Lesogaberan is a peripherally restricted high-affinity GABAB-R-specific agonist, originally developed for the treatment of gastroesophageal reflux disease (GERD) that appears to be safe for human use. The toxicity profile shows no indication of hepatic effect. Lesogaberan has been shown to induce decreased body weight and decreased food consumption. A dose-dependent diuretic effect was also noted in rats. Treatment with lesogaberan significantly enhanced replication of human islet cells in vitro, which was abrogated by a GABAB-R antagonist. Lesogaberan may be a promising drug candidate for clinical studies of diabetes intervention and islet transplantation. Disappointingly, in phase IIb study it was shown that lesogaberan is only marginally superior to placebo in gastroesophageal reflux disease (GERD) patients who are partially responsive to proton pump inhibitor (PPI) therapy.

Cronidipine (LF 2.0254) is a calcium channel blocker. LF 2.0254 inhibited in a time-dependent fashion K(+)- and Ca2(+)-induced contractions of rabbit aorta with respective IC50 of 2.7 nM and 1.7 nM. Cronidipine had a long-lasting antihypertensive action in spontaneously hypertensive rats and was able to decrease blood pressure and increase heart rate and plasma renin activity in hypertensive dogs.

Propoxate (R7464) is a potent anesthetic agent in cold-blooded vertebrates, which has never been marked and has never been used on humans.

Fluzinamide (AHR-8559), an anticonvulsant agent that was studied in patients with refractory partial seizures. However, information about the further development of this drug is not available.

Carotegrast is phenylalanine derivative patented by pharmaceutical company Ajinomoto Co. for the treatment or prevention of inflammatory disease states related to the α4 integrin-dependent adhesion process. In preclinical studies, Carotegrast shows pharmacological activity in rheumatoid arthritis and inflammatory bowel disease.

LAVOLTIDINE, also known as loxtidine, is a highly potent and selective histamine H2-receptor antagonist. It is a member of triazoles. It produces gastric carcinoid tumors in rodents that is why its clinical development was discontinued.

Isoxepac (also known) as HP-549 is a non-steroidal anti-inflammatory drug with analgesic activity. Isoxepac was studied in the clinical trial for the treatment of postoperative pain after knee surgery for meniscectomy. It was shown, that 200 mg of isoxepac would appear to be the minimal effective dose. In case of rheumatoid arthritis, isoxepac showed significantly fewer adverse effects.

Becampanel (AMP397) is an aminomethylquinoxalinedione AMPA receptor antagonist. Also, AMP397 demonstrates binding to hydroxyapatite. AMP397 has no genotoxic potential in vivo. In particular, no genotoxic metabolite is formed in mammalian cells, and, if formed by intestinal bacteria, is unable to exert any genotoxic activity in the adjacent intestinal tissue. AMP397 has a significant oral bioavailability of 22% in mice and approximately 50% in humans. It was under development for the potential treatment of status epilepticus and other types of seizures. However, this research has been discontinued. It is also being evaluated for use in the treatment of neuropathic pain and cerebrovascular ischemia.

There is no much available information related to the biological and pharmacological application of imidoline, but this compound has been found to be as potent as chlorpromazine in increasing striatal DOPA accumulation and prolactin secretion in vivo. Imidoline exhibited only weak inhibitory activity towards dopamine-sensitive adenylate cyclase and 3H-spiroperidol binding to striatal membranes in vitro. A proposed active conformation involves intramolecular hydrogen bonding between the protonated dimethylamino group and the oxygen of the imidazolidinone ring. The spatial relationship between the amine nitrogen and phenyl ring in this conformation allows proper fit of imidoline with key dimensions described for the dopamine receptor.

Mazapertine (RWJ-37796) is an arylpiperazine antipsychotic with high affinity to dopamine D2 and D3, serotonin 5-HT1A and alpha 1A-adrenergic receptors. It was being studied in the treatment of schizophrenia.