Emopamil is a phenylalkylamine calcium antagonist. Emopamil has optically active stereoisomers. Emopamil enhanced the postischemic restoration of high-energy phosphate levels. The racemic mixture and the (-)-enantiomer of emopamil caused similar metabolic changes while (+)-enantiomer of emopamil proved to be ineffective. Emopamil is able to reverse multi-drug resistance in human KB cell lines. No differences in reversing potency were observed between emopamil (R)-isomers, (L)-isomers and the racemic form. There is a pharmacological relationship between sigma1-binding site and the mammalian sterol C8-C7 isomerase which is identical with the emopamil binding protein.

Clofeverine is a compound synthesized by the Japanese company Fujisawa Pharmaceutical. Clofeverine is a highly selective relaxant for gastrointestinal smooth muscles with a beta-receptor stimulative nature. On isolated ileum, the inhibitory effect of clofeverine for spontaneous motility was comparable to that of isoproterenol and 100 times higher than that of papaverine.

Levemopamil is a novel compound of the phenylalkylamine class of calcium channel blockers, possesses exceptionally high blood-brain barrier penetrability characteristics. It has a potent antagonistic action on serotonin 5-HT2-receptors. Activation of these receptors stimulates inositol phospholipid hydrolysis that can lead to the release of Ca2+ from intracellular stores as well as protein kinase C activation. Levemopamil thus has the potential for blocking deleterious increases of intracellular calcium arising from both intracellular stores and from the extracellular space. Levemopamil reduce both infarct size and extent of neuronal injury following permanent focal or transient global ischemia. The acute effect of bilateral clamping of carotid arteries on local cerebral blood flow was measured in the presence and absence of levemopamil in a separate group of rats. The data suggest that pretreatment with levemopamil reduces impairment in spatial behaviour and that this effect seems not related to the compound's cerebral vasodilatory action, but to direct neuronal mechanisms.

Compound M24 is a selective angiotensin II AT2 receptor agonist with a Ki value of 0.4 nM for the AT2 receptor. Compound enhances in vivo duodenal alkaline secretion in Sprague-Dawley rats, and lowers the mean arterial blood pressure in anesthetized, spontaneously hypertensive rats. In a mouse model of atherosclerosis, plaque size and stability were improved in ApoE‐/‐ mice treated with M24. Treatment with M24 resulted in decrease in scar size and reduction in markers of inflammation in a rat model of myocardial infaction.