Swainsonine is an indolizidine alkaloid found in Australian Swainsona canescens, North American plants of the genera Astragalus and Oxytropis and also in the fungus Rhizoctonia leguminocola. It is competitive inhibitor of Golgi alpha-mannosidase II and lysosomal alpha-mannosidases. This compound has been reported to be a potent antiproliferative and immunomodulatory agent. However, no evidence of anti-tumor activity of swainsonine was seen in phase II clinical trial, in patients with locally advanced or metastatic renal cell carcinoma. Adverse events such as fatigue, nausea and diarrhea were common but generally mild. Swainsonine is locoweed toxin. Locoweed poisoning is seen throughout the world and annually costs the livestock industry millions of dollars. Swainsonine inhibits lysosomal alpha-mannosidase and Golgi mannosidase II. Poisoned animals are lethargic, anorexic, emaciated, and have neurologic signs that range from subtle apprehension to seizures.

Nisterime is a dihydrotestosterone derivative. Nisterime acetate (ORF-9326) was shown to inhibit implantation in several species. It is also interrupts the postimplantation stage of gestation.

Nafimidone is a candidate anticonvulsant agent. The anticonvulsant effectiveness of nafimidone was evaluated in the kindled amygdaloid seizure model in rats. Nafimidone (25-50 mg/kg) significantly reduced supranthreshold elicited afterdischarge length and seizure severity only at doses with some prestimulation toxicity. The maximum anticonvulsant effectiveness for the 25 mg/kg i.p. dose of nafimidone was seen between 15 and 30 min utilizing a suprathreshold kindling paradigm. Nafimidone did not significantly elevate seizure thresholds at the doses tested; however, nafimidone (3.1-50 mg/kg) reduced the severity and afterdischarge duration of threshold elicited seizures in a non-dose response manner. Nafimidone is a new antiepileptic drug which may be effective in partial onset seizures in humans.

Mirfentanil was developed as CNS analgesic with a short duration of action. It induced antinociception predominately through mu opioid receptors. It was shown that at doses larger than those, which exert opioid effects, mirfentanil had nonopioid analgesic effects. The drug was successfully encapsulated in liposomes having a variety of compositions. The lipid composition of the formulation was varied to optimize the stabilization of liposomes and the encapsulation of solutes. Mirfentanil participated in phase II clinical trials for the treatment of pain. However, this study was discontinued.

Modaline is piperidinopyrazine derivative developed by Warner-Lambert Pharmaceutical Co. as Antidepressant. Modaline is a potent monoamine oxidase (MAO) inhibitor of the order of the more effective hydrazines. Pretreatment with harmaline, a reversible MAO inhibitor, or with serotonin prevented the irreversible inhibition by Modaline, suggesting that Modaline (as an active MAO inhibitor) occupies the same site on MAO as harmaline, the hydrazines, or serotonin. Modaline differs from the monoamine oxidase inhibitors by producing an increase in body temperature in fully reserpinized animals. Modaline differs from imipramine‐like drugs in not potentiating the hyperthermic effect of isoprenaline.

Metergotamine (MY-25 or 1-methyl-ergotamine-bitartrate) is a derivative of ergotamine and belongs to peptide alkaloids. It exerts a dampening effect on vessels, in that relaxation is brought about in contracted vessels, whereas contraction is brought in dilated vessels. Metergotamine was being studied in migraine prophylaxis.

Miboplatin (DWA 2114R) is a platinum analog developed for the treatment of cancer. Miboplatin is an alkylating agent that reached phase III clinical trials in Japan. In spite of its good anticancer activity, the drug did not show any advantage over cisplatin. Further development of this drug for the treatment of breast, ovarian and prostate cancer was discontinued.

Losulazine (U-54,669F) is an antihypertensive agent acting by a sympatholytic mechanism. It appears to alter peripheral sympathetic neurogenic function but apparently does not enter the central nervous system. Losulazine effectively lowered the blood pressure in patients with hypertension.

Dexclamol is a sedative agent. It was found to potentiate the anesthetic actions of halothane. In potentiating the effects of halothane, dexclamol behaved both qualitatively and quantitatively in a manner similar to droperidol. Dexclamol, however, was approximately 37 times less potent than droperidol in antagonizing the vasopressor effects of epinephrine. The neuroleptic agent (+)-dexclamol, but not (-)-dexclamol, affects central dopamine (DA) and norepinephrine (NE) turnover and indicates a stereochemical specificity with respect to antagonism of central DA and NE receptors. Dexclamol was as effective as droperidol at the same dose in inducing neurolepsy and in supplementing nitrous oxide anaesthesia. Changes in heart rate, respiratory rate and rectal temperature in the animals treated with dexclamol were not different from those observed in the animals treated with droperidol.