Thiorphan is the first potent synthetic inhibitor of enkephalinase. Thiorphan displays antinociceptive activity after systemic administration. Thiorphan also inhibits to a lesser extent the widely distributed angiotensin-converting enzyme, a carboxydipeptidase implicated in blood pressure regulation. Thiorphan failed to potentiate allergen-induced airway responses in asthma. Thiorphan significantly reduced the castor oil-induced diarrhea in rats when administered intravenously but not when administered intracerebroventricularly. Racecadotril, via its active metabolite thiorphan, was consistently effective in animal models and patients with various forms of acute diarrhea by inhibiting pathologic (but not basal) secretion from the gut without changing gastro-intestinal transit time or motility.

Dioxethedrin is the ephedrine derivative. It is the beta-adrenergic agonist. As a bronchodilator and sympathomimetic agent is was used in antitussive syrup Bexol.

Bentiamine (also known as dibenzoyl thiamine), a derivative of thiamine, is rapidly absorbed and converted to thiamine. Experiments on rodent have shown that this compound had low toxicity and absence of carcinogenicity.

Dexpemedolac is long-acting non-narcotic analgesic. Dexpemedolac exhibited potent analgesic effects against chemically induced pain in rats and mice and against inflammatory pain in rats. Dexpemedolac differed from standard nonsteroidal anti-inflammatory drugs (NSAIDs) in that the doses, which produced analgesia were much lower than those required for either anti-inflammatory or gastric irritant effects. The common to the NCAIDs class actions are antipyresis and inhibitory effects on platelet aggregation. In yeast-induced hyperthermic rats, dexpemedolac exhibited antipyretic actions, whereas the drug did not affect body temperature in normothermic animals. Aggregation of human platelets was inhibited by high concentrations of dexpemedolac.

Oxadimedine, an antihistamine that was developed as a local anesthetic. Information about the current use of this compound is not available.

Nifenalol is the beta-receptor antagonist. It has optical isomers. The racemic mixture and the levo-isomer are active in antagonizing beta-receptors, but the dextro-isomer is inactive. The levo-isomer seems to be about twice as active in blocking beta-receptors as the racemate. Nifenalol is virtually devoid of local anesthetic properties in contrast to procaine, propranolol, and butidrine. Nifenalol exacerbated the fighting behavior in male mice by foot-shock. Nifenalol has been studied in patients with coronary artery disease. It afforded the coronary patient good protection against angina and ischemic changes in the EKG. It was further noted that nifenalol had no antiarrhythmic action and that it was devoid of evident side effects. Nifenalol possessed weak action against tremorine and oxotremorine induced tremor.

Norbudrine (KWD2109) is a sympathomimetic drug. It is an active bronchospasmolytic agent. KWD2109 shows an in vitro bronchospasmolytic acitivity which is about 14 times better than that of KWD2025. In the in vivo tests or guinea pig bronchospasmolytic activity KWD2109 has an effect which is about 3 times that of KWD2025 after intraperitoneal and oral administration

Pimetine has been reported to be an antiatherogenic agent of particular interest since its activities are unrelated to blood cholesterol levels. Pimetine hydrochloride (IN 379) alters the production and utilization of acid mucopolysaeeharides and may block the formation of atherosclerotic plaque. The initial clinical evaluation of pimetine in neuropsychiatric disorders was performed in hospitalized patients with the diagnosis of "chronic brain syndrome". Behavioral effects of pimetine were increased alertness, interest and sociability with improvement in organization of thought processes. In patients suffering from chronic organic diseases, pimetine was reported to produce a feeling of "more energy", a general feeling of "well being" and mild insomnia was reported as a non-limiting side effect. Pimetine was found to be a less active stimulant than amphetamine.

Benzetimide, a muscarinic acetylcholine receptor antagonist that was investigated as an antiparkinson-agent and was studied in the treatment of diarrheas of cattle and calves. Benzetimide is an enantiomer of dexetimide that has been used to treat neuroleptic-induced Parkinsonism.

Ezatiostat (TLK199) [γ-glutamyl-S-(benzyl)cysteinyl-R-phenyl glycine diethyl ester] is an inhibitor of Glutathione S-transferase P1–1 (GSTπ). The drug is a peptidomimetic of GSH (glutathione), esterified to enhance cellular uptake and designed to bind to the “G-site” of GSTP1–1. Independent of catalysis inhibition, TLK199 also disrupts the protein:protein interaction site(s) between GSTP1–1 and JNK1. Telik Inc was developing TLK-199 for the potential prevention of myelosuppression in blood diseases, namely myelodysplastic syndrome.