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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Gabapentin hydrochloride (Standard)
0 ImagesCat. No.: HY-A0057ARCAS No.: 60142-95-2Gabapentin (hydrochloride) (Standard) is the analytical standard of Gabapentin (hydrochloride). This product is intended for research and analytical applications. Gabapentin hydrochloride is a potent, orally active P/Q type Ca2+ channel blocker. Gabapentin hydrochloride inhibits neuronal Ca2+ influx and reduction of neurotransmitter release. Gabapentin hydrochloride is a GABA analog that can be used to relieve neuropathic pain.
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PD 122860
0 ImagesCat. No.: HY-124229CAS No.: 122576-86-7PD 122860 is a calcium channel blocker. PD 122860 also can stimulate sodium channel. PD 122860 can be used for the research of cardiovascular and cerebrovascular diseases.
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Wilforgine (Standard)
0 ImagesCat. No.: HY-N1072RCAS No.: 37239-47-7Wilforgine (Standard) is the analytical standard of Wilforgine. This product is intended for research and analytical applications. Wilforgine is a bioactive sesquiterpene alkaloid in Tripterygium wilfordii Hook. F. Wilforgine can induce microstructural and ultrastructural changes in the muscles of Mythimna separata larvae, and the sites of action are proposed to be calcium receptors or channels in the muscular system.
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Saquinavir-13C6
0 ImagesCat. No.: HY-17007S2Synonyms: Ro 31-8959-13C6Saquinavir-13C6 (Ro 31-8959-13C6) is 13C labeled Saquinavir (HY-17007). Saquinavir (Ro 31-8959) is an orally active HIV protease inhibitor that can be used in the research of AIDS. Saquinavir also has anti-inflammatory activity and can induce apoptosis of human red blood cells.
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Carboxyatractyloside dipotassium (Standard)
0 ImagesCat. No.: HY-N2522RCAS No.: 33286-30-5Synonyms: Gummiferin dipotassium (Standard)Carboxyatractyloside (dipotassium) (Standard) is the analytical standard of Carboxyatractyloside dipotassium (HY-N2522). This product is intended for research and analytical applications. Carboxyatractyloside dipotassium is a diterpenoid. Carboxyatractyloside dipotassium can be isolated from plants of the genus Xanthium. Carboxyatractyloside dipotassium is an ADP/ATP carrier inhibitor, inhibiting mitochondrial ADP/ATP transport. Carboxyatractyloside dipotassium promotes ROS production, induces Ca2+ release, and leads to mitochondrial dysfunction. Carboxyatractyloside dipotassium induces lethargy, weakness, and epileptic seizures in rats.
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Nicardipine (Standard)
0 ImagesSynonyms: YC-93 free base (Standard)Nicardipine (Standard) is the analytical standard of Nicardipine. This product is intended for research and analytical applications. Nicardipine (YC-93 free base) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine acts as an agent for chronic stable angina and for controlling blood pressure.
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Psoralenoside (Standard)
0 ImagesCat. No.: HY-N7503RCAS No.: 905954-17-8Psoralenoside is a benzofuran glycoside from Psoralea corylifolia. Psoralenoside exhibits high binding affinities against histaminergic H1, calmodulin, and voltage-gated L-type calcium channels (E-value≥-6.5 Kcal/mol). Psoralenoside shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.
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Diltiazem (Standard)
0 ImagesDiltiazem (Standard) is the analytical standard of Diltiazem. This product is intended for research and analytical applications. Diltiazem is an orally active L-type Ca2+ channel blocker. Diltiazem shows antihypertensive and antiarrhythmic effects. Diltiazem can be used for the research of cardiac arrhythmia, hypertension, and angina pectoris.
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NAADP receptor modulator-1
0 ImagesCat. No.: HY-121253CAS No.: 854091-96-6NAADP receptor modulator-1 is a cell-permeable NAADP receptor modulator. NAADP receptor modulator-1 competes with NAADP for binding sites and inhibits NAADP-induced Ca2+ release.
