Cat. No. 0870
Chemical Name: α-Phenyl-1-(2-phenylethyl)-4-piperid
Biological ActivityOrally active 5-HT2A receptor antagonist; displays selectivity for 5-HT2A receptors over 5-HT2C receptors (Ki values are 0.54, 2.5, 81.6 and ~10,000 nM at rabbit 5-HT2A, human 5-HT2A, rabbit 5-HT2C and human 5-HT2C receptors respectively).
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Jensen et al (2013) Design, synthesis, and pharmacological characterization of N- and O-substituted 5,6,7,8-tetrahydro-4H-isoxazolo[4,5-dazepin-3-ol analogues: novel 5-HT2A/5-HT2C receptor agonists with pro-cognitive properties. J.Med.Chem. 56 1211. PMID: 23301527.
Aloyo and Harvey (2000) Antagonist binding at 5-HT2A and 5-HT2C receptors in the rabbit: high correlation with the profile for the human receptors. Eur.J.Pharmacol. 406 163. PMID: 11020478.
Dudley et al (1988) Pharmacological effects of MDL 11,939: a selective, centrally acting antagonist of 5-HT2 receptors. Drug Dev.Res. 13 29.
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Citations are publications that use Tocris products. Selected citations for MDL 11,939 include:
Corcoran et al (2014) Dual effects of 5-HT(1a) receptor activation on breathing in neonatal mice. J Neurosci 34 51. PMID: 24381267.
Goda et al (2013) Serotonergic hallucinogens differentially modify gamma and high frequency oscillations in the rat nucleus accumbens. Psychopharmacology (Berl) 228 271. PMID: 23525524.
Williams et al (2012) Reduced levels of serotonin 2A receptors underlie resistance of Egr3-deficient mice to locomotor suppression by clozapine. Neuropsychopharmacology 37 2285. PMID: 22692564.
Halberstadt and Geyer (2010) LSD but not lisuride disrupts prepulse inhibition in rats by activating the 5-HT(2A) receptor. Psychopharmacology (Berl) 208 179. PMID: 19937319.
Ptak et al (2009) Raphé neurons stimulate respiratory circuit activity by multiple mechanisms via endogenously released serotonin and substance P. Biomol Ther (Seoul) 29 3720. PMID: 19321769.
Yu and Yamaguchi (2009) 5-HT2C-like receptors in the brain of Xenopus laevis initiate sex-typical fictive vocalizations. J Neurophysiol 102 752. PMID: 19474172.
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Keywords: MDL 11,939, supplier, 5-HT2A, antagonist, Serotonin, Receptors, MDL11939, Tocris Bioscience, 5-HT2A Receptor Antagonist products