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Subtype-selective α1A-adrenoceptor antagonist that displays > 600-fold selectivity over other adrenoceptors (Kivalues are 0.35, 220, 370, 540, 800 and 1200 nM for α1A, α1B, α2C, α1D, α2B and α2A subtypes respectively and 540 nM for L-type Ca2+ channels). Inhibits noradrenalin-induced contractions in rabbit vascular and lower urinary tissues.
|Storage||Store at +4°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 645.19. 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||1.55 mL||7.75 mL||15.5 mL|
|5 mM||0.31 mL||1.55 mL||3.1 mL|
|10 mM||0.15 mL||0.77 mL||1.55 mL|
|50 mM||0.03 mL||0.15 mL||0.31 mL|
References are publications that support the biological activity of the product.
Wetzel et al (1995) Discovery of α1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine. J.Med.Chem. 38 1579 PMID: 7752182
Leonardi et al (1997) Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15-2739 (SB 216469): role of the alpha-1L adrenoceptor in tissue selectivity, Part I. J.Pharmacol.Exp.Ther. 281 1272 PMID: 9190863
Kava et al (1998) α1L-adrenceptor mediation of smooth muscle contraction in rabbit bladder neck: a model for lower urinary tract tissues of man. Br.J.Pharmacol. 123 1359 PMID: 9579731
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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.