Bifemelane is a psychotropic drug, was found to inhibit monoamine oxidase (MAO). It inhibited type A MAO (MAO-A) competitively and type B (MAO-B) noncompetitively and it was a more potent inhibitor of MAO-A than of MAO-B. Bifemelane is an antidepressant and cerebral activator that is used in Japan for the treatment of cerebral infarction patients with depressive symptoms, and in the treatment of senile dementia as well. It also appears to be useful in the treatment of glaucoma.

Proglumide is a drug that inhibits gastrointestinal motility and reduces gastric secretions. It acts as a cholecystokinin antagonist, which blocks both the CCKA and CCKB subtypes. It was used mainly in the treatment of stomach ulcers, although it has now been largely replaced by newer drugs for this application. An interesting side effect of proglumide is that it enhances the analgesia produced by opioid drugs, and can prevent or even reverse the development of tolerance to opioid drugs. This can make it a useful adjuvant treatment to use alongside opioid drugs in the treatment of chronic pain conditions such as cancer, where opioid analgesics may be required for long periods and development of tolerance reduces clinical efficacy of these drugs.

Pimethixene is an antihistamine exerting sedative and antitussive properties. Pimethixene displayed high affinity to serotonin 5-HT2A and 2B, histamine H1 and muscarinic acetylcholine M2 receptors. Oral pimethixene used to calm dry cough and irritation coughs in children.

Ketanserin is a selective 5HT2A receptor antagonist which was initially developed as an anti-hypertensive medicine. However, now the drug is available as a topical gel formulation for the treatment of wounds, burns, ulcers and anal fissure (Sufrexal brand name). The drug action is explained by its ability to accelerate epithelialization.

Mepindolol is a selective beta1-adrenoreceptor blocker with intrinsic sympathetic activity. Treatment with mepindolol dose not significantly affect the lipid levels - the total cholesterol in plasma was decreased by mepindolol but HDL-cholesterol increased. During beta-receptor blockade with mepindolol-sulfate angina was compensated, the unfavourable hemodynamic effects seen during placebo did not occur. No signs of congestive heart failure were found during mepindolol-sulfate-therapy. Mepindolol-sulfate showed a pronounced blood-pressure lowering effect.

Enoximone is an inhibitor of PDE3, which is used for the treatment of congestive heart failure. Also enoximone was shown to inhibit PDH in cardiac myocytes. The inhibition was shown to occur secondary to stimulating fatty acid oxidation

Lercanidipine is antihypertensive drugs which acts by blocking L-type calcium channels, allowing relaxation and opening of blood vessels. Lercanidipine exists as a racemate, with anti-hypertensive activity residing primarily in S-enantiomer. NDA for lercanidipine was submitted to FDA in 2002 by Forest Laboratories, but FDA refused to approve the drug, and lercanidipine is not marketed in USA. Lercanidipine is also investigated in preclinical models of epilepsy and ischemic stroke.

Ticlatone (trade name Landromil) is an antifungal for topical use.

Vetrabutine is a spasmolytic agent. As a musculotropic spasmolytic agent vatrabutine was reported to act directly on the smooth muscle fibers and to have no neurotropic activity. In pigs, its activity was specific to the uterine body and cervical musculature where it acted on the myometrial cells, sealing off the membrane against the passage of potassium ions, thereby increasing membrane potential and lowering tonus. Vetrabutine was of moderate acute oral toxicity. Vetributine hydrochloride has been used in human medicine as a spasmolytic agent in obstetrics.

Lorcainide is a class Ic antiarrhythmic medication. It was reported to be highly efficient for the treatment of ventricular arrhythmias, ventricular fibrillation, and tachycardia. The drug was used under the name Remivox. The mechanism of lorcainide action involves the blockage of sodium channels. Lorcainide was withdrawn from the market for a commercial reason, but later it was admitted that the use of the drug is associated with high risk of death.