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.

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.

FLORBENAZINE F-18 is a fluorinated vesicular monoamine transporter type 2 (VMAT-2) ligand for positron-emission tomography. It has completed Phase II/III as a commercial radiopharmaceutical for the early detection and monitoring of neurodegenerative diseases including Parkinson's disease, Alzheimer's disease, and dementia with Lewy bodies.

Demoxepam is a major pharmacologically active metabolite of the benzodiazepine chlordiazepoxide, the first drug within the class to gain approval by the Food and Drug Administration for use as an anticonvulsant, muscle relaxant and sedative hypnotic. Demoxepam has been shown to have antianxiety activity in man. The eventual elimination of demoxepam from the plasma was slow, with a range in half-life of 14-95 hr. The half-life of demoxepam was markedly longer than that of chlordiazepoxide. Demoxepam has an inhibitory effect on in vitro [3H]tryptophan binding to rat hepatic nuclei.

Dieldrin is an organochlorine pesticide belonging to the class of substances which are known to have a toxic effect on various physiological systems of the human body. Despite an imposed ban on their manufacture and commercial use, these pesticides can still be detected in high probability areas of consumption such as agriculture land. Dieldrin has been epidemiologically associated with an increased risk for Parkinson's disease (PD). Early studies identifying dieldrin as an antiandrogen estrogen mimetic have been contradicted by more recent studies which do not show any estrogenic activity.

Tetrazolast (also known as MDL 26,024GO) is a tetrazoloquinoline derivative patented by Merrell Dow Pharmaceuticals, Inc. as an antiallergic and antiasthmatic agent. Tetrazolast was shown to be an orally absorbed mediator release inhibitor in the rat passive cutaneous anaphylaxis and passive peritoneal anaphylaxis tests. In addition, the compound was shown to both elicit and inhibit elicitation of the Bezold-Jarisch reflex in the dog. Tetrazolast also significantly reduced Ascaris-induced changes in pulmonary mechanics in cynomolgus monkeys. The compound inhibited both early and late phase antigen induced-changes in Ascaris-sensitive sheep, as well as the increased airway hyperreactivity which normally follows antigen challenge.

Pepstatin is a pentapeptide of microbial origin. The peptide inhibits the acid proteases pepsin and cathepsin D and the pressor enzyme renin. Pepstatin was shown to provide long-lasting inhibition (3 to 6 days) of cathepsin D in vivo in non-tumor bearers particularly in spleen, liver, kidney, lung, and heart. Pepstatin may prove useful as "anticachexia" agent by decreasing proteolysis in muscle and other tissues. The in vivo pepstatin and IL-2 treatment decreased the T-cells and increased the natural killer-like LAK precursor cells, possibly also with an increase in its activity, which were further induced by in vitro IL-2 culture to generate an augmented LAK cell activity. This suggests the clinical potential of pepstatin in IL-2-related immunotherapy. In rats injected centrally with the specific cathepsin D inhibitor, pepstatin, the protease activity was inhibited up to 90% in most brain regions.

Trefentanil is a short-acting synthetic opioid of the piperidine class. The drug caused potent analgesia with the peak effect occurring 3 min after injection. There was no significant difference in analgesic potency of trefentanil and alfentanil as measured by tolerance to tibial pressure at 3 min. Trefentanil had a pharmacokinetic and pharmacodynamic profile similar to alfentanil, with a small extent of tissue distribution and a rapid blood/brain equilibration. Trefentanil caused significant respiratory depression at doses of 32 ug/kg and 64 ug/kg. It is a mu-opioid receptor agonist. Trefentanil produced naloxone reversible anti-nociception equi-efficacious to that of fentanyl.