Xamoterol (ICI 118,587) is a partial agonist of beta1-adrenoceptors. Xamoterol acts on the cardiac beta 1-adrenergic receptor, modifies the response of the heart to variations in sympathetic activity. At rest, it produces modest improvements in cardiac contractility, relaxation, and filling without increase in myocardial oxygen demand. The improvements are maintained during exercise although the attendant tachycardia is attenuated. The beneficial effects of xamoterol on both systolic and diastolic function suggested that it would be effective in patients with mild-to-moderate heart failure, and this was demonstrated in small placebo-controlled studies where effort tolerance and symptoms were improved. Xamoterol produced improvements in exercise capacity, clinical signs, symptoms and quality of life with a low incidence of adverse experiences. Xamoterol is effective as monotherapy in heart failure.

Tolonidine, 2(2-chloro-p-toluidino)-2-imidazoline-nitrate, is a substance chemically related to clonidine. In the anesthetized dog, tolonidine administered i.v. decreased the amplitude of ventricular contractions, reduced aortic blood flow and increased peripheral vascular resistances. In the bivagotomized pithed rat, tolonidine induced a long-lasting increase in blood pressure with no secondary hypotension, thus suggesting peripheral sympathomimetic properties, however, contractions of seminal vesicles in vitro were not obtained. The product proved to have no peripheral sympatholytic or parasympatholytic properties.

Rilmenidine (brand names Albarel, Hyperium, Iterium and Tenaxum) is an imidazoline derivative used for the treatment of hypertension. Rilmenidine, an oxazoline compound with antihypertensive properties, acts on both medullary and peripheral vasomotor structures. Rilmenidine shows greater selectivity for imidazoline receptors than for cerebral alpha2-adrenergic receptors, distinguishing it from reference alpha2-agonists. Rilmenidine is as effective in monotherapy as all other first line classes of drugs, including diuretics, beta-blockers, angiotensin converting enzyme (ACE) inhibitors, and calcium antagonists. It is well tolerated and can be taken in combination for greater efficacy. Sedation and dry mouth are not prominent side effects and withdrawal hypertension is not seen when treatment is stopped abruptly. In addition to a reduction in blood pressure, Rilmenidine has been shown to improve glucose tolerance, lipid risk factors, and insulin sensitivity.

Bezafibrate is a lipid-lowering fibric acid derivative. Bezafibrate directly bound to and activated all three peroxisome proliferator-activated receptor (PPAR) subtypes respectively in PPAR binding and transactivation assays. However, from a biochemical point of view, bezafibrate is a PPAR ligand with a relatively low potency. Bezafibrate leads to considerable raising of HDL cholesterol and reduces triglycerides, improves insulin sensitivity and reduces blood glucose level, significantly lowering the incidence of cardiovascular events and new diabetes in patients with features of metabolic syndrome. It is the only pan-PPAR activator with more than a quarter of a century of therapeutic experience with a good safety profile.

There is no available information about this compound

Celiprolol is beta blocker, used to treat high blood pressure. Celiprolol is a selective β1 receptor antagonist, β2 receptor partial agonist. Celiprolol is not approved by the FDA, but is available worldwide under brand names Cardem, Selectol, Celipres, Celipro, Celol, Cordiax, Dilanorm. It is used to treat mild to moderate hypertension and angina prectoris. In 2010 celiprolol has demonstrated positive results in the prevention of vascular complications of Ehlers-Danlos syndrome. Celiprolol has fewer CNS-related side effects than other beta blockers presumably because of limited penetration through blood-brain barrier because of its solubility.

Talinolol (brand name Cordanurn) is the cardioselective beta-receptor antagonist which has been used for a long time in the treatment of various cardiovascular diseases and in tachyarrhythmia. The mean dosage is 10-20 mg intravenously administered over a period of 3-5 minutes, while the chronic oral dosage for this patient group amounts to 300mg/day. Cordanum eliminates the stimulating effect of catecholamines on the heart for physical and psychoemotional stress. The hypotensive effect is stabilized by the end of 2 weeks of course treatment. Reduces the frequency and severity of angina attacks; Contributes to the limitation of the heart attack zone and reduces the risk of arrhythmia in the presence of myocardial infarction, resulting in a decrease in mortality and the frequency of relapses. In average therapeutic doses, it has a less pronounced effect on the smooth muscles of the bronchi, myometrium, and peripheral arteries compared to non-selective beta-blockers. Talinolol is used in supraventricular (atrial fibrillation and flutter with high ventricular rate, paroxysmal supraventricular 1 tachycardia, sinus tachycardia) as well as ventricular extrasystoles and ventricular tachyarrhythmias. Patients with an increased tonus of the sympathetic nervous system related to sinus tachycardia, exercise-induced arrhythmias, hypertension, hyperthyroidism and coronary heart disease show a particularly positive reaction.

Peruvoside, main component of neriperside, a tevetoside extracted from Thevitia neriifolia Juss, cardiac glycoside, is used for the treatment of heart failure. It is Na+, K(+)-ATPase inhibitor. Peruvoside also demonstrates anti-cancer activities. Peruvoside inhibited cell growth in androgen-resistant LNCaP-abl prostate at 50 nM, lower than the concentrations required by both Digoxin and Strophanthidin (500 nM), suggesting that it may be a more potent anti-cancer candidate that other CGs. Peruvoside induced apoptotic cell death in human primitive AML KG1a cells and chronic myelogenous leukemia (CML) cell K562.

Methyldopa is an aromatic-amino-acid decarboxylase inhibitor in animals and in man. Methyldopa is a medication that has been used to treat high blood pressure since the 1960s. Methyldopa is indicated in the treatment of moderate to severe hypertension, including that complicated by renal disease. Only methyldopa, the L-isomer of alpha-methyldopa, has the ability to inhibit dopa decarboxylase and to deplete animal tissues of norepinephrine. D-isomer is relatively inactive. In man the antihypertensive activity appears to be due solely to the L-isomer, which became generally known as methyldopa (Aldomet). About twice the dose of the racemate (Methyldopa anhydrous, (±)-; DL-alpha-methyldopa) is required for equal antihypertensive effect. Racemic alpha-methyldopa was shown to be much less effective or ineffective for the treatment of hypertension. The comparative study of the hypotensive effect of L-alpha-methyl-dopa (L-isomer) versus the racemic form was performed. The short-term hypotensive effects of the racemic form and the L-isomer of alpha-methyl-dopa were compared in 13 hospitalized patients with arterial hypertension. After a placebo period the active preparations in a fixed dose of 1.5 g daily were administered for three-day periods separated by a second placebo period of three days, the sequence of the active drugs being alternated. Both substances were shown to exert significant hypotensive effects. The L-isomer produced significant blood-pressure reductions irrespective of whether or not it was given first, whereas the racemic form was effective only when given first. The blood-pressure levels obtained with the L-isomer were throughout lower than those with the racemic form. Methyldopa is a centrally acting antihypertensive agent. It is metabolized to alpha-methylnorepinephrine in the brain, and this compound is thought to activate central alpha-2 adrenergic receptors