1α-HYDROXYVITAMIN D5 (CARD-024) is non-hypercalcemic, selective vitamin D receptor agonist under development for the treatment of cardiovascular disease, secondary hyperparathyroidism in chronic kidney disease and intestinal bowel disease fibrosis. CARD-024 attenuated the pro-fibrotic response of colonic myofibroblasts to high matrix stiffness, suggesting that it may ameliorate intestinal fibrosis.

Nesapidil is a vasodilator, it is used as an antiarrythmic and antihypertensive therapy.

Nitromiphene (NIT; CI 628) is a triarylethylene antiestrogen shown to be effective in treatment of experimental breast cancer. Nitromiphene is one of the earliest nonsteroidal selective estrogen receptor modulators (SERMs). It is an anti-estrogen capable to translocate the estrogen receptor to the nucleus and to induce the replenishment of the cytosol receptor. Nitromiphene inhibited the uptake of [3H]-estradiol in rat whole homogenates and isolated cell nuclei tissues and the pituitary, and inhibited estradiol-induced female sexual behavior. Nitromiphene has thus been shown to suppress the growth of chemically induced and ransplantedmammary tumors in rodents. Also, Nitromiphene was shown to have potent, prolonged antiuterotropic effects in immature rats. Nitromiphene has been shown to undergo conversion to demethyl Nitromiphene (CI628M), a phenolic metabolite which had greater affinity for estrogen receptors and greater biological potency in vitro than did Nitromiphene. However, the in vivo antiestrogenic effects of Nitromiphene and demethyl Nitromiphene were similar, possibly due to facile O-demethylation of the former compound after administration.

Paranyline was used in dispersible formulations of anti-inflammatory agents. Information about the current use of this drug is not available.

FLUCIPRAZINE is an antitussive, antiemetic, neuroleptic agent.

Cinfenoac is a chalcone derivative patented by a pharmaceutical company Biorex Laboratories from the UK. The compound is claimed for the treatment of inflammatory and allergic conditions, as well as for the treatment of the ulcerous condition of the gastrointestinal tract.

Cinepaxadil is cinnamoyl-piperazine derivative developed by Delalande SA for treatment cardiovascular system disorders. Cinepaxadil decrease dogs cardiac activity after i.v. administration.

Amiflamine is a selective and reversible inhibitor of monoamine oxidase (MAO) type A which exerts a preferential effect on serotonin (5-HT) catabolism. The (+)-enantiomer is the active stereoisomer. In a series of p-aminosubstituted phenethylamines, the ( + )-enantiomer of the compound amiflamine (4-dimethylamino-2-a-dimethylphenethylamine) was found to be a potent, selective, and reversible MAO type A inhibitor. Amiflamine (FLA 336(+] and its two metabolites, FLA 788(+) and FLA 668(+) were found to be competitive inhibitors of the activity of monoamine oxidase-A in homogenates of human hypothalamus and liver obtained at autopsy. Ki values, determined at pH 7.2, were 1.3, 0.3 and 22 uM (liver) and 0.8, 0.2 and 14 uM (hypothalamus) for amiflamine, FLA 788(+) and FLA 668(+), respectively. Monoamine oxidase-B activity was only weakly inhibited by the compounds. This initial phase I study in six normal subjects showed that the new MAO inhibitor amiflamine can be tolerated in single oral doses up to 80 mg without significant pharmacologic effects. Doses up to 60 mg were tolerated without any subjective or objective effects.

Nitralamine is an antifungal agent.

Octasine is an antihistamine agent that has never been marketed.