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Indoramin-d5 is intended for use as an internal standard for the quantification of indoramin by GC- or LC-MS. Indoramin is an antagonist of α1-adrenergic receptors (α1-ARs; Kis = 5, 10, and 50 nM for the human α1A-, α1B-, and α1D-ARs, respectively).1 It also binds to α1L-ARs (pA2 = 8.5) and inhibits norepinephrine and serotonin (5-HT) uptake in rat brain cortical slices (IC50 = 2 µM for both).2,3 Indoramin (5 mg/kg) decreases blood pressure in normotensive anesthetized rats.4 Intrathecal administration of indoramin decreases micturition pressure and increases bladder capacity and micturition volume in conscious rats.5 Formulations containing indoramin have been used in the treatment of urinary outflow obstruction in patients with benign prostatic hyperplasia.
WARNING This product is not for human or veterinary use.
1. Evaluation of the pharmacological selectivity profile of α1 adrenoceptor antagonists at prostatic α1 adrenoceptors: Binding, functional and in vivo studies. Br. J. Pharmacol. 118(4), 871-878 (1996).
2. RS-
3. The action of indoramin and other compounds on the uptake of neurotransmitters into rat cortical slices. Br. J. Pharmacol. 51(3), 467-469 (1974).
4. Synthesis and hypotensive activity of benzamidopiperidylethylindoles. J. Med. Chem. 14(11), 1054-1059 (1971).
5. Stimulation of bladder activity by volume, L-