Trodusquemine (MSI-1436) is a "first-in-class" highly selective non-competitive, allosteric inhibitor of PTP1B that can cross the blood-brain barrier to suppress feeding and promote insulin sensitivity and glycemic control. Trodusquemine is a naturally occurring cholestane that can be purified from the liver of the dogfish shark, Squalus acanthias, but it can also be manufactured synthetically by a fairly laborious process that requires several weeks. Trodusquemine has potential hypoglycemic, anti-diabetic, anti-obesity, and antineoplastic activities. Upon administration, trodusquemine selectively targets and inhibits PTP1B, thereby preventing PTP1B-mediated signaling. This prevents the dephosphorylation of the insulin receptor, which improves insulin signaling and insulin sensitivity, and decreases blood glucose levels. In susceptible cancer cells, inhibition of PTP1B causes a reduction of tumor cell proliferation.

Darotropium is a muscarinic acetylcholine antagonist, developed by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease (COPD). Darotropium in combination with salmeterol was investigated in phase 2 clinical trial in COPD patients. The addition of darotropium to salmeterol in partially reversible COPD patients resulted in greater bronchodilation than salmeterol or tiotropium alone and was well tolerated. In a clinical trial of darotropium as monotherapy, all doses of the drug were well tolerated and demonstrated bronchodilatory activity. However, the rapid onset of bronchodilation was not sustained over 24 h, and GSK has discontinued the development of darotropium in favor of GSK573719, which has more favorable pharmacokinetics.

Cyacetacide is a biochemical used in the past as an anti-tuberculosis agent and currently used in Russia to for the treatment of various forms of tubercular lesions of the eye: keratitis, scleritis, uveitis, chorioretinitis, tuberculosis-allergic diseases and eye diseases of non-tubercular origin. Cyacetacide has also been used to derive compounds that may have antitumor properties.

Denpidazone is a 1,2-diphenylpyridazine-3,6-dione derivative. It is listed as a muscle relaxant.

Ecipramidil is a peripheral and cerebral vasodilator.

Eganoprost is a prostaglandin derivative.

Diethazine is the antimuscarinic agent. It has actions similar to those of ethopropazine but it is more toxic. Diethazine is used for the palliative treatment of the parkinsonian syndrome. It is more useful in the treatment of Parkinson’s disease than in allergies. Blockade of single contractions observed in these experiments after administration of diethazine was independent of the frequency of stimulation of the nerve. This suggests that the drug acts directly on the postsynaptic receptor in the endplate.

Omocianine was developed as an enhancer of fluorescence optical mammography allowed better detection of more superficially located lesions. It was shown that the lowest doses of omocianine performed best in lesion detection. Diffuse optical tomography using a low-dose fluorescent agent is feasible and safe for breast cancer visualization in patients. This compound participated in phase I clinical trials in Germany and in the Netherlands, however, these studies were discontinued.

Paliroden is an orally active drug that activates the synthesis of endogenous neurotrophins or nerve growth factors. Paliroden was investigated in phase II clinical trial in patients with Alzheimer's disease and to evaluate its effect on 18F-Dopa PET imaging in patients with Parkinson's disease. The further development of paliroden was discontinued due to its insufficient efficacy.