Formulation: A solid
Formal Name: 5-[(2R)-2-[[2-(2-ethoxyphenoxy)ethyl-1,1,2,2-d4]amino]propyl]-2-methoxy-benzenesulfonamide, monohydrochloride
Purity: ≥99% deuterated forms (d1-d4)
Formula Markup: C20H24D4N2O5S • HCl
Formula Weight: 449
Shelf life (days): 1460
CAS Number: 1231943-97-7
Notes: Tamsulosin-d4 is intended for use as an internal standard for the quantification of tamsulosin (Item No. 24020) by GC- or LC-MS. Tamsulosin is a potent antagonist of α1-adrenergic receptors (α1-ARs; Ki = 0.229 nM in a radioligand binding assay).{36342} It is 3,800-fold selective for α1-ARs over α2-ARs (Ki = 871 nM). Tamsulosin antagonizes norepinephrine-induced contraction of isolated rabbit aorta (pA2 = 10.11) but has no effect on contraction stimulated by histamine, serotonin (Item No. 14332), angiotensin II (Item No. 17150), or prostaglandin F2α (Item No. 16010). In vivo, tamsulosin reverses the pressor effect of phenylephrine (Item Nos. 17205 / 18619) in pithed rats. It reversibly reduces fertility in male rats when administered at a dose of 0.15 mg/kg.{36343} Tamsulosin (1-100 μg/kg) also reduces prostatic pressure in a dose-dependent manner with minimal hypotensive effects in anesthetized dogs.{36344} Formulations containing tamsulosin have been used in the treatment of benign prostatic hyperplasia.
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