Rilmenidine (hemifumarate)

Rilmenidine is an antihypertensive agent. It binds to imidazole receptors in bovine rostral ventrolateral medulla homogenates (Ki = 6.1 nM), as well as alpha2-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. Rilmenidine (1 µM) increases levels of LC3-II, a marker of autophagy, in PC12 cells. Formulations containing rilmenidine have been used in the treatment of hypertension.Formal Name: N-(dicyclopropylmethyl)-4,5-dihydro-2-oxazolamine, 2E-butenedioate (2:1). CAS Number: 207572-68-7. Synonyms: Oxaminozoline, S 3341. Molecular Formula: C10H16N2O . 1/2C4H4O4. Formula Weight: 238.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/ml, DMSO: 3 mg/ml, Ethanol: 10 mg/ml, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml. SMILES: OC(/C=C/C(O)=O)=O.C1(NC(C2CC2)C3CC3)=NCCO1.C4(NC(C5CC5)C6CC6)=NCCO4. InChi Code: InChI=1S/2C10H16N2O.C4H4O4/c2*1-2-7(1)9(8-3-4-8)12-10-11-5-6-13-10,5-3(6)1-2-4(7)8/h2*7-9H,1-6H2,(H,11,12),1-2H,(H,5,6)(H,7,8)/b,,2-1+. InChi Key: LZFATBMLSYHRTC-WXXKFALUSA-N.