Rilmenidine-d4

Rilmenidine-d4 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  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.

• Einzelnachweise

  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)

Rilmenidine-d4 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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