Pranolium (UM-272) is propranolol derivative. It can reduce the extent of myocardial injury sustained during severe ischemia. UM-272 lacks significant beta-adrenergic blocking activity but retains the negative chronotropic, negative inotropic and antiarrhythmic effects common to both d- and l-propranolol. The protective effects of UM-272 during myocardial ischemia cannot be due to metabolic effects of the beta-adrenergic blockade but may be due to effects on oxygen consumption or to effects on myocardial membrane properties that are related to its antiarrhythmic and myocardial depressant activity. The ability of UM-272 to enhance blood flow to subendocardial myocardium may also play a role in its beneficial effects during ischemia. UM-272 may protect the ischemic heart through direct effects on myocardial Ca++ regulating mechanisms. UM-272 has kinetically similar use-dependent inhibitory action of the fast sodium channels of cardiac muscles as other Class Ia antiarrhythmic drugs like quinidine or procainamide. Pranolium was investigated as an antiarrhythmic agent.

Entospletinib (GS-9973) is an adenosine triphosphate competitive inhibitor of Syk that disrupts kinase activity, which is currently in clinical trials for multiple B-cell malignancies. The most common treatment-emergent serious adverse events included dyspnea, pneumonia, febrile neutropenia, dehydration, and pyrexia.

N-(4-[(1-(Dimethylamino)-ethylidene)-amino]-phenyl)-2 methoxyacetamide hydrochloride (amidantel, BAY d 8815) is an aminophenylamidine with an interesting anthelminthic spectrum. In rodents the compound is active against nematodes, filariae and cestodes. Of special interest is the high efficacy in dogs against hookworms and large roundworms. Amidantel was well tolerated by all animals tested and did not show teratogenic effects. The drug was moderately potent inhibitor of both E. electricus and C. elegans acetylcholinesterase but at concentrations too high to account for its abilitiy to contract cut worms. The primary mode of action of amidantel appears to be as agonist at the level of the acetylcholine receptor, a view supported by the observation that its effect may be blocked by the nicotinic antagonists d-tubocurarine and gallamine. Amidantel was also investigated it clinical trials as the treatment against Ancylostoma duodenale infection. Amidantel proved to be very effective against A. duodenale as well as Ascaris lumbricoides. With regard to dosage, a single dose of 6.0 mg/kg body weight of amidantel was found to be the most effective and well tolerated than the other dosages employed.

4,4’-Diamino-2,2’-stilbenedisulfonic acid (also known as amsonic acid) is used in the synthesis of dyes and optical brighteners or fluorescent whitening agents. Amsonic acid possesses estrogenic activity, and thus provided a possible mechanistic explanation for the complaints of impotency in factory workers exposed to this compound. In the 2-year feed studies on rodents, there was no evidence of carcinogenic activity of amsonic acid, in male or female F344/N rats receiving 12,500 or 25,000 ppm. In addition, there was no evidence of carcinogenic activity of this compound in male or female B6C3F1 mice receiving 6,250 or 12,500 ppm.

Nicofibrate is an antilipidemic drug. Treatment of diabetics led to a significant reduction in plasma cholesterol and triglycerides and brought the lipoprotein picture back within the norm. Nicofibrate did not lead to significant increases in uricaemia nor to any worsening in carbohydrate tolerance. Nicofibrate may also lead to a significant drop in plasma prothrombinic activity.

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.

N-Gene Research Laboratories is developing BGP-15 (NP-51), a small molecule, orally available, indirect Jun kinase (JNK) inhibitor and insulin sensitiser, for glycaemic control in patients with type-2 diabetes mellitus, and as an adjunct treatment for insulin resistance due to antipsychotics or obesity. In March 2002, N-Gene Research Laboratories granted Allos Therapeutics an exclusive license to its intellectual property surrounding BGP 15 in the US. BGP-15 has previously been used in clinical trials for the treatment of skeletal muscle pathology associated with Type 2 Diabetes (through insulin sensitization), Duchenne Muscular Dystrophy (DMD) and heart failure (through anti-inflammatory and anti-fibrotic mechanisms). Via its action as a modulator of the cytoprotective response to cellularstress, and specifically as a poly (ADP-ribose) polymerase (PARP) inhibitor, heat shock protein-inducer, membrane lipid therapeutic and an antioxidant inducer, BGP-15 has previously been shown to protect against skeletal muscle dysfunction, damage and wasting.