Ampyzine is a pyrazine derivative patented by Warner-Lambert Pharmaceutical Co. as a central nervous system stimulant.

Anatibant was a selective small-molecule antagonist of the bradykinin B2 receptor that was undergoing clinical development with Xytis and Fournier for the treatment of brain injuries. Anatibant reduces brain oedema in animal TBI models. Noserious toxicity was found in Phase 1 clinical trials. Following subcutaneous administration of clinically relevant doses, there were no systemic effects but there was pain, inflammation and nodule formation at the injection site. Anatibant inhibits the binding of BK to the B2 receptor. After subcutaneous injection Anatibant is bio-available and crosses the BBB.

Butopyrammonium is organic cationic compound.

Benzindopyrine belongs to anticholinergic agents. It was studied as an antipsychotic drug.

Etorphine was the first potent opiate agonist employed primarily for use in non-domestic and wild species. Etorphine was 500 times as potent as morphine, with a very rapid onset and short duration of action. In morphine-dependent subjects, etorphine suppressed abstinence but for a shorter period than morphine. Etorphine is a full opiate agonist and binds to multiple opiate sites in the central nervous system. It is believed to produce its clinical effects through binding the µ-, δ-, and κ- opiate sites. It has a potent effect on depressing the respiratory centers of the CNS thus resulting in apnea being commonly seen in immobilized animals. Etorphine revolutionized the ability of biologists and veterinarians to safely capture and restrain many species that previously could not be handled. Etorphine is not currently commercially available due to lack of production by the manufacturer.

Fedotozine [(1R)-1-phenyl-1-[(3,4,5-trimethoxy) benzyloxymethyl]-N,N- dimethyl-n-propylamine, (2S,3S-tartrate], derived from the arylacetamide series, is an opioid drug which acts as a selective agonist for kappa(1a)-opioid receptor. Pharmacological studies have shown that fedotozine exerts a peripheral antinociceptive action, comparable with that of other kappa-agonists. Results of Phase III trials of fedotozine against irritable bowel syndrome and dyspepsia have ultimately been disappointing and was lack of efficacy in subsequent studies.

Exepanol (KC 2450), a benzoxepine derivative, is a gastrokinetic. It facilitated the peristaltic reflex. Exepanol enhances resting pressure of the lower esophageal sphincter.

Hydromorphinol, an opioid, and is a derivative of morphine and possesses similar properties: sedation, analgesia, and respiratory depression. Hydromorphinol is under the control according to US Single Convention 1961.

Rimacalib (SMP 114) is a prostaglandin E2 antagonist that has been evaluated for use in rheumatoid arthritis. This orally bioavailable compound is a CaMKII inhibitor developed for human use. A phase II clinical trial to compare the effects of rimacalib to placebo in patients with rheumatoid arthritis has been terminated in 2009. Rimacalib also reduces SR Ca2+ leak and was therefore suggested as a candidate drug to treat proarrhythmogenic events in human atrial cardiomyocytes and cardiomyocytes from patients with heart failure.

Tazomeline (also known as LY 287041), a neuropsychiatric agent, is a muscarinic M1 acetylcholine receptor agonist that was studied in patients with cognitive dysfunction. Tazomeline participated in clinical trials for the treatment of Alzheimer’s disease and dementia. However, all these studied were discontinued for unknown reasons.