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Rilmenidine-d4 is intended for use as an internal standard for the quantification of rilmenidine by GC- or LC-MS. Rilmenidine is an antihypertensive agent.1 It binds to imidazole receptors in bovine rostral ventrolateral medulla homogenates (Ki = 6.1 nM), as well as α2-adrenergic receptors in bovine prefrontal cortex homogenates (Ki = 87 nM). Rilmenidine induces hypotension and bradycardia in anesthetized rats (ED50s = 0.25 and 0.35 mg/kg, respectively). It also reduces mean arterial pressure and renal sympathetic nerve activity in a rabbit model of renal hypertension induced by a renal artery clip when administered at a dose of 2.5 mg/kg.2 Rilmenidine (1 µM) increases levels of LC3-II, a marker of autophagy, in PC12 cells.3 Formulations containing rilmenidine have been used in the treatment of hypertension.

1.Gomez, R.E., Ernsbarger, P., Feinland, G., et al.Rilmenidine lowers arterial pressure via imidazole receptors in brainstem C1 areaEur. J. Pharmacol.195(2)181-191(1991) 2.Burke, S.L., Evans, R.G., and Head, G.A.Effects of chronic sympatho-inhibition on renal excretory function in renovascular hypertensionJ. Hypertens.29(5)945-952(2011) 3.Williams, A., Sarkar, S., Cuddon, P., et al.Novel targets for Huntington's disease in an mTOR-independent autophagy pathwayNat. Chem. Biol.4(5)295-305(2008)

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