Doxpicomine is the hydrochloride salt of l-3[(dimethylamino)-(m-dioxan-5-yl)methyl]pyridine, a derivative of substituted 1,3 dioxanes. Its analgesic effect appears to be mediated centrally through opiate-like receptors. Preclinical animal studies revealed analgesic activity and duration of action of the same order as that of meperidine and codeine when administered subcutaneously and of codeine but of shorter duration when administered orally. The analgesic effects were reversed by naloxone. The drug did not reduce or antagonize the analgesic effect of morphine. Drowsiness is an expected response to effective analgesics. It was the foremost side effect observed but was of short duration and minimal intensity and did not interfere with the postoperative regimen of coughing, deep breathing, and early ambulation. Nausea and vomiting were not reported after doxpicomine.

FLUMEXADOL is a non-opioid analgesic. Its prodrug OXAFLOZANE was used as an antidepressant in France till 2004.

Espatropate (UK 88060) is an antagonist of M3 muscarinic receptors. Espatropate is a bronchodilator with anticholinergic activity. It was undergoing preclinical development with Pfizer for the treatment of asthma.

Fenabutene controls pituitary activity.

Acebrochol is a neuroactive steroid that may act as a sedative and hypnotic, through the mechanism of altering ligand-gated ion channels and cell surface receptors.

Nitraquazone (TVX 2706) is an phosphodiesterase inhibitor with antiinflammatory action. It strongly enhances the increase in intracellular levels of cyclic AMP caused by appropriate effectors in all systems tested so far. EC50 values are in the submicromolar range. The effect is apparently neither due to an increased responsiveness of the hybrid cells for an effector like prostaglandin E1 nor to an increased activity of adenylate cyclase, but to an inhibition of both low and high affinity cyclic AMP phosphodiesterases. Half-maximal inhibition of enzyme activity is obtained at 10 uM TVX 2706. TVX 2706 does not interfere with the calmodulin activation of phosphodiesterase. Nitraquazone affected cytokine production by PHA-stimulated human blood cells. Nitraquazone was active in reducing the production of IL-5 (IC50 = 0.8 uM), while its potency against IL-2, GM-CSF and IFN-gamma was 3-6 times lower.

In the early stages of testing was shown that it is about 4 times more potent than gallopamil and 12 times more potent than verapamil in its effects on smooth muscle tone and labeled calcium uptake.

Divabuterol or terbutaline dipivalate is a prodrug of terbutaline. The half-life of terbutaline dipivalate in human plasma is less than five minutes. Therapeutically, most forms of terbutaline can be used as bronchodilators in antiasthmatic treatment, as smooth muscle relaxants to treat premature labour (uterine relaxant) and for a number of other indications.

Rifamexil (also known as MDL 62769 or P/DEA) is a derivative of rifamycin (a natural antibiotic produced by Amycolatopsis rifamycinica). This drug has greater intrinsic activity against Myobacterium avium (MAC) than rifampin. Information on current use of this compound is not available.