Verticine is a steroidal alkaloid compound extracted from the Fritillaria species of medicinal plants. Verticine was not only able to block the Nav1.7 ion channel but also preferably inhibited the Kv1.3 ion channel. It inhibits the production of inflammatory cytokines induced by LPS through blocking MAPKs and NF-κB signaling pathways. Verticine inhibited the hERG peak tail currents in a concentration dependent manner. Verticine exhibits anti-inflammatory, antitussive, antihypertensive and pain suppression properties.

1,9-Dideoxyforskolin (DFK) is an inhibitor of glucose transporter, has been synthesized in 8 steps and 37% overall yield. 1,9-Dideoxyforskolin is a biologically inactive forskolin analog and does not stimulate adenylyl cyclase. DFK mimics some activity of forskolin, demonstrating alteration of K+ channel activity, reversal of doxorubicin resistance in multidrug resistant sarcoma cells, protection against TNF-α-mediated cytotoxicity, and desensitization at GABAA receptors. The inhibitory effect of DFK on high K (+)-induced contraction was antagonized by an increase in extracellular Ca2+ concentration. DFK inhibited the increase in cytosolic Ca2+ level and contraction in parallel whereas forskolin inhibited the contraction more strongly than the cytosolic Ca2+ level. These results suggest that DFK, but not forskolin, inhibits vascular smooth muscle contraction by a Ca2+ channel blocker-like action.

AM-36 is a novel arylalkylpiperazine with combined antioxidant and Na(+) channel blocking actions. This compound was discovered as a four-year Amrad-funded program with the Departments of Pharmacology and Chemistry at Monash University. In preclinical studies was shown, that AM-36 might have great promise in the acute treatment of human stroke. But these investigation were discontinued.

Scutellarin is the main bioactive component of Breviscapine prepared from the traditional Chinese herb Erilgeron breviscapus (Vant) Hand-Mazz. Scutellarin demonstrated protective effect on cardiovascular and cerebrovascular ischemia. The potential cytoprotective effects of the drug against cerebrovascular ischemia were evidenced by reducing cerebral infarct sizes, ameliorating neurological deficit and inhibiting neuronal apoptosis. Scutellarin is capable of inhibiting I(Na) in neurons through predominantly affecting the inactivated state of I(Na). Scutellarin may alleviate cognitive impairment in a mouse model of hypoxia by promoting proliferation and neuronal differentiation of neural stem cells. Scutellarin might play an therapeutic role by inhibiting oxidative stress and apoptosis in Alzheimer's disease treatment.

(R)-Ropivacaine (Dextroropivacaine) is a voltage-dependent potassium channel blocker with local anesthetic activity. (S)-Ropivacaine is a medication used for the production of local or regional anesthesia for surgery and for acute pain management. Ropivacaine shows a difference in channel blockade between two enantiomers, and R-Ropivacaine shows greater cardiotoxicity than (S)-Ropivacaine. (R)-Ropivacaine is the impurity in commercial formulations of Ropivacaine.

Bufalin is a traditional oriental medicines, originally isolated from the Chinese toad venom. Bufalin is a cardiotonic steroid that has the potential to induce differentiation and apoptosis of tumor cells. Research on bufalin has so far mainly involved leukemia, prostate cancer, gastric cancer and liver cancer, and has been confined to in vitro studies. The bufadienolides bufalin and cinobufagin have been shown to induce apoptosis in a wide spectrum of cancer cell. Bufalin has being shown to be a potent small-molecule inhibitor of the steroid receptor coactivators SRC-3 and SRC-1. Bufalin is a component of Huachansu, a Chinese medicine that comes from dried toad venom from the skin glands of Bufo bufo gargarizans Cantor or B.melanotictus Schneider, has been used in the treatment of various cancers in China.

WIN 55212-2 is the synthetic cannabimimetic compound. It is a potent aminoalkylindole cannabinoid receptor agonist. WIN 55,212-2 increases expression of anti-oxidant Cu/Zn SOD and is able to prevent inflammation induced by Aβ1-42 in cultured astrocytes. It exerts neuroprotective and anti-inflammatory actions against Aβ damage through both CB₁ and CB₂ receptors. WIN 55212-2 attenuates hyperalgesia and allodynia in a rat model of neuropathic pain. In the clinical trial, it was revealed that WIN 55212-2, applied topically, decreases the intraocular pressure of human glaucoma resistant to conventional therapies within the first 30 min.

Phenthiazamine was developed by Sekizawa et al. as a centrally acting anesthetic for fish. The time required to reduce the positive ganglionic potential in the sympathetic ganglion by phenthiazamine was prolonged in the presence of higher concentrations of Ca2+. The Ca2+-dependent action potential of guinea-pig ureter was reduced by this compound, whereas it did not affect the Na+-dependent action potential.