Tamsolusin hydrochloride

Tamsolusin (10^-10 M-100 μM; 24 h) hydrochloride exhibits no cytotoxicity against AZ-AhR, AZ-GR or LS174T cell lines even at concentrations as high as 100 μM; it shows only weak AhR inhibitory activity in AZ-AhR cells at the concentration of 100 μM^[1].
Tamsolusin (10^-10 M-100 μM; 24 h) hydrochloride acts as a weak agonist of PXR in transiently transfected LS174T cells, exerting significant activation at a concentration of 100 μM, but it is not a potent PXR antagonist^[1].
Tamsolusin hydrochloride acts as a noncompetitive inhibitor of CYP3A4-mediated testosterone 6β-hydroxylation in human liver microsomes, with a K_i value of 6.75 μM; its potency is weaker than that of the R-enantiomer but stronger than that of the S-enantiomer^[2].
Tamsolusin hydrochloride weakly inhibits CYP3A4-mediated midazolam 10-hydroxylation in human liver microsomes, with an IC₅₀ greater than 100 μM^[2].
Tamsolusin hydrochloride binds to α₁-adrenergic receptors labeled with ³H-prazosin in rat brain cell membranes, with a pK_i value of 9.78, and shows 8100-fold higher selectivity for α₁-adrenergic receptors over α₂-adrenergic receptors. It also binds to labeled α₂-adrenergic receptors, with a pK_i value of 5.87^[3].
Tamsolusin ((±)-YM-12617) hydrochloride acts as a competitive antagonist of Phenylephrine (HY-B0769)-induced contraction mediated by post-junctional α₁-adrenergic receptors in isolated rabbit thoracic aorta, with a pA₂ value of 9.88. It shows 8300-fold higher selectivity for α₁-adrenergic receptors over α₂-adrenergic receptors. It also functions as a competitive antagonist of UK-14304 (HY-B0659)-induced pre-synaptic α₂-adrenergic receptors in electrically stimulated longitudinal muscle of guinea pig ileum, with a pA₂ value of 5.96^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.