Bimakalim (also known as EMD 52692), a potassium channel opener, was studied for patients with bronchial asthma and with stable angina pectoris. Besides the drug was used against arrhythmias and hypertension. However, the development of bimakalim has been discontinued.

Carmoxirole is a dopamine D2 receptor agonist with limited central activity that modulates sympathetic activation and subsequently reduces pre-load and afterload in animals. It was shown, that carmoxirole induced beneficial effects on hemodynamic and neurohumoral parameters in heart failure. In addition, experimental evidence showed that carmoxirole lowered blood pressure in various models of hypertension mainly or exclusively through inhibition of noradrenaline release from sympathetic nerve endings. That effect of carmoxirole was mediated by presynaptic dopamine receptors with the characteristic that release inhibition was restricted to low rates of sympathetic nerve discharge.

Iomazenil (also known as Ro16-0154, benzodine) is a partial inverse agonist of central-type benzodiazepine receptors (BZR) which binds specifically to BZR with high affinity and a potential treatment for alcohol abuse. The compound was introduced in 1989 by pharmaceutical company Hoffmann-La Roche as an Iodine-123-labelled SPECT tracer for imaging benzodiazepine receptors (GABAA receptors) in the brain.

Normorphine is an opiate analog, specifically the N-demethylated derivative of morphine. It was first described in the 1953 as part of an effort to characterize N-substituted morphine analogs. Normorphine has relatively little opioid activity, but it is a useful intermediate for the production of more potent morphine analogs. It is also a major metabolite of morphine.

Vinleucinol (also known as vinblastine-isoleucinate or V-LEU) was developed as a vinca alkaloid derivative. This compound exhibited superior antitumor activity in malignant melanoma, small cell lung carcinoma, and breast cancer lines. Experiments on animals have shown that metabolite of vinleucinol was mainly responsible for the antitumor.

Dolastatin 10 is an unusual peptide of marine origin which binds to tubulin, inhibits microtubule assembly, resulting in the formation of tubulin aggregates and inhibition of mitosis. Dolastatin 10 has been used in trials phase II studying the treatment of Sarcoma, Leukemia, Lymphoma, Liver Cancer, among others. In case of hormone-refractory prostate cancer, it lacks significant clinical activity as a single agent and also dolastatin-10 is inactive against hepatobiliary and pancreatic carcinomas.

Tetraisopropyl 2-(3,5-Di-Tert-Butyl-4-Hydroxyphenyl)Ethyl-1,1-Biphosphonate (also known as SR-9223I and SR 45023A) is a gem-diphosphonate derivative patented by Symphar S. A. as an antihypertensive and anti-inflammatory agent. Tetraisopropyl 2-(3,5-Di-Tert-Butyl-4-Hydroxyphenyl)Ethyl-1,1-Biphosphonate acts as 3-hydroxy-3-methylglutaryl reductase inhibitor, besides that SR-9223I suppresses acyl-CoA: cholesterol acyltransferase activity and prevents the oxidation of plasma lipoproteins. In preclinical studies, SR-9223i reduces blood cholesterol concentrations in mice, hamsters, dogs, and monkeys. SR-9223i inhibits the growth of a wide variety of tumor cell lines in vitro and triggered apoptosis in HL60 cells in less than 2 h. SR-9223i induces caspase-3 activity at concentrations similar to it’s IC(50) values for cell proliferation. Unfortunately, in clinical trials SR-9223I failed to demonstrate efficacy in patients with refractory melanoma and further development was discontinued.

6-O-BENZYLGUANINE is a guanine analogue with antineoplastic activity. O(6)-benzylguanine binds the DNA repair enzyme O(6)-alkylguanine DNA alkyltransferase (AGT), transferring the benzyl moiety to the active-site cysteine and resulting in inhibition of AGT-mediated DNA repair. Co-administration of this agent potentiates the effects of other chemotherapeutic agents that damage DNA. 6-O-benzylguanine has been used in trials studying the treatment of HIV Infection, Adult Gliosarcoma, Adult Glioblastoma, Stage I Adult Hodgkin Lymphoma, and Stage II Adult Hodgkin Lymphoma, among others.

Celgosivir is a butanoyl ester derivative of castanospermine, a compound derived from the Australian chestnut with activity against hepatitis C virus. Celgosivir rapidly converts to castanospermine in the body, where it is a potent inhibitor of alpha-glucosidase I, a host enzyme required for viral assembly, release, and infectivity.