Acevaltrate is an iridoid found in variable amounts in Valerianaceae and might be among the bioactive compounds which confer anxiolytic properties to the Valeriana species. Acevaltrate inhibited total H⁺/K⁺-ATPase activity (60.7 ± 7.3 %) from rat gastric epithelium. Acevaltrate inhibited Na⁺/K⁺-ATPase with IC₅₀ value of 22.8 uM. Na⁺/K⁺-ATPase might be one of their molecular targets of Acevaltrate in vivo.

Metaglycodol is a tranquilizer.

Niravoline [RU 49679, RU 51599, niravolin], a novel aqueous diuretic with κ-opioid agonistic action. The drug was originally being developed by Hoechst Marion Roussel. Niravoline is a selective agonist of kappa-opioid receptors having potent aquaretic activity. Niravoline was studied with respect to the treatment of brain oedema, heart failure and liver cirrhosis. Niravoline, administered at moderate doses, safely induced a powerful aquaretic effect in patients with cirrhosis and ascites. Moderate doses of niravoline appeared to be a promising pharmacological tool in the treatment of water retention in patients with cirrhosis. The development of niravoline as an aquaretic for the treatment of cirrhosis with ascites and other hyponatraemic disorders has also been halted.

Batelapine (or CGS 13429), an antipsychotic drug, that was undergoing preclinical development, but the further studied were discontinued

Oxepinac was developed as an anti-inflammatory drug. Results of clinical trials have revealed that oxepinac was an effective and well-tolerated drug in the treatment of painful osteoarthritis. Experiments on animal have shown that oxepinac had no teratogenic effect on fetuses in mice and rabbits. Information about the current use of this drug is not available.

Sumacetamol is a acetylaminothioalkanoate derivative patented by Sterwin A.-G. as an analgesic and antipyretic agent. Sumacetamol is used in combination with free paracetamol. In clinical trials, Sumacetamol failed to demonstrate superior efficacy in pain and swelling management compare to paracetamol but shows a longer duration of analgesia. The rates of reported adverse events were similar in paracetamol and Sumacetamol, although reports of mild to moderate drowsiness were more common after the Sumacetamol combination.

Fenclorac is a potent nonsteroidal anti-inflammatory agent with significant analgesic and antipyretic activity. It inhibits prostaglandin synthesis both in vitro and in vivo.

Alvameline is a partial agonist of the M1 mAChR that also displays M2/M3 antagonist effects. It readily crosses the blood-brain barrier. It has an effect profile that makes it of interest to test its ability to counteract bladder overactivity in humans. Behaviorally, alvameline has been shown to significantly improve Morris water maze (MWM) performance in both young and ageimpaired rats. It failed to improve cognition in patients with mild to moderate Alzheimer's disease.

Ritanserin (INN, USAN, BAN) is a serotonin receptor antagonist which was never marketed for clinical use but has been used in scientific research. In humans, ritanserin increases deep slow-wave sleep, improved liveliness in a variety of psychiatric disorders and facilitated participation in behaviour therapy. During clinical trials, unexpected observations indicated that ritanserin may be of value in treating obsessive-compulsive disorder, acute mania, negative symptoms of schizophrenia, drug addicts, etc. Clinical observations confirmed the efficacy of ritanserin in the chronic withdrawal phase after detoxification from ethanol. Ritanserin had been in phase III clinical trials by Janssen L.P. for the treatment of anxiety disorder and major depressive disorder. However, the clinical development of ritanserin was discontinued.

Procymate is a cyclohexylpropyl derivative patented by Compagnie Francaise des Matieres Colorantes as a non-hypnogenic depressor of the nervous system.