Tamsulosin (hydrochloride)

Tamsulosin is a potent antagonist of alpha1-adrenergic receptors (alpha1-ARs, Ki = 0.229 nM in a radioligand binding assay). It is 3,800-fold selective for alpha1-ARs over alpha2-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 (Cay-14332), angiotensin II (Cay-17150), or prostaglandin F2alpha (Cay-16010). In vivo, tamsulosin reverses the pressor effect of phenylephrine (Cay-17205, Cay-18619) in pithed rats. It reversibly reduces fertility in male rats when administered at a dose of 0.15 mg/kg. Tamsulosin (1-100 µg/kg) also reduces prostatic pressure in a dose-dependent manner with minimal hypotensive effects in anesthetized dogs. Formulations containing tamsulosin have been used for the treatment of benign prostatic hyperplasia.Formal Name: 5-[(2R)-2-[[2-(2-ethoxyphenoxy)ethyl]amino]propyl]-2-methoxy-benzenesulfonamide, monohydrochloride. CAS Number: 106463-17-6. Synonyms: LY253351, YM-12617-1. Molecular Formula: C20H28N2O5S . HCl. Formula Weight: 445.0. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: 2 mg/ml, DMSO:PBS (pH 7.2)(1:9): 0.10 mg/ml. SMILES: COC1=CC=C(C[C@@H](C)NCCOC2=CC=CC=C2OCC)C=C1S(N)(=O)=O.Cl. InChi Code: InChI=1S/C20H28N2O5S.ClH/c1-4-26-17-7-5-6-8-18(17)27-12-11-22-15(2)13-16-9-10-19(25-3)20(14-16)28(21,23)24,/h5-10,14-15,22H,4,11-13H2,1-3H3,(H2,21,23,24),1H/t15-,/m1./s1. InChi Key: ZZIZZTHXZRDOFM-XFULWGLBSA-N.