Doxazosin mesylate
Chemical Name: 4-Amino-2-[4-(1,4-benzodioxan-2-carbonyl)piperazin-1-yl]-6,7-dimethoxyquinazoline methanesulfonate
Purity: ≥99%
Biological Activity
Doxazosin mesylate is a selective α1-adrenoceptor antagonist (pKi values are 9.0, 8.5 and 8.4 for human α1B, α1A and α1D receptors respectively). Displays antihypertensive activity.Scientific Data
Reduced viability of differentiated cardiomyocytes exposed to cardiotoxic small molecules. The viability of differentiated cardiomyocytes was assessed using a Resazurin metabolism assay. A) Untreated cells metabolize Resazurin (Catalog # AR002) to produce resorufin, a fluorescent molecule that can be measured using a fluorometric plate reader. Resorufin fluorescence accumulated in untreated cardiomyocytes. Cells treated with the cardiotoxic small molecules Staurosporine (blue; Catalog # 1285), a non-selective protein kinase inhibitor, or Doxazosin (tan; Catalog # 2964), an alpha 1 antagonist, did not metabolize Resazurin, as shown by lack of fluorescence accumulation, indicating a loss of viability upon treatment. B) Cell morphology of untreated, Staurosporine-treated, and Doxazosin-treated cardiomyocytes was assessed by brightfield microscopy.
Technical Data
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.
Background References
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The α1-adrenoceptor antagonist profile of doxazosin: preclinical pharmacology.
Alabaster and Davey
Br.J.Clin.Pharmacol., 1986;21:9S -
Evaluation of the pharmacological selectivity profile of α1 adrenoceptor antagonists at prostatic α1 adrenoceptors: binding functional and in vivo studies.
Kenny et al.
Br.J.Pharmacol., 1996;118:871
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Citations for Doxazosin mesylate
The citations listed below are publications that use Tocris products. Selected citations for Doxazosin mesylate include:
4 Citations: Showing 1 - 4
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The anti-hypertensive drug pra. inhibits glioblastoma growth via the PKCδ-dependent inhibition of the AKT pathway.
Authors: Kahn Et al.
EMBO Mol Med 2016;8:511
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Moderate Alcohol Exposure during the Rat Equivalent to the Third Trimester of Human Pregnancy Alters Regulation of GABAA Receptor-Mediated Synaptic Transmission by DA in the Basolateral Amygdala.
Authors: Diaz Et al.
Front Cell Neurosci 2014;2:46
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DArgic modulation of GABAergic transmission in the entorhinal cortex: concerted roles of α1 adrenoreceptors, inward rectifier K+, and T-type Ca2+ channels.
Authors: Cilz Et al.
Cereb Cortex 2014;24:3195
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A drug repositioning approach identifies tricyclic antidepressants as inhibitors of small cell lung cancer and other neuroendocrine tumors.
Authors: Jahchan Et al.
Cancer Discov 2013;3:1364
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