Calcium Channel
Calcium channels generate intracellular Ca2+ signals by mediating Ca2+ entry during depolarization in excitable cells[1]. These signals support neurotransmitter release, hormone release, excitation-contraction coupling, pacemaker activity, gene transcription, and synaptic plasticity[1][2]. Mechanistically, adrenergic agonists increase cardiac Ca2+ influx through PKA phosphorylation of Rad, which releases inhibition of calcium channels and enhances contractility[3]. In disease research, CACNA1C/CaV1.2 links L-type calcium channel signaling to bipolar disorder, depression, schizophrenia, autism spectrum disorders, brain function, and rodent antidepressant-like behavioral actions of LTCC inhibitors[4]. Compared with related isoforms, CaVα1 splice variants show tissue-specific expression, distinct protein-domain composition, and different pharmacological sensitivities[5]. CaV2.2 e37a is enriched in nociceptors and couples N-type calcium channels to voltage-independent G protein inhibition by µ-opioid and GABA_B receptors[6]. For experimental applications, blockers, toxins, gene-knockout models, agonists, and inhibitors help dissect channel-specific functions and guide next-generation CaV channel modulators[1][5].
References:
- [1]. Striessnig J, et al. Exploring the function and pharmacotherapeutic potential of voltage-gated Ca2+ channels with gene knockout models. Channels (Austin). 2008 Jul-Aug;2(4):233-51. [Content Brief]
- [2]. Prakriya M. Calcium and cell function. J Physiol. 2020 May;598(9):1647-1648. doi: 10.1113/JP279541. PMID: 32350889; PMCID: PMC7885240. et al. Calcium and cell function. J Physiol. 2020 May;598(9):1647-1648. [Content Brief]
- [3]. Papa A, et al. Adrenergic Regulation of Calcium Channels in the Heart. Annu Rev Physiol. 2022 Feb 10;84:285-306. [Content Brief]
- [4]. Bhat S, et al. CACNA1C (Cav1.2) in the pathophysiology of psychiatric disease. Prog Neurobiol. 2012 Oct;99(1):1-14. [Content Brief]
- [5]. Lipscombe D, et al. Calcium Channel CaVα₁ Splice Isoforms - Tissue Specificity and Drug Action. Curr Mol Pharmacol. 2015;8(1):22-31. [Content Brief]
- [6]. Lipscombe D, et al. Alternative splicing matters: N-type calcium channels in nociceptors. Channels (Austin). 2007 Jul-Aug;1(4):225-7. [Content Brief]
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Calcium Channel Related Products (961)
Related Products (961)
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TGR5 Receptor Agonist
0 ImagesSynonyms: CCDCTGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity.
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Acetylcholine chloride (Standard)
0 ImagesAcetylcholine (chloride) (Standard) is the analytical standard of Acetylcholine (chloride). This product is intended for research and analytical applications. Acetylcholine chloride (ACh chloride), a neurotransmitter, is a potent and BBB-permeable cholinergic agonist. Acetylcholine chloride is a modulator of the activity of dopaminergic (DAergic) neurons through the stimulation of nicotinic acetylcholine receptors (nAChRs). Acetylcholine chloride inhibits p53 mutant peptide aggregation in vitro.
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Pulegone
0 ImagesPulegone is a monoterpene ketone compound widely present in the essential oils of many plants. Pulegone can also be used as a bird repellent. Pulegone has multiple activities such as anti-inflammatory, antibacterial, antifungal, and anti-hyperalgesic effects. Pulegone is particularly effective against bacteria of the Salmonella species.
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MRS 1523
0 ImagesMRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons.
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Nicardipine hydrochloride
0 ImagesSynonyms: YC-93Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.
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Tetracaine
0 ImagesTetracaine (Amethocaine) is a sodium channel inhibitor and ryanodine receptor (RyR) inhibitor. Tetracaine blocks sodium conduction across nerve cell membranes, preventing rapid sodium ion influx and depolarization. Tetracaine exhibits biphasic effects on spontaneous sarcoplasmic reticulum Ca2+ release in Ca2+-overloaded ventricular myocytes, and increases sarcoplasmic reticulum Ca2+ load. Tetracaine can be used in research related to eye diseases.
