Cinnofuradione is a cinnoline derivative with analgesic properties. It was patented in 1954 and was claimed to be useful in combatting inflammation and rheumatism.

Siramesine is a sigma2 opioid agonist under development by H Lundbeck as a potential treatment for anxiety. In March 1998, the compound was licensed to Forest Laboratories under a strategic alliance. In August 2000, siramesine entered phase II trials. Siramesine has been shown to trigger cell death of cancer cells and to exhibit a potent anticancer activity in vivo. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Siramesine is a lysosomotropic detergent that induces cytoprotective autophagosome accumulation. Siramesine involves lysosomal leakage and oxidative stress.

Cidoxepin is the cis-isomer of the widely prescribed tricyclic compound doxepin. Commercial preparations of the tricyclic anti-depressant doxepin contain 15% of the more active cis-doxepin and 85% of the trans-isomer. Elorac, Inc., a rapidly growing specialty pharmaceutical company focused on the treatment of dermatological disorders, is pleased to announce that it has acquired worldwide rights to the active agent Cidoxepin from Gideon Pharmaceuticals. Cidoxepin appears to be much more potent than doxepin while having less sedative and cholinergic side effects. Elorac plans to develop oral formulations of the drug to treat urticaria and topical formulations for treatment of atopic and contact dermatitis.

Velneperit, also known as S-2367, is a once-daily, oral, centrally acting, small molecule neuropeptide Y (NPY) Y5 receptor antagonist that was discovered by Shionogi Research Laboratories. It was developed for the oral treatment of obesity. Velneperit was in phase II trials, however, development was discontinued.

Tiflamizole is a fluorinated diarylamidazole derivative patented by du Pont de Nemours, E. I., and Co. as an anti-inflammatory agent. Tiflamizole acts as a non-steroidal anti-inflammatory drug, that exerts potent inhibition of prostaglandin synthesis and exhibits anti-inflammatory, antipyretic, and analgesic activity in animal studies. Preliminary studies in animals and man have shown that Tiflamizole is rapidly absorbed from the gastrointestinal tract, is highly protein-bound, and is slowly excreted. Toxicity studies in animals focused on the gastrointestinal tract. Short-term toxicity studies in rats indicated that the margin of safety of Tiflamizole is greater than that for piroxicam, ibuprofen, or sulindac.

Propanocaine is a benzyl alcohol derivative with local anesthetics activity

Pinadoline is a competitive PGE2 antagonist. It is an analgesic agent. Pinadoline demonstrated the antinociceptive activity in the rat using the writhing and the formalin tests. In the writhing test, pinadoline was significantly more potent than inhibitors of PG synthesis, but less potent than opiate analgesics. In the formalin test, pinadoline appeared less active than aspirin and ibuprofen and more active than acetaminophen. Pinadoline does not possess the antiinflammatory activity of aspirin and ibuprofen and may be more like acetaminophen, which had diminished antiinflammatory activity. At high concentrations, pinadoline is a non-competitive antagonist of serotonin in guinea-pig ileum.

Tolamolol is a phenoxypropranolamine derivative that preferentially inhibits myocardial beta adrenoreceptors, possesses beta blocking potency equivalent to propranolol, has little or no direct cell membrane effect and lacks beta adrenergic stimulating action. Cardioselective beta adrenergic blockade with tolamolol was highly effective in controlling ventricular rate in supraventricular arrhythmias and reduced the frequency of ventricular ectopic beats in half of the small group of patients with this arrhythmia. It is particularly applicable in patients with obstructive pulmonary disease in whom cardiac beta adrenergic blockade is indicated. Hypotension is an important potential side effect. Tolamolol and propranolol are equal in anti-anginal efficacy but tolamolol has the advantage of being cardioselective. It is superior to practolol. Tolamolol had no effect on sperm motility.

Tofetridine is an analgesic agent.