Moxiraprine (also known as CM-30366) is aminopyridazine derivative with antidepressant activity. In preclinical studies Moxiraprine induced stereotyped behaviour and antagonized haloperidol-induced catalepsy in rats, after parenteral and oral administration. In 6-hydroxy dopamine (6-OHDA)-lesioned mice, Moxiraprine induced contralateral rotations and, when injected before 6-OHDA, protected mice against its neurotoxicity. Moxiraprine also provoked contralateral rotations when injected directly into the mouse right striatum. After parenteral injection, Moxiraprine slightly increased motility in mice, at least at low doses. The stereotypies and rotations (after intrastriatal injection) induced by Moxiraprine were antagonized by haloperidol, alpha-methyl-p-tyrosine and reserpine. The effects of Moxiraprine were compared to those of direct and indirect dopamine-like drugs. Bromocriptine induced a behavioural profile, which in most aspects, was qualitatively and quantitatively similar to that of Moxiraprine. Apomorphine was found slightly more potent than Moxiraprine, but in contrast to the latter, apomorphine-induced stereotypies were insensitive to alpha-methyl-p-tyrosine or reserpine. (+)-Amphetamine and nomifensine were less potent than Moxiraprine, and unlike Moxiraprine, induced ipsilateral rotations in 6-OHDA-lesioned mice.

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.

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.

Sulamserod is a methanesulfonamide derivative patented by British multinational pharmaceutical company GlaxoSmithKline as 5-HT4 receptor antagonist, with antiarrhythmic activities for the treatment of the certain cardiovascular condition. 5-HT4 receptor blockade could have antiarrhythmic effects by decreasing intracellular Ca2+ concentration and delayed rectifier potassium current and prolonging atrial refractory period. In preclinical models, Sulamserod prolongs mean atrial effective refractory period and wavelength, reduces the dispersion of effective refractory period, and minimally slows conduction velocity in pigs.

Felipyrine is a 1-aryl-2-pyrrolidinone derivative exerting anti-inflammatory activity.

Phencarbamide is an anti-spasmodic and anticholinergic drug used during parturition. It has a specific antispasmodic action on the smooth muscle, both directly like papaverine and through the autonomic nervous system (atropine effect). It has also an analgesic effect of its own. Side-effects generally associated with the atropine group of drugs.

Telcagepant (MK-0974) is a calcitonin gene-related peptide receptor antagonist. Merck & Co was developing telcagepant for the treatment of pain. Telcagepant is an extremely potent CGRP antagonist with a Ki = 0.77 (0.07 nM). Telcagepant showed efficacy against acute migraines; however, different patient populations may show more beneficial effects with telcagepant versus triptans. In the acute treatment of migraine, Telcagepant was found to have equal potency to rizatriptan and zolmitriptan in two Phase III clinical trials. Merck & Co has now terminated development of the drug.

Serlopitant, Originally developed by Merck, is a once-daily oral NK1 receptor antagonist being developed for the treatment of pruritus, or itch, associated with various conditions such as prurigo nodularis, psoriasis and chronic pruritus of unknown origin. It is highly selective for the human NK1 receptor and in both animal and human testing it has been well tolerated. In 2012, Merck licensed serlopitant to Menlo to develop it in indications other than nausea and vomiting. Development of serlopitant for the treatment of overactive bladder, alcohol dependence and pruritus was discontinued at phase II, by Merck & Co. and Japan. Menlo has completed three positive Phase 2 clinical trials with serlopitant showing a statistically significant reduction in pruritus compared to placebo. Serlopitant has been evaluated in over 1,600 patients and has been shown to be well-tolerated, including in patients who have received treatment for up to one year. Serlopitant is an investigational drug that is not currently approved for use in any indication in any country.