Serazapine (CGS15040) is an anxiolytic agent. It is structurally novel 5-HT2 receptor antagonist. Preliminary preclinical findings indicated an anticonflict effect in a behavioral suppression test, and two preliminary investigations in volunteers also suggested anxiolytic potential. In the first of these studies serazapine resembled diazepam, a reference anxiolytic drug, electroencephalographically. Additionally, in a test of psychogenic stress in volunteers it reduced cardiac output.

Tomelukast (previously known as LY171883), an orally active antagonist of the CysLT1 receptor (leukotriene D4), which was investigated to treat asthma, but this study was discontinued because of adverse gastrointestinal effect.

SPK-843 is a water-soluble partricin derivative patented by SPA Societa Prodotti Antibiotici S.p.A. and developed by Aparts and Kaken for the potential treatment of systemic fungal infections. In preclinical models, SPK-843 shows in vitro inhibitory activity comparable to or better than that of Amphotericin B against Candida spp., Cryptococcus neoformans, and Aspergillus spp. SPK-843 exhibits dose-dependent efficacy on murine pulmonary aspergillosis models. SPK-843 doses of higher than 1.0 mg/kg of body weight exhibit no renal toxicities and a tendency toward better survival prolongation than the estimated maximum tolerated doses of amphotericin B (Fungizone) and liposomal amphotericin B.

Tampramine (also known as AHR-9377) is a potent and selective, noncompetitive inhibitor of norepinephrine reuptake possesses antidepressant activity. This drug was studied for the treatment of the major depressive disorder; however, this study was discontinued.

Azepexole (or previously known as B-HT 933), a selective alpha 2-adrenoceptor agonist that was studied for the man with physiological tremor. It was shown that the drug produced sedation compared to placebo but not when compared to pre-treatment values. Some studies also have revealed the anti-tussive and antihypertensive properties of azepexole.

Tandamine was developed as a selective serotonin reuptake inhibitor for the treatment of depression. Tandamine participated in clinical trials in hospitalized depressed patients, where it showed that the well-tolerated drug could be of some benefit for retarded depressions. In addition, was found in human volunteers, that tandamine possessed significant anticholinergic activity, to reduce appetite and to produce sedation. However, this drug has never been marketed.

Dezaguanine is a broad spectrum guanine antimetabolite. This compound differs from guanine only in the substitution of a carbon for the 3-nitrogen of guanine. Dezaguanine must be converted to its nucleotides to be active. Dezaguanine nucleotides inhibit synthesis of guanine nucleotides, and can be incorporated into nucleic acids in place of guanine nucleotides; incorporation into DNA may be particularly important in the cytotoxicity of this compound. Addition of certain purines or purine nucleosides can prevent dezaguanine cytotoxicity in vitro. It has exhibited sufficient preclinical antitumor activity, particularly against rat and mouse mammary adenocarcinomas, slow and fast growing mammary tumors in mice and the human breast xenograft subrenal capsule implant system. It has completed one phase I trial.

Pridefine (AHR-1118) is a pyrrolidine derivative with clinically established antidepressant efficacy. Pridefine acted predominantly as a reuptake blocker of norepinephrine, dopamine, and 5-hydroxytryptamine, although some releasing activity was also present. Several clinical studies have demonstrated that pridefine is clinically as efficacious as imipramine and, perhaps more importantly, less toxic than standard antidepressants used.

Etoxadrol is an NMDA receptor antagonist. It exerts phencyclidine-like properties. Etoxadrol has anticonvulsant and anesthetic activity. Intravenous etoxadrol was clinically tested as an anesthetic.