Acetryptine is an antihypertensive agent. Acetryptine was found to bind 5-HT1A and 5-HT1D receptors with high affinity. It may also act as a monoamine oxidase inhibitor (MAOI), specifically, as an inhibitor of MAO-A.

CI-201 (also known as VB-201) is pure synthetic Lecinoxoid, oxidized phospholipid analog, for prevention and treatment of atherosclerosis and central nervous system (CNS) autoimmune inflammatory disease. In preclinical models, CI-201 ameliorated the severity of experimental autoimmune encephalomyelitis (EAE) induced by myelin oligodendrocyte glycoprotein (MOG) peptide, and constrained the infiltration of pathogenic CD4+ T-cells into the CNS and impaired their IFN-γ production. CI-201 inhibits Toll-like receptor (TLR) signaling restricted to TLR-2 and TLR-4 in human monocytes and dendritic cells, and exhibits up to 90% inhibition of monocyte chemotaxis in vitro. Interestingly, CI-201 did not inhibit monocyte adhesion or phagocytosis and had no effect on chemotaxis of neutrophils. In vivo, oral treatment with CI-201 reduced monocyte migration in a peritonitis model and inhibited atheroma development in ApoE(-/-) mice, without affecting cholesterol or triglyceride levels. CI-201 is developed by Vascular Biogenics for the oral treatment of atherosclerosis, rheumatoid arthritis (RA), plaque psoriasis and multiple sclerosis (MS). However, in Phase 2 clinical trials CI-201 failed to demonstrate a statistically significant reduction in vascular inflammation associated with atherosclerotic lesions over placebo. As a result, Vascular Biogenics discontinued the development of CI-201 in psoriasis and atherosclerosis. No information about rheumatoid arthritis and multiple sclerosis clinical trials are currently available.

Toloxychlorinol is a sedative agent. It is more pleasant alternative to chloral. Toloxychlorinol had low toxicity in the mouse, rat and guinea pig. Large doses of toloxychlorinol induced hypnosis rapidly. The duration of action was intermediate between that induced by moderate-, and long-acting barbiturates. Small doses, insufficient to cause outward signs of depression, significantly prolonged the period of sleep induced by hexobarbital. Toloxychlorinol antagonized convulsions induced by pentylenetetrazole. It displayed no analgesic activity. Pentylenetetrazole completely antagonized the effects of overdosage with toloxychlorinol.

Tolpyrramide is a sulfonamide derivative with antihyperglycemic properties. It was used as an oral antidiabetic drug.

Atrasentan (ABT-627, A-127722) is a selective endothelin A receptor antagonist. Atrasentan is being developed by AbbVie as an oral treatment for diabetic nephropathies.Abbott Laboratories was conducting clinical development of atrasentan for the treatment of certain cancers, including phase II trials for prostate cancer. However, no recent development has been reported for cancer indications and development is presumed to be discontinued.

FENISOREX is an anorexic agent.

Peradoxime is an antihypertensive agent. In normal animals, 37-48% of the radioactivity from an oral dose of labeled peradoxime or parenteral dose was excreted in the urine, and 48-50% in the feces. Biliary and urinary metabolites of peradoxime were principally found as conjugates with glucuronic acid.

Elpetrigine (GW293273 or JZP-4) is potent calcium and sodium channel blocker. In animal models, elpetrigine exerts anxiolytic, anticonvulsant, antidepressant and antimania effects. Jazz Pharmaceuticals is developing elpetrigine for the treatment of mood disorders and epilepsy.

Picoprazole is substituted benzimidazole. Picoprazole inhibited the gastric (H+ + K+)-ATPase in a concentration-and time-dependent manner, which may explain its inhibitory action on acid secretion in vitro and in vivo. This compound inhibits acid secretion at the level of the parietal cell by its ability to inhibit the gastric proton pump. Picoprazole affects pepsin secretion probably indirectly via its effect on the parietal cell. Studies on the (Na+ + K+)-ATPase indicated that this enzyme was unaffected by picoprazole.

IPROXAMINE is a peripheral vasodilator.