LAPAQUISTAT is a squalene synthase inhibitor. It was shown to lower cholesterol levels in several animal models. It was investigated for the treatment of diabetes and hypercholesterolemia, however, its development was discontinued.

Neosaxitoxin is a site-1 specific sodium channel blocker which acts synergistically with local anesthetics to provide surgical anesthesia by peripheral nerve blocks or local infiltration and markedly increases the duration of post-operative analgesia. Saxitoxin and neosaxitoxin, small molecules synthesized by marine dinoflagellates and freshwater cyanobacteria. Neosaxitoxin, one of the saxitoxin analogs, differs from saxitoxin by the addition of one oxygen atom, wherein the hydrogen (-H) at Nitrogen 1 in saxitoxin is replaced by a hydroxyl group (-OH) in neosaxitoxin. Neosaxitoxin has shown greater potency than saxitoxin and its analogs and is also more potent than tetrodotoxin in in vitro and in vivo animal studies.Neosaxitoxin showed an effective local anesthetic effect when injected in the subcutaneous plane. The efficacy of a 50-ug dose of neosaxitoxin was shown. Neosaxitoxin has poor affinity for the cardiac isoform of the sodium channel and does not cross the blood–brain barrier, thus this compound is virtually devoid of cardiac and central nervous system toxicity—the limiting toxicities of traditional local anesthetics.

Modaline is piperidinopyrazine derivative developed by Warner-Lambert Pharmaceutical Co. as Antidepressant. Modaline is a potent monoamine oxidase (MAO) inhibitor of the order of the more effective hydrazines. Pretreatment with harmaline, a reversible MAO inhibitor, or with serotonin prevented the irreversible inhibition by Modaline, suggesting that Modaline (as an active MAO inhibitor) occupies the same site on MAO as harmaline, the hydrazines, or serotonin. Modaline differs from the monoamine oxidase inhibitors by producing an increase in body temperature in fully reserpinized animals. Modaline differs from imipramine‐like drugs in not potentiating the hyperthermic effect of isoprenaline.

Losulazine (U-54,669F) is an antihypertensive agent acting by a sympatholytic mechanism. It appears to alter peripheral sympathetic neurogenic function but apparently does not enter the central nervous system. Losulazine effectively lowered the blood pressure in patients with hypertension.

ISOMOLPAN is a selective D3/D2 receptor agonist.

Dexsotalol is an isomer of antiarrhythmic drug d,l-sotalol, but in opposite to drug, it increases the incidence of arrhythmias

Ipexidine is a biologically active carbamimidoylurea derivative