-
ATPase and GTPase inhibitor
Etidronate Disodium is a bisphosphonate bone resorption inhibitor. -
AMPA antagonist
YM90K hydrochloride is a selective AMPA receptor antagonist that delays neuronal death in a global ischemia model and cerebral infarction in a focal ischemia model following postischemic administration. - Linoleylethanolamide is an endocannabinoid that also binds to TRPV1 (Ki = 5.60 uM).
-
TRPA1 activatior/TRPM8 blocker
Cannabichromene is a major non-psychotropic phytocannabinoid that inhibits endocannabinoid inactivation and activates the transient receptor potential ankyrin-1 (TRPA1). Both endocannabinoids and TRPA1 may modulate gastrointestinal motility. -
AMPA/kainate receptor antagonist
Talampanel is a non-competitive antagonist of AMPA-receptor. - (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca2+-permeable nonselective cation channel, to increase [Ca2+]i. Antitumor activity.
-
5-HT3 receptor inhibitor
Eucalyptol is a bicyclic monoterpene that has been found in Eucalyptus and other plants. It is an inhibitor of 5-HT3 receptor ,potassium channel, TNF-α and IL-1β. -
L-type calcium channel blocker
Amlodipin is L-type calcium channel blocker that displays antihypertensive properties. It inhibits Ca2+-induced contractions in depolarized rat aorta (IC50 = 1.9 nM) and displays vasoprotective effects in cardiovascular disease. -
L-type calcium channel blocker
Amlodipine-besylate is L-type calcium channel blocker that displays antihypertensive properties. It inhibits Ca2+-induced contractions in depolarized rat aorta (IC50 = 1.9 nM) and displays vasoprotective effects in cardiovascular disease. -
AMPA Receptor Inhibitor
Aniracetam is an ampakine and nootropic of the racetam chemical class purported to be considerably more potent than piracetam. -
Protein kinase inhibitor
Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.
- Artemisinin and its derivatives are a group of drugs that possess the most rapid action of all current drugs against Plasmodium falciparum malaria.
- Bupivacaine is a more potent inhibitor of cAMP production than are chemically related local anesthetics that are less prone to produce cardiovascular toxicity.
-
Calcium channel blocker
Cilnidipine is a dual blocker of L-type voltage-gated calcium channels in vascular smooth muscle and N-type calcium channels in sympathetic nerve terminals that supply. - Diethylstilbestrol is a synthetic nonsteroidal estrogen that was first synthesized in 1938. It is also classified as an endocrine disruptor.
- Diltiazem is a nondihydropyridine (non-DHP) member of the class of drugs known as calcium channel blockers, used in the treatment of hypertension, angina pectoris, and some types of arrhythmia.
-
Proton pump inhibitor
Esomeprazole sodium is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells. -
TRP agonist
Evodiamine is a chemical extracted from the Tetradium family of plants. It acts primarily as a thermogenic and stimulant. -
Kir6.2/SUR inhibitor
Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus. -
AMPA and Kainate antagonist
GYKI-52466 dihydrochloride is selective non-competitive AMPA receptor antagonist (IC50 values are 10-20, ~ 450 and >> 50 μM for AMPA- , kainate- and NMDA-induced responses respectively). - Hydralazine hydrochloride is a hydrochloride salt of hydralazine (Apresoline) that is a direct-acting smooth muscle relaxant with an IC50 of 1.9 mM.
-
proton pump inhibitor
Lansoprazole(AG 1749) is a proton pump inhibitor which prevents the stomach from producing acid. - Lidocaine (Alphacaine) is an anasthetic and class Ib antiarrhythmic agent. Blocks voltage-gated sodium channels in the inactivated state.
- Lubiprostone is a bicyclic fatty acid metabolite analog of Prostaglandin E1. It activates specific chloride channels in the gastrointestinal tract to stimulate intestinal fluid secretion, and increase gastrointestinal transit.
-
PDE4 inhibitor
Luteolin is a PDE4 inhibitor, phosphodiesterase inhibitor, and an interleukin 6 inhibitor, affecting xylazine/ketamine-induced anesthesia in mice. Luteolin acts as a monoamine transporter activator, and is one of the few chemicals demonstrated to possess this property. - Manidipine is a dihydropyridine compound and calcium channel protein inhibitor and antagonist.
- Minoxidil (U-10858) is a selective ATP dependent K+ (Kir6) channel activator.
- Nateglinide(Starlix) is an insulin secretagog agent that lowers blood glucose levels by stimulating insulin secretion from the pancreas.
-
calcium channel blocker
Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker belonging to the dihydropyridines class, specific for L-type Cav1.2 with IC50 of 10 nM. -
ATPase Inhibitors
Omeprazole is a cell-permeable, selective proton pump inhibitor. -
CFTR Inhibitor
Oridonin (Isodonol), an entkaurane diterpenoid isolated from Rabdosia rubescens, is an important traditional Chinese herbal remedy. - Phenytoin sodium (Dilantin) is a sodium channel protein inhibitor.
-
P-gp inhibitor
P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance. - Atagabalin is related to gabapentin, which similarly binds to the α2δ calcium channels (1 and 2).
-
Serotonin transporter inhibitor
Imipramine Hydrochloride is a tricyclic antidepressant. Inhibits the serotonin and norepinephrine transporters but has little effect on the dopamine transporter. -
SGLT2 Inhibitor
Luseogliflozin is an orally active second-generation sodium-glucose co-transporter 2 (SGLT2) inhibitor developed by Taisho Pharmaceutical for the treatment of patients with type 2 diabetes mellitus (T2DM). -
P-gp inhibitor
Laniquidar is a third-generation P-gp inhibitor, which has been used in clinic trials for modulating multidrug resistance transporters.

