5-Methoxy-2-aminotetraline hydrochloride - CAS 3880-88-4
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
Dopamine Receptor
5-Methoxy-2-Aminotetraline hydrochloride is a dopamine receptor agonist.
Brife Description:
dopamine receptor agonist
2-amino-5-methoxytetralin HCl; 2-amino-5-methoxytetralin Hydrochloride; Aminotetraline hydrochloride, 5-Methoxy-2-; AK209995; 5-Methoxy-1,2,3,4-tetrahydro-naphthalen-2-yl amine HCl
Canonical SMILES:
1.Effect of cyclosporine and rifampin on the pharmacokinetics of macitentan, a tissue-targeting dual endothelin receptor antagonist.
Bruderer S;Aänismaa P;Homery MC;Häusler S;Landskroner K;Sidharta PN;Treiber A;Dingemanse J AAPS J. 2012 Mar;14(1):68-78. doi: 10.1208/s12248-011-9316-3. Epub 2011 Dec 22.
Macitentan is a dual endothelin receptor antagonist under phase 3 investigation in pulmonary arterial hypertension. We investigated the effect of cyclosporine (Cs) and rifampin on the pharmacokinetics of macitentan and its metabolites ACT-132577 and ACT-373898 in healthy male subjects. In addition, in vitro studies were performed to investigate interactions between macitentan and its active metabolite ACT-132577 with human organic anion-transporting polypeptides (OATPs). The clinical study (AC-055-111) was conducted as a two-part, one-sequence, crossover study. Ten subjects in each part received multiple-dose macitentan followed by multiple-dose co-administration of Cs (part A) or rifampin (part B). In the presence of Cs, steady-state area under the plasma concentration-time profiles during a dose interval (AUC(τ)) for macitentan and ACT-373898 increased 10% and 7%, respectively, and decreased 3% for ACT-132577. Steady-state AUC(τ) of macitentan and ACT-373898 in the presence of rifampin decreased 79% and 64%, respectively. For ACT-132577, no relevant difference in AUC(τ) between the two treatments was observed. Macitentan co-administered with Cs or rifampin was well tolerated. The complementary in vitro studies demonstrated no marked differences in uptake rates of macitentan and ACT-132577 between the wild-type and OATP over-expressing cells over the concentration range tested.
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CAS 3880-88-4 5-Methoxy-2-aminotetraline hydrochloride

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