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Verticilide
0 ImagesCat. No.: HY-N7491CAS No.: 693778-57-3Verticilide is a ryanodine-binding inhibitor and inhibits ryanodine binding to ryanodine receptors in the cockroach at an IC50 value of 4.2 μM (whereas inhibition against mouse ryanodine receptors was weak (IC50=53.9 μM)).
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1-Octanol-d2-1
0 ImagesCat. No.: HY-W032013S2CAS No.: 1335435-64-7Synonyms: Octanol-d2-11-Octanol-d2-1 is deuterated labeled 1-Octanol (HY-W032013). 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. 1-Octanol is a highly attractive biofuel with diesel-like properties.
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Bay K 8644 (Standard)
0 ImagesSynonyms: (±)-Bay K 8644 (Standard)Bay K 8644 (Standard) is the analytical standard of Bay K 8644. This product is intended for research and analytical applications. Bay K 8644 ((±)-Bay K 8644) is a racemate consisting of two isomers (R)-(+)-Bay-K-8644 and (S)-(-)-Bay-K-8644. Bay K 8644 is a L-type Ca2+ channel agonist with an EC50 of 17.3 nM. Bay K 8644 increases Ca2+ influx through sarcolemmal Ca2+ channels by increasing the open time of the channel. Bay K 8644 has vasoconstrictive effects.
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Manidipine-d4
0 ImagesCat. No.: HY-B0419SCAS No.: 1189656-59-4Manidipine-d4 is the deuterium labeled Manidipine (HY-B0419). Manidipine is an orally active calcium channel antagonist. Manidipine regulates the expression of cytokines (IL-1β, IL-6). Manidipine has a hypotensive effect. Manidipine can be used in the study of cardiovascular diseases (such as hypertension, myocardial ischemia-reperfusion injury, ventricular hypertrophy), kidney diseases (such as glomerular diseases), and epilepsy.
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Clonixin (Standard)
0 ImagesSynonyms: SCH-10304 (Standard)Clonixin (SCH-10304) (Standard) is the analytical standard of Clonixin. This product is intended for research and analytical applications. Clonixin is an orally active non-steroidal anti-inflammatory agent (NSAID) that inhibits COX synthesis. Clonixin acts as a voltage-gated L-type calcium channel blocker, exerts vasodilatory effects by antagonizing Ca2+ in vascular smooth muscle. Clonixin inhibits TGF-β, reduces lung coefficient, immune cell infiltration level, oxidative stress response, airway resistance, hydroxyproline content and collagen deposition. Clonixin can be used in research related to inflammation such as idiopathic pulmonary fibrosis and moderate to severe pain.
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Isradipine (Standard)
0 ImagesSynonyms: PN 200-110 (Standard)Isradipine (Standard) is the analytical standard of Isradipine. This product is intended for research and analytical applications. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease.
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Norverapamil-d6 hydrochloride
0 ImagesCat. No.: HY-W699430CAS No.: 1329651-21-9Synonyms: (±)-Norverapamil-d6 hydrochloride; D591-d6 hydrochlorideNorverapamil-d6 ((±)-Norverapamil-d6) hydrochloride is deuterium labeled Norverapamil (hydrochloride). Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
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Ranolazine (Standard)
0 ImagesCat. No.: HY-B0280RCAS No.: 95635-55-5Synonyms: CVT 303 (Standard); RS 43285-003 (Standard)Ranolazine (Standard) is the analytical standard of Ranolazine. This product is intended for research and analytical applications. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor. Antianginal agent.
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Sadopine
0 ImagesCat. No.: HY-120411CAS No.: 111127-62-9Sadopine is an allosteric modulator for dihydropyridine receptor ((-)Sadopine as positive allosteric modulator and (+)Sadopine as negative allosteric modulator). Sadopine interacts with dihydropyridine (DHP)-sensitive L-type calcium channels.
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Ro 18-3981
0 ImagesCat. No.: HY-117055CAS No.: 103295-92-7Ro 18-3981 is a dihydropyridine that inhibits cardiac Ca2+ channels. Ro 18-3981 shows higher inhibitory activity when the cell membrane is in a depolarized state (Vh=-20 mV: IC50=2.3 nM; Vh=-50 mV: IC50=100 nM).
