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Biological Activity for MDL 11,939
MDL 11,939 is an orally 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).
Technical Data for MDL 11,939
|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.
Solubility Data for MDL 11,939
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for MDL 11,939
The following data is based on the product molecular weight 295.42. 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|
|0.5 mM||6.77 mL||33.85 mL||67.7 mL|
|2.5 mM||1.35 mL||6.77 mL||13.54 mL|
|5 mM||0.68 mL||3.39 mL||6.77 mL|
|25 mM||0.14 mL||0.68 mL||1.35 mL|
References for MDL 11,939
References are publications that support the biological activity of the product.
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
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 J.Med.Chem. 56 1211 PMID: 23301527
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Keywords: MDL 11,939, MDL 11,939 supplier, 5-HT2A, antagonist, Serotonin, Receptors, MDL11939, 0870, Tocris Bioscience
7 Citations for MDL 11,939
Citations are publications that use Tocris products. Selected citations for MDL 11,939 include:
Williams et al (2012) Reduced levels of serotonin 2A receptors underlie resistance of Egr3-deficient mice to locomotor suppression by cloz. 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
Hodges et al (2009) Transgenic mice lacking serotonin neurons have severe apnea and high mortality during development. J Neurosci 29 10341 PMID: 19692608
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
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
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
Do you know of a great paper that uses MDL 11,939 from Tocris? Please let us know.
Reviews for MDL 11,939
Average Rating: 5 (Based on 1 Review.)
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We used MDL for in vivo infusion at different regions of the brain. It works very well. It is very stable and easy to dissolve and not sticky which make it easy to infuse.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.
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