Enecadin (NS 7 or ZK 228326) is a voltage-dependent sodium and calcium channel blocker. Enecadin is a neuroprotective agent demonstrated efficacy in animal models of ischemic injury of brain, spinal cord and retina. Enecadin was undergoing phase II development in stroke with PAION in Germany. Enecadin development has been discontinued.

Procodazole is a non-specific active immunoprotective agent against viral and bacterial infections

Chlorogenic acid is the ester of caffeic acid and (-)-quinic acid. Chlorogenic acid is a naturally occurring plant metabolite and can be found with the related compounds cryptochlorgenic acid and neochlorogenic acid in the leaves of Hibiscus sabdariffa, coffee, potato, eggplant, peaches, and prunes. Chlorogenic acid has been investigated as a dietary supplement to improve glucose intolerant hypoglycemia and non-alcoholic fatty liver disease. It has also been identified as a potential anticancer agent by reducing the expression of HIF-1a and Sphingosine Kinase-1. Chlorogenic acid was also identified as a neuraminidase blocker effective against influenza A virus (H1N1 and H3N2).

ABT-639 is a T-type calcium (Cav3.2) channel antagonist that was in development with AbbVie for the treatment for pain. ABT-639 is a potent and selective T-type calcium channel blocker. ABT-639 effectively reduces nociceptive and neuropathic pain in rats. ABT-639 produces robust antinociceptive activity in experimental pain models at doses that do not significantly alter psychomotor or hemodynamic function in the rat. ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50=2 uM) and attenuates low voltage-activated (LVA) currents in rat DRG neurons (IC50=8 uM). ABT-639 was significantly less active at other Ca²⁺ channels (e.g. Ca(v)1.2 and Ca(v)2.2) (IC₅₀ > 30 uM). ABT-639 has high oral bioavailability (%F = 73), low protein binding (88.9%) and a low brain:plasma ratio (0.05:1) in rodents.

Tesofensine (also known as NS-2330) is a novel triple monoamine reuptake inhibitor with intrinsic inhibitory activity on norepinephrine (NE), serotonin (5-HT), and dopamine (DA) transporter function. It was development by NeuroSearch as a potential therapy for Alzheimer's disease (AD) and Parkinson's diseases, but these efforts have been discontinued. In phase II clinical trials with tesofensine in obese individuals, dose-related reductions in body weight, body fat and waist circumference, as well as improvements in other obesity-related endocrine factors were observed and the FDA recently endorsed the phase III trial program for this agent.

Iganidipin is a new dihydropiridynic derivative of calcium antagonist. It is the only currently available calcium antagonist in the form of ophthalmic solution. Its topical administration increases ipsilateral optic nerve head blood flow in rabbits and monkeys and inhibits the contraction of blood vessels induced by endothelin -1. Iganidipin is also used for treat Angina pectoris and Hypertension.

PF-05089771 is an oral administrated Nav1.7 channel inhibitor. PF-05089771 provided the best opportunity to explore Nav1.7 blockade for the treatment of acute or chronic pain conditions. PF-05089771 has completed Phase II clinical trials of third molar extraction and primary inherited erythromelalgia. The magnitude of efficacy of PF-05089771 in the randomized, placebo-controlled, double-blind clinical study in subjects with painful diabetic peripheral neuropathy was disappointing. Although there was a trend towards a reduction in pain and improvement in sleep rating in patients with painful DPN when compared to placebo treatment, this was not statistically significant.

Carboxyamidotriazole (L651582) is a carboxyamide-amino-imidazole compound originally developed as a coccidiostat, an antiprotozoal agent that acts upon Coccidia parasites. Carboxyamidotriazole (L651582) is an orally-active agent with potential antineoplastic activity. Carboxyamidotriazole binds to and inhibits non-voltage-operated Ca2 channels, blocking both Ca2 influx into cells and Ca2 release from intracellular stores and resulting in the disruption of calcium channel-mediated signal transduction and inhibition of vascular endothelial growth factor (VEGF) signaling, endothelial proliferation, and angiogenesis. This agent may also inhibit tumor cell growth, invasion, and metastasis.

Berlafenone (previously known as GK 23 G), a sodium channel antagonist was studied as a class Ic antiarrhythmic agent, but development has been discontinued.