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Selective α1A adrenoceptor antagonist (Ki = 0.036 nM). Displays >55 fold selectivity for α1A over α1B and α1D. Inhibits norepinephrine-induced [Ca2+]I increase in α1A expressing CHO cells (IC50 = 0.32 nM). Inhibits norepinephrine-induced contraction of isolated human prostate tissue.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 495.53. 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|
|1 mM||2.02 mL||10.09 mL||20.18 mL|
|5 mM||0.4 mL||2.02 mL||4.04 mL|
|10 mM||0.2 mL||1.01 mL||2.02 mL|
|50 mM||0.04 mL||0.2 mL||0.4 mL|
References are publications that support the biological activity of the product.
Shibata et al (1995) KMD-3213, a novel, potent, alpha 1a-adrenoceptor-selective antagonist: characterization using recombinant human alpha 1-adrenoceptors and native tissues. Mol.Pharmacol. 48 250 PMID: 7651358
Moriyama et al (1997) KMD-3213, a novel alpha1A-adrenoceptor antagonist, potently inhibits the functional alpha1-adrenoceptor in human prostate. Eur.J.Pharmacol. 331 39 PMID: 9274928
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Literature in this Area
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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.