Huwentoxin XVI, an analgesic, is a highly reversible and selective mammalian N-type calcium channel (IC50 of ~60 nM) antagonist from Chinese tarantula Ornithoctonus huwena. Huwentoxin XVI has no effect on voltagegated T-type calcium channels, potassium channels or sodium channels[1].
YS-201 is a dihydropyridine-type calcium channel antagonist previously in clinical trials for the treatment of angina pectoris and hypertension.
Huwentoxin I (HWTX-I) is a peptide toxin that inhibits voltage-gated sodium channels and N-type calcium channels. Huwentoxin I inhibits sodium channels in rat hippocampus and cockroach dorsal unpaired median (DUM) neurons with IC50 values of 66.1 and 4.80 nM, respectively[1].
Levetiracetam(UCB L059) is a novel anticonvulsant with antihyperalgesic efficacy in inflammatory pain.Target: Calcium ChannelLevetiracetam is used to control some types of seizures in patients with epilepsy. This medicine cannot cure epilepsy and will only work to control seizures for as long as you continue to use it. The exact mechanism for levetiracetam is unknown. However, the drug binds to a synaptic vesicle protein, SV2A, which is believed to impede nerve conduction across synapses [1].Levetiracetam (10-200 mg/kg), ibuprofen (12.5-100 mg/kg), celecoxib (3.75-30 mg/kg), paracetamol (50-200 mg/kg), caffeine (15-100 mg/kg), and 2-drug combinations of levetiracetam with analgesics/caffeine produced a significant, dose-dependent reduction of inflammatory hyperalgesia. Isobolographic analysis revealed that levetiracetam exerts a synergistic interaction with analgesics, with approximately 7-, 9-, and 11-fold reduction of doses of both drugs in combination of levetiracetam with paracetamol, celecoxib, and ibuprofen, respectively. Analysis of the log dose-response curves for levetiracetam (1-50 mg/kg) in the presence of caffeine (10 mg/kg) and levetiracetam applied alone also revealed a synergistic interaction. Levetiracetam's ED50 in the presence of caffeine was reduced approximately 11-fold [2].Clinical indications: Epilepsy; Social phobiaFDA Approved Date: November 2008Toxicity: depression; hallucinations; suicidal thoughts
Azumolene (EU4093 free base), a Dantrolene analog, is a muscle relaxant. Azumolene is a ryanodine receptor (RyR) modulator and inhibits the calcium-release through ryanodine receptor. Azumolene can be used for malignant hyperthermia research[1][2].
Myomodulin is a neuropeptide present in molluscs, insects, and gastropods.
Ionomycin (calcium) is a Calcium ionophore and an antibiotic produced by Streptomyces conglobatus.
Ionomycin is a Calcium ionophore and an antibiotic produced by Streptomyces conglobatus ATCC 31005.
Bay-K-8644 (S)-(-)- is an agonist of L-type Ca2+ channel. Bay-K-8644 (S)-(-)- activates Ba2+ currents (IBa) (EC50=32 nM).
Psoralenoside is a benzofuran glycoside from Psoralea corylifolia[1]. Psoralenoside exhibits high binding affinities against histaminergic H1, calmodulin, and voltage-gated L-type calcium channels (E-value≥-6.5 Kcal/mol)[2]. Psoralenoside shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity[3].
1-Octanol-d2 is the deuterium labeled 1-Octanol[1]. 1-Octanol (Octanol), a saturated fatty alcohol, is a T-type calcium channels (T-channels) inhibitor with an IC50 of 4 μM for native T-currents[2]. 1-Octanol is a highly attractive biofuel with diesel-like properties[3].
Paxilline is an indole alkaloid mycotoxin from Penicillium paxilli, acts as a potent BK channels inhibitor by an almost exclusively closed-channel block mechanism. Paxilline also inhibits the sarco/endoplasmic reticulum Ca2+ ATPase (SERCA) with IC50s between 5μM and 50μM for differing isoforms. Paxilline possesses significant anticonvulsant activity[1][2][3].
(R)-IDHP is an isomer of IDHP, a salvia metabolite that exerts vasorelaxant effects by inhibiting Ca2+ release and Ca2+ inward flow in voltage-dependent and receptor-operated calcium channels in vascular smooth muscle cells. IDHP is used in studies of cardiovascular disease[1].
Manidipine-d4 is the deuterium labeled Manidipine. Manidipine is a calcium channel blocker that is used clinically as an antihypertensive[1][2].
Lercanidipine-13C,d3 (hydrochloride) is the deuterium and 13C labeled Lercanidipine hydrochloride[1]. Lercanidipine hydrochloride is a lipophilic third-generation dihydropyridine-calcium channel blocker (DHP-CCB). Lercanidipine hydrochloride has long lasting antihypertensive action and reno-protective effect[2][3][4].
Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive drug and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
Ethosuximide, a widely prescribed anti-epileptic drug, improves the phenotypes of multiple neurodegenerative disease models and blocks the low voltage activated T-type calcium channel.
Imperatoxin A, a peptide toxin derived from the venom of the African scorpion Pandinus imperator, activator of Ca2+-release channels/ryanodine receptors (RyRs)? enhances the influx of Ca2+ from the sarcoplasmatic reticulum into the cell[1].
Antiarrhythmic agent-2 is a nonspecific Ca2+ inward current blocker that inhibits ionic currents in sensory neuron membranes. Antiarrhythmic agent-2 can be used in the study of cardiovascular diseases, such as arrhythmias[1].
MK-8998 is a potent and selective antagonist of the T-type calcium channel.
Mibefradil dihydrochloride hydrate (Ro 40-5967 dihydrochloride hydrate) is a effectively long-acting calcium channel antagonist, used as an antihypertensive agent. Mibefradil dihydrochloride hydrate acts via a higher affinity block for low-voltage-activated (T) than for high-voltage-activated (L) calcium channels[1].
Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect[1][2][3][4][5][6][7].
Gallopamil (Methoxyverapamil), a methoxy derivative of Verapamil, is a phenylalkylamine calcium antagonist. Gallopamil acts on the vascular system and the heart and nodal structure[1]. Gallopamil inhibits acid secretion in a concentration-dependent manner with an IC50 of 10.9 μM[2].
SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, is a potent, high affinity, selective and voltage-dependent R-type CaV2.3 channel blocker with an IC50 of 30 nM. SNX-482 has antinociceptive effect[1][2][3].
Iganidipine is a Ca2+ antagonist.
2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of IP3R. 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca2+ (SOC) channel and activates some TRP channels (V1, V2 and V3)[1][2][3].
Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2, with EC50s of 14.23 μM and 3.34 μM, respectively, and is used as a potential treatment for motor nerve terminal dysfunction.
Teludipine is a lipophilic calcium channel blocker.
(S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells[1].
Thapsigargin is an inhibitor of microsomal Ca2+-ATPase.