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.

Detajmium bitartrate anhydrous is Rauwolfia alkaloid. It is a sodium-channel-blocking drug with an extremely long recovery from use-dependent sodium channel block. Detajmium has antiarrhythmic properties. It caused comparable prolongations of the intraventricular conduction time during sinus rhythm and progressively broadened the QRS complex. Rauwolfia alkaloids use is restricted by serious adverse effects, such as dysrhytmias. Several detajmium bitartrate lethal intoxications were reported.

Cyprolidol is a pyridylcyclopropane derivative, developed by Neisler Laboratories. In animal models, cyprolidol produced an antidepressant effect qualitatively similar to those produced by imipramine. The compound blocked the tyramine-induced rise in blood pressure only in anesthetized dogs but potentiated it in conscious dogs. In man, cyprolidol was less effective than imipramine.

Mergocriptine (2-methyl-a-ergocryptine or CBM36-733) is a synthetic long-acting ergot derivative. It exerts agonistic action at dopamine receptors. Mergocryptine may induce the suppression of striatal dopamine turnover by reducing dopamine release via the stimulation of presynaptic dopaminergic autoreceptors. In animal experiments, it may affect cerebral hemodynamics. Mergocriptine has a protective effect on the brain against ischemia.

Tosifen was synthesized originally in a series of compounds whose basic structural moiety, the sulfonyl urea nucleus, was of interest for potential hypoglycemic action. But tosifen is only a weak hypoglycemic agent. It is a potential antianginal and antiarrhythmic agent. The duration of action of tosifen was considerably longer than nitroglycerin and its lack of side effects considerably greater than propranolol. No long-term harmful effects have been observed during 13-week toxicity studies in animals. Tosifen differed from standard antianginal agents which may act via beta-adrenergic blocking activity or alteration of cardiac or circulatory dynamics since no acute pharmacological changes were observed after tosifen was administered. Tosifen was readily absorbed in both rats and dogs. The rates of absorption, metabolism, and urinary excretion were higher in the rat than in the dog.

LEVOFENFLURAMINE is a levorotatory enantiomer of fenfluramine, a substituted amphetamine which was formerly used to treat obesity. LEVOFENFLURAMINE has dopamine-antagonistic properties and, at high doses, increases dopamine concentrations in rat striatal dialysates. It is essentially inactive to reduce food intake in human subjects.

Coleneuramide (MCC-257) is a cholestane amide conjugate originated in Mitsubishi Pharma Corporation. It has been shown to enhance the effect of nerve growth factor (NGF) on cell survival and on tyrosine phosphorylation in PC12 cells. Coleneuramide is believed to act directly on TrkA receptor. In preclinical models, MCC-257 rescued clinical sign and pathological changes in rats after exposure to environmental neurotoxin methylmercury and protected against dysfunction of the peripheral nervers in hyperglycemic animals. The compound was investigated in phase 2 clinical study for the treatment of diabetic polyneuropathy, but no results were reported.

Anisodamine is a naturally occurring atropine derivative that has been isolated, synthesized and characterized by scientists in the People's Republic of China. Anisodamine is a non-specific cholinergic antagonist. Anisodamine has been shown to interact with and disrupt liposome structure which may reflect its effects on cellular membranes. Experimental evidence implicates anisodamine as an anti-oxidant that may protect against free radical-induced cellular damage. Its cardiovascular properties include depression of cardiac conduction and the ability to protect against arrhythmia induced by various agents. Anisodamine is a relatively weak alpha(1) adrenergic antagonist which may explain its vasodilating activity. Its anti-thrombotic activity may be a result of inhibition of thromboxane synthesis. Numerous therapeutic uses of anisodamine have been proposed including treatment of septic shock, various circulatory disorders, organophosphorus (OP) poisoning, migraine, gastric ulcers, gastrointestinal colic, acute glomerular nephritis, eclampsia, respiratory diseases, rheumatoid arthritis, obstructive jaundice, opiate addiction, snake bite and radiation damage protection. The primary therapeutic use of anisodamine has been for the treatment of septic shock. Several mechanisms have been proposed to explain its beneficial effect though most mechanisms are based upon the assumption that anisodamine ultimately acts by an improvement of blood flow in the microcirculation. Preliminary studies suggest another important therapeutic use of anisodamine is for the treatment of OP poisoning. Anisodamine has been employed therapeutically since 1965 in the People’s Republic of China primarily to improve blood flow in circulatory disorders such as septic shock, disseminated intravascular coagulation (DIC) and as an antidote to organophosphate poisoning.

Mideplanin (MDL 62873), a teicoplanin amide derivative, was studied as an antibacterial agent against Gram-positive bacteria. However, further, development appears to have been discontinued.

Vinleurosine is a vinca alkaloid found in species of Catharanthus. This compound was studied as an anticancer agent and participated in clinical trials. However, the drug was more toxic and unpredictable in effect in comparison with vinblastine. Its further development was discontinued.