Adoprazine (SVL-313) is a full 5-HT1A receptor agonist and full D2/3 receptor antagonist possessing characteristics of an atypical antipsychotic, representing a potential novel treatment for schizophrenia and bipolar disorder. This drug together with some others, e.g. Mazapertine succinate, PF-217830 was discontinued from clinical trials due to either non-optimal pharmacokinetic properties or insufficient therapeutical efficacy.

MK-0893, developed by Merck, is a reversible and competitive antagonist with high binding affinity (IC(50) of 6.6 nM) and functional cAMP activity (IC(50) of 15.7 nM). MK-0893 reached Phase 2; 12 weeks of once daily oral dosing led to significant and dose-dependent reductions in fasting and post-prandial plasma glucose and in HbA1c, with similar low incidences of hypoglycaemia as a metformin cohort. Combinations with metformin and sitagliptin were also trialled, and risk for hypoglycaemia was assessed in healthy males which showed the drug caused lengthening of recovery times. However, plasma levels of LDL cholesterol and liver transaminases were increased in some studies, as was body weight and blood pressure, all of which were not evident pre-clinically, and MK-0893 was discontinued.

Boehringer Ingelheim is developing BI-671800, an orally administered treatment for seasonal allergic rhinitis and asthma. BI-671800 is an antagonist of the PGD2 receptor, CRTH2. PGD2 stimulates bronchoconstriction and allergic airway inflammation in animal models. Inhibition of CRTH2 may reduce airway inflammatory cells, IL -4, -5, -13 production, serum IgE and airway hyper reactivity. Treatment with BI-671800 in poorly controlled asthmatic patients receiving FP was associated with a significant improvement in FEV1. BI-671800 was well tolerated at a total daily dose of 800 mg for 6 weeks.

Indopanolol is indole derivative patented by German pharmaceutical company Sandoz-Patent-G.m.b.H. as α- and β-adrenergic receptor blocking agent.

FEPRADINOL is an analgesic, antipyretic and anti-inflammatory agent. Its anti-inflammatory activity does not seem to be related to an inhibitory effect on prostaglandin biosynthesis.

Mesulergine, an antagonist of 5-HT2C, and dopamine receptors was studied in clinical trials for the treatment of Parkinson's disease. However, further, development was discontinued due to toxicological observations in animal experiments.

Almorexant (ACT-078573) is an orally active dual orexin receptor antagonist that is being developed by Actelion Ltd, in collaboration with GlaxoSmithKline plc, for the treatment of primary insomnia. Almorexant is a first-in-class compound that targets the orexin system, which plays a key role in wake promotion and stabilization; In January 2011, GlaxoSmithKline (GSK) and Actelion Ltd announced that clinical development of Phase III of almorexant has been discontinued. This decision follows a review of data from additional clinical studies, which were conducted to further establish the clinical profile of almorexant, including the tolerability profile.

Racemethorphan is racemic mixture of Dextromethorphan and Levomethorphan. Racemethorphan is listed under the Single Convention on Narcotic Drugs 1961 and is therefore listed in the United States as a Controlled Substance, specifically as a Narcotic in Schedule II. Dextromethorphan is a non-narcotic morphine derivative widely used as an antitussive. Dextromethorphan is a cough suppressant in many over-the-counter cold and cough medicines. In 2010, the FDA approved the combination product dextromethorphan/quinidine for the treatment of pseudobulbar affect. Dextromethorphan suppresses the cough reflex by a direct action on the cough center in the medulla of the brain. Levomethorphan is an opioid analgesic of the morphinan family that has never been marketed.

Monatepil is a calcium antagonist that, as do existing calcium antagonists, inhibits the influx of extracellular Ca 2 + through voltage-dependent Ca 2 + channels. It is a new type of antihypertensive agent. Its unique chemical structure was specially designed with intrinsic calcium antagonist and a1 -adrenoceptor-blocking moieties, creating a dual mechanism of action. Positive effects on plasma lipid metabolism are derived from the a1 -adrenoceptor-blocking activity and the antiatherosclerotic effect derives from the calcium antagonist properties. The novel structure of monatepil produces a slow onset of action and a long-lasting antihypertensive effect in experimental animals.

ABT-102 is a selective antagonist of transient receptor potential vanilloid type 1 (TRPV1), designed for the treatment of nociceptive pain. ABT-102 potently blocks multiple modes of TRPV1 receptor activation and effectively attenuates downstream consequences of receptor activity.