Disease relevance of CARMOXIROLE

• Experimental evidence shows that carmoxirole lowers blood pressure in various models of hypertension mainly or exclusively through inhibition of noradrenaline release from sympathetic nerve endings [1].
• In the carmoxirole-treated subjects (n = 16), 6 subjects reported spontaneously adverse events such as syncope, dizziness and vomiting tendencies and/or fatigue [2].

High impact information on CARMOXIROLE

• Furthermore, carmoxirole (0.003-0.3 mumol/l) markedly reduced pressor responses induced by the alpha 1-adrenoceptor agonist methoxamine (1 mumol/l) but even the highest concentration of carmoxirole (0.3 mumol/l) had no effect on pressor responses induced by bolus injections of either neuropeptide Y (1.5 ng) or angiotensin II (1 ng) [3].
• The effect of carmoxirole on neurohormones and hemodynamics in humans was evaluated in 12 normotensive patients with NYHA class III-IV heart failure on stable ACE 1 and diuretic therapy [4].
• Thus, carmoxirole modulates sympathetic activation, accompanied by changes in vasopressin and ANP, and the renin-angiotensin system at higher dosages [4].
• Carmoxirole inhibits platelet aggregation in vitro and ex vivo [5].
• In an open study 15 patients with essential hypertension received 3 doses of carmoxirole, 0.5, 1 and 2 mg daily, each for a 2-week period, following a 2-week placebo phase [5].

Biological context of CARMOXIROLE

• Carmoxirole did not affect supine blood pressure in healthy subjects, but under the conditions of the Schellong's test some orthostatic reactions occurred with high doses [6].
• Blood pressure and heart rate were not changed during carmoxirole administration in these normal men [2].

Anatomical context of CARMOXIROLE

• Erythrocyte and platelet cationic concentrations and transport systems in normal volunteers treated with carmoxirole [2].

Associations of CARMOXIROLE with other chemical compounds

• Compared to 100% before treatment, the 5-hydroxytryptamine induced platelet aggregation velocity ex vivo decreased to 70%, 38% and 69% after the administration of 0.5, 1 and 2 mg carmoxirole, respectively [5].
• The inhibitory effect of carmoxirole (0.03 microM) was prevented by the D2-receptor antagonist (-)-sulpiride (10 microM) but not by the D1-receptor antagonist SCH 23390 (1 microM) in human kidney slices [7].

Gene context of CARMOXIROLE

• Carmoxirole in higher concentrations (0.3 microM) blocks inhibitory prejunctional alpha-autoreceptors, which seems to mask the inhibitory D2-receptor mediated effect [7].

References