A potent α1-AR antagonist (Ki = 0.229 nM in a radioligand binding assay); 3

Tamsulosin (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
106463-17-6
Storage:
-20
UN-No:
Non-Hazardous - /

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 for the treatment of benign prostatic hyperplasia.  

 

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Description

A potent α1-AR antagonist (Ki = 0.229 nM in a radioligand binding assay); 3,800-fold selective for α1-ARs over α2-ARs (Ki = 871 nM); antagonizes norepinephrine-induced contraction of isolated rabbit aorta (pA2 = 10.11) but has no effect on contraction stimulated by histamine, serotonin, angiotensin II, or prostaglandin F2α; reverses the phenylephrine-induced pressor effect in pithed rats; reversibly reduces fertility in male rats when administered at a dose of 0.15 mg/kg; reduces prostatic pressure in a dose-dependent manner with minimal hypotensive effects in anesthetized dogs,

Formal name: 5-[(2R)-2-[[2-(2-ethoxyphenoxy)ethyl]amino]propyl]-2-methoxy-benzenesulfonamide, monohydrochloride

Synonyms:  LY253351|YM-12617-1

Molecular weight: 445

CAS: 106463-17-6

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Endocrinology & Metabolism|Reproductive Biology

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