94666-07-6
Chemical Structure
(Rac)-Tamsulosin
Synonym(s): YM12617 free base; (Rac)-LY253351 free base
- CAS No.: 94666-07-6
- Formula:C20H28N2O5S
- Molecular Weight:408.51
InChIKey: DRHKJLXJIQTDTD-UHFFFAOYSA-N
SMILES: O=S(N)(C1=CC(CC(C)NCCOC2=C(OCC)C=CC=C2)=CC=C1OC)=O
Biological Activity: (Rac)-Tamsulosin (YM12617 (free base); (Rac)-LY253351 (free base)) is an isomer of Tamsulosin (HY-B0661). (Rac)-Tamsulosin is a sulfonamide phenethylamine derivative and a competitive antagonist of selective post-synaptic α1-adrenoceptors. (Rac)-Tamsulosin inhibits CYP3A4 activity in a non-competitive, enantiomer-specific manner, with an IC50 and Ki of 6.75 μM. (Rac)-Tamsulosin produces dose-dependent hypotension, preferentially antagonizing α1-adrenoceptor-mediated pressor responses, and inhibits α2-adrenoceptor-mediated pressor responses at high doses. (Rac)-Tamsulosin can be used in research related to various diseases such as metabolism[1][2][3].
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(Rac)-Tamsulosin | (Rac)-Tamsulosin (YM12617 (free base); (Rac)-LY253351 (free base)) is an isomer of Tamsulosin (HY-B0661). (Rac)-Tamsulosin is a sulfonamide phenethylamine derivative and a competitive antagonist of selective post-synaptic α1-adrenoceptors. (Rac)-Tamsulosin inhibits CYP3A4 activity in a non-competitive, enantiomer-specific manner, with an IC50 and Ki of 6.75 μM. (Rac)-Tamsulosin produces dose-dependent hypotension, preferentially antagonizing α1-adrenoceptor-mediated pressor responses, and inhibits α2-adrenoceptor-mediated pressor responses at high doses. (Rac)-Tamsulosin can be used in research related to various diseases such as metabolism. | |||||||||||||||||||||
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References
- [1]. Novotna A, et al. Profiling of enantiopure drugs towards aryl hydrocarbon (AhR), glucocorticoid (GR) and pregnane X (PXR) receptors in human reporter cell lines. Chemico-biological interactions. 2014 Feb 05;208:64-76. [Content Brief]
- [2]. Krasulova K, et al. Enantiospecific effects of chiral drugs on cytochrome P450 inhibition in vitro. Xenobiotica; the fate of foreign compounds in biological systems. 2016;46(4):315-24. [Content Brief]
- [3]. Honda K, et al. Further studies on (+/-)-YM-12617, a potent and selective alpha 1-adrenoceptor antagonist and its individual optical enantiomers. Naunyn-Schmiedeberg's archives of pharmacology. 1987 Sep;336(3):295-302. [Content Brief]
