2A receptor antagonist in a mouse model for fragile X syndrome.
    Authors: Xu Et al.
    J Pharmacol Exp Ther 2012;7:e48741

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