Indorenate (TR3369, INDO) is a serotonin-like compound with high affinity for 5- HT1A receptors and a lower affinity for 5-HT1C and 5-HT1B receptors. Indorenate possesses antihypertensive and anxiolytic activity in animal behaviour tests. Similar to other serotonin receptor agonists, Indorenate also has anorectic activity; this effect was blocked by the administration of the 5-HT2A/2C receptor antagonists cinanserin, cyproheptadine, metergoline and methysergide. A unpublished clinical trial confirmed its antihypertensive activity in men.

Flutroline, an antipsychotic drug that was studied to treat patients with schizophrenia. Clinical trials have shown that the drug was a safe, effective, and 20 mg and above offered the best potential for optimal clinical effectiveness. However, information about the further development of this drug is not available.

Lotucaine is a local anesthetic.

Tigestol is an Estrene derivative patented by Organon Laboratories Ltd. as an anabolic, androgenic, and progestative agent.

Vinpoline was studied as a central stimulant. Information about the further development of this agent is not available.

Bimosiamose, discovered by Encysive Pharmaceutical and presently being developed by Revotar Biopharmaceuticals, is an 863 g/mol molecular weight dimer with minimal carbohydrate content and is, to date, the leading selectin inhibitor in clinical development. It was developed as anti-inflammatory drug fir the treatment of acute chronic inflammatory disorders including COPD. This compound has shown promise in a phase IIa 'proof of concept' trial in patients with asthma, reducing airway recruitment of eosinophils after intravenous administration. In acute lung injury, neutrophils (a type of white blood cells, thus belonging to the group of cells of the body’s defence system-the immune system) are drawn to the small lung bloodvessels and migrate into the air sacs (alveoli). There they release substances, which cause the inflammation leading to further destruction of the lung tissue. Bimosiamose disodium is expected to hinder the migration of these neutrophils into the alveoli.

Betacetylmethadol is a synthetic narcotic analgesic under international control according to the UN Single Convention 1961.

Mapracorat (BAY-865319, BOL-303242-X or ZK-245186) is a selective non-steroid glucocorticoid receptor agonist exerting anti-inflammatory activity. Mapracorat showed partial attenuation of the classical NF-κB pathway, consistent with traditional steroids. However, mapracorat uniquely potentiated a novel anti-inflammatory mechanism through rapid upregulation of RelB, an anti-inflammatory member of the NF-κB alternative pathway. Mapracorat was being studied in the treatment of ocular and skin inflammatory diseases.

Hydroxyflutamide is the major active metabolite of flutamide. Flutamide undergoes extensive first-pass metabolism by CYP1A2 to its metabolite hydroxyflutamide and its hydrolysis product, 3-trifluoromethyl-4-nitroaniline. Hydroxyflutamide is a more powerful antiandrogen in vivo, with higher affinity for the receptor than that of flutamide. Hydroxyflutamide is in phase II clinical trials for the treatment of prostate cancer. However, a drug resistance problem appears after about one year's treatment. Per-residue free energy decomposition analyses indicate that N705, T877, and M895 androgen receptor mutations are vital residues in the agonist/antagonist mechanism of hydroxyflutamide.

Pytamine is a nitrosamine derivative patented by Hercules Powder Co. as antioxidants, stabilizers, rubber additives, insecticides, fungicides, bactericides, and pharmaceutical intermediates. In preclinical trials Pytamine shows potent psychotropic effects associated modulation of GABAA receptors.