Cianergoline is an ergoline derivative with marked dopaminergic agonist and a predominant cardiovascular action patented by Farmitalia Carlo Erba S.p.A for hypertension treatment. The preclinical evaluation shows dose-related hypotensive effects after single oral, intraduodenal and intravenous administration of Cianergoline in cats, dogs, and rats. Cianergoline showed a prompt onset of action and a prolonged effect on blood pressure at low doses without substantially modifying animals heart rate. One month daily oral administration of Cianergoline in rats produced an antihypertensive effect persisting through the entire experiment with no signs of tachyphylaxis. Unfortunately, in clinical trials Cianergoline caused a slight, statistically non-significant blood pressure lowering effect in patients with essential hypertension and does not modify the release of prolactin, lipid metabolism or the basal activity or postural responsiveness of the renin-angiotensin-aldosterone axis and of the sympathetic nervous system.

Oglufanide, an angiogenesis inhibitor, an immunomodulator, that originally was developed and registered in Russia under the brand name timogen. Oglufanide inhibits vascular endothelial growth factor (VEGF), which may inhibit angiogenesis. This agent has also been reported to stimulate the immune response to hepatitis C virus and intracellular bacterial infections. Oglufanide was studied in the USA for the treatment of cancer, and in September 2001, it was granted Orphan Drug designation for the treatment of ovarian cancer. In addition, in Australia this drug was involved in phase II clinical trial for the treatment of hepatitis C. Oglufanide is also participated in phase III trials for patients with Kaposi's sarcoma, however, this study was discontinued.

Diapamide is an effective diuretic and saluretic agent in rats, dogs, and monkeys. A pharmacologic animal study indicated that diapamide may be equal or superior to furosemide in experimentally induced congestive failure. Diapamide possessed the ability to induce water loss approximately equally from cells and extracellular fluid with or without the presence of excess water. The most frequently occurring ad- verse reaction was mild to moderate nausea, diarrhea and vomiting. In human, urine output with furosemide was significantly greater than with diapamide. Thus, diapamide would appear to serve a role between the milder thiazide diuretics and the more effective furosemide.

Damotepine is a derivative of thiepin, structurally related to doxepin. Damotepine was discovered by the Swiss pharmaceutical company Geigy A.G. and was evaluated in clinical trials for the treatment of anxiety in the early 1970s.

Palinavir (formerly BILA2011BS) is a potent inhibitor of the human immunodeficiency virus type 1 (HIV-1) and type 2 (HIV-2) proteases and was studied for the treatment of HIV infections. However, information about the current development of this drug is not available.

Orotirelin (previously known as CG 3509) was investigated as a thyrotropin-releasing hormone. Experiments on rats have shown that compound could increase dopamine release from rodent brain. Information about the current study of this drug is not available.

Omecamtiv mecarbil (CK-1827452) is a specific cardiac myosin activator and a clinical drug for left ventricular systolic heart failure (in Phase 2 of development). Omecamtiv mecarbil is an inotropic agent that prolongs systolic ejection time and increases ejection fraction through myosin ATPase activation.

Ofornine is a vasodilator with antihypertensive activity. Experiments on rats have shown that ofornine reduced spontaneously hypertensive (SH) blood pressure through vasodilating and presynaptic adrenolytic activities, and that a dopaminergic mechanism may be involved. Information about the current use of this drug is not available.

Cericlamine (INN) is a potent and moderately selective serotonin reuptake inhibitor (SSRI) of the amphetamine family that was investigated as an antidepressant for the treatment of depression, anxiety disorders, and anorexia nervosa by Jouveinal