Zolantidine is the novel benzthiazole derivative. It is a centrally acting potent antagonist of histamine at H2-receptors. It was found to be a competitive inhibitor of the histamine catabolising enzyme in brain, histamine N-methyltransferase. High aggression in histamine N-methyltransferase knockout mice was suppressed by treatment with zolantidine, indicating that abnormal histamine H2 receptor activation promoted aggression in knockout mice. Histamine H(3) receptor antagonist JNJ-10181457-induced anxiety-like behaviours were dominantly reduced by zolantidine. Zolantidine significantly attenuated the discriminative stimulus effects of morphine.

YM022 is an extremely potent and highly selective gastrin/cholecystokinin (CCK)-B receptor antagonist. It was discovered, that this compound possesses antisecretory and antiulcer activities in rats and that it represents a useful therapeutic agent in the treatment of peptic ulcer disease. However, research into this compound has subsequently been discontinued.

CP-96,345 is a potent, selective nonpeptide Substance P (NK1) receptor antagonist. Rather than being a primary neurotransmitter, it prolongs the nociception produced by other neurotransmitters. By controlling endothelial permeability, SP plays a major role in inflammation and inflammatory aspects of asthma, possibly by regulating the access of neutrophils to an inflammatory site. These results indicate potential therapeutic applications for SP antagonists in the treatment of chronic pain, inflammation, and inflammatory aspects of asthma.

RP-67580 selectively inhibits the binding of substance-P to Neurokinin Receptor-1 and does not show meaningful antagonistic activity against NK2 and NK3. Preclinical trials had been conducted and discontinued in France for the potential treatment of inflammation and pain. RP-67580 has not been used in human trials.

RO 15-4513 is a high-affinity benzodiazepine ligand which acts as a partial inverse agonist at recombinant diazepam-sensitive (DS) benzodiazepine α1-, α2-, α3- and α5-GABAA receptors, developed by Hoffmann–La Roche in the 1980s. Ro 15-4513 reverses the sedating and anticonflict effects of alcohol, and can, therefore, be used as an antidote to the acute impairment caused by alcohol. In non-food or fluid-deprived rats, orally self-administering 10% alcohol in an operant situation, Ro 15-4513 resulted in a dose-dependent suppression of alcohol intake. The use of Ro 15-4513 would appear to be limited by the fact that the compound is proconvulsant. Ro 15-4513 has been found to induce seizures in mice undergoing ethanol withdrawal. However, it is a potentially powerful tool with which to investigate the neuropsychopharmacology of alcohol. Labelling Ro15-4513 with carbon-11 leads to the possibility of its use in PET imaging of the brain. The specificity of the compound to a small number of GABA receptor sub-types leads to the generation, with accurate modeling, of detailed images with well-defined limbic and cortical structures. These images can be useful in quantitatively analyzing conditions such as addiction, that is known to be, at least in part, associated with the GABAergic system.