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Rilmenidine-d4 is intended for use as an internal standard for the quantification of rilmenidine (Item No. 16988) 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.
WARNING This product is not for human or veterinary use.
1. Rilmenidine lowers arterial pressure via imidazole receptors in brainstem C1 area. Eur. J. Pharmacol. 195(2), 181-191 (1991).
2. Effects of chronic sympatho-
3. Novel targets for Huntington’s disease in an mTOR-