Chemical Name: (2R,4R)-5-[2-[2-[2-(3-Methoxyphenyl)ethyl]phenoxy]ethyl]-1-methyl-3-pyrrolidinol hydrochloride
Biological ActivityR-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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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[2-(ω-Phenylalkyl)phenoxy]alkylamines III: Synthesis and selective serotonin-2 receptor binding.
Tanaka et al.
Pharmacological profiles of R-96544, the active form of a novel 5-HT2A receptor antagonist R-102444.
Ogawa et al.
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.
Citations for R-96544 hydrochloride
The citations listed below are publications that use Tocris products. Selected citations for R-96544 hydrochloride include:
3 Citations: Showing 1 - 3
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
Neuroendocrine signaling via the serotonin transporter regulates clearance of apoptotic cells.
Authors: Tanaka Et al.
J Biol Chem 2014;289:10466
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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