Oxilorphan (also known as levo-BC-2605) was developed as a long-acting, narcotic antagonist that has agonist properties. Oxilorphan is a partial agonist at the kappa-opioid receptor and antagonist of the mu-opioid receptor. During clinical trials, oxilorphan had led to dysphoria, which combined with its hallucinogenic effects, serves to limit its clinical usefulness. As a result, many patients who experienced these side effects refused to take additional doses in clinical trials.

Lodoxamide ethyl, diethyl N,N'-(2-chloro-5-cyano-m-phenylene) dioxamate, is an orally active candidate for the treatment of asthma and other allergic diseases. Lodoxamide ethyl prevents mast cell mediator release during allergic reactions in rats, guinea pigs, and monkeys at doses well below toxic levels. Lodoxamide ethyl does not interfere with antigen-antibody interaction, does not antagonize the effects of histamine or slow-reacting substance of anaphylaxis, and does not have direct antiinflammatory effects. Lodoxamide ethyl has been proven capable of preventing bronchospasm in humans when the subject was given 1, 3, or 10 mg of the drug orally prior to challenge with an antigen.

Pinacyanol iodide is a fluorescent cationic cyanine dye used to stain biological specimens. It is the obstetric diagnostic aid. The mechanism of tracing with pinacyanol iodide dyes is based on their lipid solubility. Pinacyanol iodide dyes are more efficacious than classical tracing methodologies especially during early stages of development and consequently have been used to reveal the spatiotemporal patterns of axonal development in different species. The unique properties of the pinacyanol iodide dye tracing method have opened up new avenues for tracing connections in human postmortem specimens. Pinacyanol iodide dye tracing is incompatible with alcohol fixation and paraffin embedding of tissue.

Muscimol is one of the principal psychoactive constituents of Amanita muscaria and related species of mushroom. Muscimol is a potent, selective agonist for the GABAAreceptors and displays sedative-hypnotic, depressant and hallucinogenic psychoactivity. The effects of the Amanita mushrooms begin 30–120 minutes after consumption and the effects last for 5–10 hours. Some of the desired effects include euphoria, dream-like (lucid) state of mind, out-of-body experiences, and synesthesia. Neutral effects include dizziness, clumsiness, the feeling of increased physical strength, loss of equilibrium, and a glassy-eyed stare. Calming effects may be felt, but completely opposite effects such as extreme energy bursts have been described. Negative effects include mild to moderate nausea, stomach discomfort, increased salivation, and muscle twitching or tremors. In large doses, strong dissociation or delirium may be felt.

Drinidene is the analgesic agent.

Metogest, a hormone, is a progesterone receptor agonist. Metogest was used in acne treatment. However, this drug has never been marketed.

Prinomide is a carbamoylpyrrolepropionitrile derivative patented by Ciba-Geigy A.-G. as a nonsteroidal anti-inflammatory drug that has disease-modifying activity in rheumatoid arthritis. In clinical trials, Prinomide demonstrate significant improvement in symptom score and laboratory variables.

Oradon was developed as a mercurial diuretic for oral administration. Information about the current use of this drug is not available.