Decloxizine (UCB-1402; NSC289116) is a histamine 1 receptor antagonist. Decloxizine is a broncholyticum.

Eflumast (RP42068; N-(2-hydroxy-3-acetyl-5-fluorophenyl)-5-carboxamido-1H tetrazole) is an antiallergic agent. It was under development as an orally active antiasthmatic.

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.

Zaltidine (CP-57,361) is a guanidinothiazolylimidazole compound which is a highly specific H2-receptor antagonist. It potently inhibits gastric acid secretion. Zaltidine appears to be an effective treatment of duodenal ulcer in human studies. However, the incidence of hepatic damage (8%) seems higher than with commonly used H2-receptor antagonists.

Cilutazoline is phenoxymethyl-imidazoline derivative useful as cardiotonics and vasoconstrictors

Tuvatidine (HUK 978) is a potent H2-antagonist. HUK 978 was shown to be devoid of activity at the histamine H1-receptor, the muscarinic receptor and the alpha and beta-adrenergic receptors. In both the guinea-pig gastric mucosa preparation and the rat perfused stomach model, HUK 978 was a powerful inhibitor of acid secretion. HUK 978 is a highly specific H2-antagonist and inhibits acid secretion for longer periods than other competitive compounds.

FLOTRENIZINE, a diarylmethylpiperazine derivative, is an antihistaminic agent.

Setastine (Loderix) is a potent antagonist of histamine H1-receptor mediated responses. Setastine inhibits anaphylactic shock in guinea-pigs sensitized by horse serum. No antiserotonin, anticholinergic and antiadrenergic effect of the compound can be detected. Setastine has a long lasting (up to 16 h) antihistamine effect with a good oral effectiveness. It shows no cardiovascular effects in cats. Setastine shows a much weaker CNS depressant activity than clemestine fumarate. In displacement studies (3H-mepyramine) setastine had significantly weaker affinity for the central nervous system (CNS) H1-receptors than clemastine fumarate. It is concluded that setastine is a non-sedative highly active H1-antagonist.

Ramixotidine (also known as CM 57755 ) is a nicotinamide 1-oxide derivative patented by Sanofi as a gastric antisecretory agent. Ramixotidine is competitive histamine H2-receptor antagonist, that inhibits histamine-induced gastric acid secretion. In preclinical studies, Ramixotidine caused inhibition of dimaprit- or pentagastrin-induced secretion. Acid secretion stimulated by a meat meal was significantly reduced by Ramixotidine Ramixotidine appears to be an inhibitor of gastric acid secretion induced by different stimulants in dogs with a potency comparable to cimetidine. Unfortunately, in clinical trials, Ramixotidine failed to demonstrate efficacy and further development was discontinued.

Moxastine is a diarylmethane derivative with an antihistamine and anticholinergic activities.