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Levomepromazine
0 ImagesLevomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca2+ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting.
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Palmitoylglycine
0 ImagesSynonyms: N-palmitoyl glycinePalmitoylglycine (N-palmitoyl glycine), an endogenous lipid that acts as a modulator of calcium influx and nitric oxide () production in sensory neurons. Palmitoylglycine is linked to an increased risk of Background Brugada syndrome (BrS) and interacts with BrS-associated proteins, demonstrating moderate binding affinities for DCC, CR1, CTSB, NAAA, DEFB1, EPHA1, IGF1/IGFBP3/ALS, and LTA.
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Cinchonine
0 ImagesCinchonine is a natural compound present in Cinchona bark with antimalarial, antitumor, anti-inflammatory, anti platelet-aggregation and anti-obesity properties. Cinchonine inhibits cells proliferation and autophagy and induces apoptosis through activation of Caspase-3. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
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Clevidipine
0 ImagesClevidipine is a selective, short-acting L-type calcium channel antagonist with an IC50 of 7.1 nM. Clevidipine can competitively bind to calcium channels and exert rapid vasoselective vasodilation by blocking the influx of extracellular calcium ions, thereby reducing peripheral vascular resistance and effectively controlling acute severe hypertension. Clevidipine can also protect the myocardium from reperfusion injury by promoting the release of nitric oxide (NO). Clevidipine can be used in the research of acute hypertension, perioperative blood pressure management, and myocardial ischemia-reperfusion injury.
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S107
0 ImagesS107 is an orally available, blood brain barrier-permeable compound, which stabilizes RyR2 channels by enhancing the binding of calstabin 2 to the mutant Ryr2-R2474S channel. S107 inhibits Ca2+ leakage from the sarcoplasmic reticulum (SR) and prevents cardiac arrhythmias and raises the seizure threshold.
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Cyclic ADP-ribose
0 ImagesCat. No.: HY-N7395CAS No.: 119340-53-3Synonyms: cADPRCyclic ADP-ribose (cADPR) is a potent second messenger for calcium mobilization that is synthesized from NAD+ by an ADP-ribosyl cyclase. Cyclic ADP-ribose increases cytosolic calcium mainly by Ryanodine receptor-mediated release from endoplasmic reticulum and also by extracellular influx through the opening of TRPM2 channels.
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Fendiline hydrochloride
0 ImagesFendiline hydrochloride, a diphenylalkylamine type of antianginal agent, is an L-type calcium channel blocker (IC50 of 17 µM). Fendiline hydrochloride is also a selective K-Ras inhibitor, and has no effect on H-Ras and N-Ras. Fendiline hydrochloride inhibits K-Ras plasma membrane localization (IC50 of 9.64 μM), inhibits K-Ras signal output and blocks the proliferation of pancreatic, colon, lung, and endometrial cancer cell lines expressing oncogenic mutant K-Ras. Fendiline hydrochloride is a STING agonist and is able to inhibit the growth of multiple refractory cold tumors (MC38, CT26 and B16F10).
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Dantrolene sodium
0 ImagesSynonyms: F 440Dantrolene sodium is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium is also a calcium channel protein inhibitor. Dantrolene sodium inhibits the release of Ca2+ from RyR1 and RyR3, which can be beneficial in a variety of pathologies caused by disruptions in calcium homeostasis (e.g., stroke, ischemia/reperfusion injury, and neurodegenerative diseases). Dantrolene sodium offers relief of muscle spasms, malignant hyperthermia, and antitoxic, antipyretic, and anti-inflammatory properties.
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N106
0 ImagesN106 is a first-in-class sarcoplasmic reticulum calcium ATPase (SERCA2a) SUMOylation activator. N106 directly activates the SUMO-activating enzyme, E1 ligase. N106 can be used for heart failure research.
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(R)-Verapamil hydrochloride
0 ImagesSynonyms: (R)-(+)-Verapamil hydrochloride(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is an orally active P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport. (R)-Verapamil hydrochloride induces Apoptosis and inhibits L-type calcium channels BZPcc, DHPcc and PLLcc. (R)-Verapamil hydrochloride has anti-septic shock and anti-diabetic effects.
