Trioxifene (LY133314) is a selective estrogen receptor modulator (SERM) with competitive binding activity against estradiol for estrogen receptor alpha (ERalpha) and antagonistic activity against ERalpha-mediated gene expression. Trioxifene has demonstrated activity in dimethyl-benzanthracene-induced mammary carcinoma in rats and human breast cancer patients. Trioxifene mesylate, an antiestrogen with a high FR affinity, was developed with the hope of improving the response rate of ER-positive patients, especially those with a borderline concentration of ER in their tumors. When used in vitro and in vivo, trioxifene has been shown to bind to the estradiol receptors with a binding affinity exceeding that of estradiol by a factor 1.7, whereas tamoxifen has a relative affinity of only 0.18 compared with trioxifene.

Tiodazosin is a newly developed antihypertensive agent, structurally related to prazosin. Prazosin and tiodazosin administrated intravenously to anesthetized rats, are equally effective hypotensive agents, but that the hypotensive potency of prazosin is greater than that of tiodazosin. However, chronic administration of equivalent doses of the two compounds for 25 and 52 days via the drinking water indicated approximately equivalent, sustained reductions in blood pressure. Furthermore, at the end of the 52-day chronic dosing period tiodazosin caused appreciably less alpha-adrenergic receptor antagonist activity than prazosin as assessed by the norepinephrine dose-pressor response profiles.

Drobuline is a potent cardiac depressant (anti-arrhythmic) agent, which has been found to be effective against ventricular arrhythmias in dogs. This compound is a racemic mixture having a single center of optical activity. The two isomers of drobuline were found to be equally potent in converting cardiac arrhythmias in dogs after intravenous administration. The major route of biotransformation of drobuline in the dog was shown to be conjugation with glucuronic acid.

Cyclophenazine is an antagonist of dopamine receptors, discovered by Eli Lilly. The drug is claimed to possess tranquilizing, anti-emetic action, and is able to potentiate the action of anticholinergic compounds in inhibiting the gastric secretion.

Tepirindole (also known as HR-592), an indole derivative has a high affinity for DA, 5-HT and NE receptors but has little properties to cause catalepsy. Animal experiments have shown that this compound could alleviate the adverse effect of neuroleptics such as haloperidol. Information about the current development of tepirindole is not available.

Ristianol (Ristianol phosphate) is a bioactive chemical that is registered as an anti-inflammatory agent and immunoregulator (in Europe), but no further information is available.

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.

Phenampromide is an opioid analgesic, which is considered to be structurally similar to isomethadone. Phenampromide belongs to the ampromide family of drugs, which also include propiram and diampromide. According to the literature, (R)-phenampromide has greater analgesic potency than its (S)-enantiomer. Synthetic narcotic analgesic phenampromide is under international control according to the UN Single Convention 1961 and its amendments, Schedule I.

Setazindol is an anorectic.

Pelrinone, a cardiotonic drug, is a phosphodiesterase III inhibitor that was studied in clinical trials phase II for the treatment of patients with heart failure.