Pinolcaine is 10-methyl-2-substituted piperidine. Pinolcaine is a local anesthetic.

Alozafone is an anticonvulsant (CNS depressant).

Benolizime is a sedative and hypnotic drug but was never marketed.

Tesofensine (also known as NS-2330) is a novel triple monoamine reuptake inhibitor with intrinsic inhibitory activity on norepinephrine (NE), serotonin (5-HT), and dopamine (DA) transporter function. It was development by NeuroSearch as a potential therapy for Alzheimer's disease (AD) and Parkinson's diseases, but these efforts have been discontinued. In phase II clinical trials with tesofensine in obese individuals, dose-related reductions in body weight, body fat and waist circumference, as well as improvements in other obesity-related endocrine factors were observed and the FDA recently endorsed the phase III trial program for this agent.

Metrazifone was developed as an analgesic agent. However, this drug has never been marketed.

Adaprolol is a beta-adrenergic antagonist that is being developed as a topical agent to treat glaucoma. Adaprolol demonstrated a safer cardiovascular profile, especially in the population over 70 years old. It was in Phase II clinical trials for the treatment of glaucoma. This research has been discontinued.

Capeserod is benzodioxanoxadiazolone derivative patented by patented by pharmaceutical company Synthelabo S. A. as a novel 5-hydroxytryptamine4 receptor partial agonist with potent cognition-enhancing properties. In cells expressing the 5-HT4(b) and 5-HT4(e) splice variants, Capeserod acted as a partial agonist, stimulating cAMP prodn. with a maximal effect of 40 to 50% of serotonin. However, in the rat esophagus preparation, Capeserod acted as a 5-HT4 antagonist with a pKb of 8.81. In addition, Capeserod potently improved performance in several tests of learning and memory. In the object recognition task, it improved retention at 24 h when administered i.p. or p.o. (0.001-0.1 mg/kg). This effect was antagonized by the 5-HT4 antagonist SDZ 205,557, itself without effect, demonstrating that the promnesic effects of Capeserod are mediated by 5-HT4 agonism. Capeserod also reversed the cognitive deficits of aged rats in the linear maze task and the scopolamine-induced deficit of mice in the water maze task. Furthermore, the combined administration of an inactive dose of Capeserod with the cholinesterase inhibitor rivastigmine resulted in a significant promnesic effect, suggesting a synergistic interaction. Capeserod was devoid of unwanted cardiovascular, gastrointestinal, or central nervous system effects with doses up to more than 100-fold higher than those active in the cognitive tests. These results characterize Capeserod as a novel promnesic agent acting via 5-HT4 receptors, with an excellent preclinical profile.

Monometacrine is an acridan derivative and Dimethacrine metabolite patented by pharmaceutical company Siegfried A.-G. as an antidepressant.

Tolpadol is an analgesic agent. It is a prostaglandin synthesis inhibitor.

Ethylmethylthiambutene is a potent analgesic compatible with morphine. It possesses addiction liability similar to that of morphine.