Aminoacridine derivative that is a potent intercalating antineoplastic agent. It is effective in the treatment of acute leukemias and malignant lymphomas, but has poor activity in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy protocols. It produces consistent but acceptable myelosuppression and cardiotoxic effects. Although its mechanism of action is incompletely defined, amsacrine inhibits DNA synthesis by binding to and intercalating with DNA. Amsacrine also inhibits topoisomerase II activity and may exert an effect on cell membranes. This agent also possesses immunosuppressive and antiviral properties. While amsacrine is not cell cycle phase-specific, cytotoxicity is maximal during the G2 and S phases.

Hopantenic acid (homopantothenic acid) is a central nervous system depressant. Formulated as the calcium salt, it is used as a pharmaceutical drug in the Russian Federation under the brand name Pantogam. In Russia it is widely used to treat a variety of neurological, psychological and psychiatric conditions. The drug has been on the pharmaceutical market since 1979 and has been proven to be safe even for children from 3 years old upwards. Hopantenic acid is a natural forming substance, has some of the lowest side effects and considered to be very safe. Use Pantogam to treat a wide variety of cognitive and nervous system disorders with combined sedative and mild stimulant effect. Hopantenic acid is not approved for use in Europe or the United States. GABA receptor agonist.

Aptazapine is a “non-classic” tetracyclic antidepressant drug. Compound bears a structural resemblance to mianserin. Aptazapine possesses a high degree of potency and selectivity for central alpha-2, as opposed to alpha-1, adrenoceptors. Aptazapine failed to inhibit in vitro uptake of norepinephrine or serotonin to an appreciable extent. However, it exhibited a moderate ability to compete for 5-HT2 receptor binding in calf frontal cortex, as measured by displacement of 3H-spiroperidol. Another property apparently shared with other antidepressants is the ability of aptazapine to inhibit histamine-activated adenyl cyclase. As centrally acting alpha-2 adrenoceptor antagonists, aptazapine significantly suppressed cataplexy, a major symptom of narcolepsy, in Doberman pinschers.

Alifedrine, a beta-adrenergic partial agonist, significantly improved performance of the failing heart. Alifedrine resulted in a significant dose-dependent increase in cardiac output. There were significant reductions in peripheral resistance, but little observed change in arterial pressure. With intravenous alifedrine, there were significant increases in stroke volume with little change in heart rate. With the 40 mg oral dose, there was a small increase in heart rate There were no clinically or statistically significant changes in arterial (non-invasive), pulmonary artery, pulmonary capillary or right atrial pressures with any dose of alifedrine. No significant arrhythmias were noted clinically with the doses studied.

Zatebradine is a bradycardic compound that blocks hyperpolarization-activated inward current (If) through cyclic nucleotide-gated cation (HCN) channels in sinoatrial node cells. Additionally, it can block voltage-gated outward K+ (IK) currents and related neuronal hyperpolarization-activated inward current (Ih) channels but exhibits little or no activity for L-type Ca2+ (ICa) currents. When assessed through telemetric ECG recording in mice, zatebradine reduced heart rate from 600 to 200 beats per minute with an ED50 value of 1.8 mg/kg and induced increasing arrhythmia at concentrations >10 mg/kg.

Bisoxatin (Laxonalin, Wylaxine) acetate is a stimulant laxative that has been used in the treatment of constipation. The drug showed good effects to habitual constipation and dolichocolon but was not sufficient acting in megacolon. It seems that the drug is effective to constipation due to functional disorders but the effect is not sufficient to constipation caused chiefly by organic colonic changes. No side effect was observed even in long term administration.