Cloquinozine is a quinazoline derivative discovered by Japanese company Chugai Pharmaceutical in the 1960s. Cloquinozine has oxytocic properties and induces uterine contractions when administered to rabbits intravenously at 1 mg/kg.

Pheneridine is a synthetic opioid. It was developed as a narcotic agent.

PYM50018 (also known as Myogane or SARSAGENIN) has demonstrated neuroprotective effects in several preclinical models. It was observed that PYM50018 protects against neuronal damage, increases neurite outgrowth, reverses oxidative damage and reversed neuronal apoptosis. PYM50018 is in phase I clinical study for the treatment of amyotrophic lateral sclerosis (ALS).

Brifentanii, a potent narcotic analgesic structurally similar to alfentanil, that was studied in clinical trials in the early 1990s. The effects of brifentanil are very similar to those of alfentanil, with strong but short lasting analgesia and sedation, and particularly notable itching and respiratory depression. Side effects of Brifentanii are similar to those of fentanyl itself, which include itching, nausea and potentially serious respiratory depression, which can be life-threatening.

Xylocoumarol is an anticoagulant that has never been marketed. Information about the current use of this compound is not available.

Dioxamate is the anticonvulsant. It was developed as anti-epileptic agent.

Ensaculin is related to naturally occurring benzopyranones like scoparone. The compound is a potent functional antagonist of excitatory amino acid-induced convulsions and mortality. In receptor-binding studies, Ensaculin showed high affinity to dopaminergic (D2, D3), serotoninergic (5-HT1A, 5-HT7), and adrenergic (A1a, A1b) receptors in the nanomolar range. Ensaculin antagonizes NMDA responses in a voltage-dependent manner. Various studies support the notion that this compound could indeed have a broad range of nootropic properties. Although few patients presented postural hypotension and dizziness after receiving ensaculin in phase I clinical trials, this drug candidate was further discontinued in phase III due to potential side effects.

FLAVAMINE is a diterpenoid alkaloid isolated from the roots of Aconitum fiavum.

Sulmarin is a water-soluble coumarin derivative with vitamin P activity. In preclinical models Sulmarin facilitates excitatory transmission from parasympathetic fibers to the gastric musculature, increasing acetylcholine release. Sulmarin reduced the tone of isolated calf coronary arteries and also inhibited the contractile response of the arteries to angiotensin II amide (Hypertensin).

KETORFANOL, a morphinan derivative, is an opioid analgesic. It showed potent antiwrithing activity in the animal assay. It was equipotent with morphine as an agonist and lacked antagonist activity up to 10 mg/kg.