ca2+ channel

Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2 (EC50s: 14.23 μM and 3.34 μM) and is used as a potential treatment for motor nerve terminal dysfunction.

Calcium Channel antagonist 2 is a calcium channel antagonist (IC50=5-20 μM) that can be used to study diseases due to Ca2+ channels like pain and diabetes.

KCa1.1 channel activator-2, a hybrid derivative of Quercetin, selectively stimulates the vascular KCa1.1 channels. This compound demonstrates significant myorelaxant activity.

T-Type calcium channel inhibitor 2 (compound 6g) is a potent inhibitor of the T-type calcium channel, specifically acting on Cav3.1 (α1G) with an IC50 of 31.0 μM, Cav3.2 (α1H) with an IC50 of 83.1 μM, and Cav3.3 (α1I) (α1H). T-Type calcium channel inhibitor 2 exhibited cytotoxicity against A549 and HCT-116 cells with IC50s of 5.0 μM and 6.4 μM, respectively.

Sodium Channel Inhibitor 2 [Sodium Channel inhibitor 2] is a blocker of sodium channels.

Compound 4H is a potent carbonic anhydrase inhibitor with an IC50 value of 0.033 μM [1].

KCa2 channel modulator 2 (compound 2q) is an effective, subtype-selective K Ca 2 channel positive modulator with similar potency on the human K Ca 2.3 channel and rat K Ca 2.2a subtypes, exhibiting EC50 values of 0.60 μM and 0.64 μM, respectively [1].

Thapsigargin is a natural product, an inhibitor of sarcoplasmic/endoplasmic reticulum Ca2+ ATPase (SERCA) and an endoplasmic reticulum stress inducer. Thapsigargin increases cytoplasmic calcium concentration by blocking the ability of cells to pump calcium into the sarcoplasmic and endoplasmic reticulum.

Penfluridol (TLP-607) is a highly potent antipsychotic.

Nicardipine hydrochloride (YC-93 Hydrochloride) is the hydrochloride salt form of nicardipine, a synthetic derivative of nitrophenyl-pyridine and potent calcium channel blocker, Nicardipine (Nifedipine Family) blocks calcium ions from certain cell walls and inhibits contraction of coronary and peripheral arteries, resulting in lowered oxygen requirements for heart muscle and decreased arterial contraction and spasm. It is used clinically as a cerebral and coronary vasodilator.

Tetracaine hydrochloride (Amethocalne HCl) (Pontocaine), a potent local anaesthetic, is a channel function allosteric inhibitor. It is primarily used as an antipruritic and topically in ophthalmology, and it has been used for surface and spinal anesthesia.

Flufenamic acid (Arlef) is an anthranilic acid derivative with analgesic, anti-inflammatory, and antipyretic properties. It is used in musculoskeletal and joint disorders and administered by mouth and topically.

Ranolazine dihydrochloride (Ranolazine 2HCl) , an antianginal agent, can treat arrhythmia via a novel mechanism of action (inhibition of the late phase of the inward sodium current), and do not affect blood pressure or heart rate.

Gabapentin hydrochloride (Neurontin HCl) is a GABA analogue, used to treat seizures and neuropathic pain.

Nitrendipine (BAY-E-5009) is a calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.

Lomerizine dihydrochloride (KB-2796) is an antagonist of L- and T-type voltage-gated calcium channels used to treat migraine.

Nifedipine (Procardia) is a dihydropyridine calcium channel blocking agent. Nifedipine inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation of the main coronary and systemic arteries and decreasing myocardial contractility. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in some multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents.

Topiramate (RWJ 17021) is a unique antiseizure medication that is used in the treatment of partial and generalized seizures. Topiramate has been rarely associated with hepatic injury and largely when used in combination with other anticonvulsant medications.

Manidipine (Iperten), a calcium channel blocker, which is dihydropyridine type. It is utilized

Nimodipine (BAY-e 9736), a 1, 4-dihydropyridine calcium channel blocker, acts primarily on vascular smooth muscle cells.

Dantrolene sodium (Lapatinib ditosylate monohydrate) salt is a skeletal muscle relaxant and can interfere with excitation-contraction coupling in the muscle fiber. It is used for the treatment of spasticity and other neuromuscular abnormalities. Its mechanism of action is may not central, but dantrolene is usually grouped with the central muscle relaxants.

Ranolazine (RS 43285-003) is a calcium uptake inhibitor via the sodium calcium channel, used to treat chronic angina. It affects the sodium-dependent calcium channels during myocardial ischemia in rabbits by altering the intracellular sodium level.

Levamlodipine (S-amlodipine) belongs to the dihydropyridine group of calcium channel blockers. Levamlodipine, also known as S-amlodipine, is a pharmacologically active enantiomer of amlodipine, an antihypertensive and anti-anginal medication. The names S-amlodipine and levamlodipine may be used interchangeably as both substances are the same, however, with differing nomenclature. As a racemic mixture, amlodipine contains (R) and (S)-amlodipine isomers, but only (S)-amlodipine as the active moiety possesses therapeutic activity.

Manidipine dihydrochloride (Manidipine 2HCl) is a potent calcium channel blocker for Ca2+ current(IC50=2.6 nM).

Lercanidipine hydrochloride (Corifeo) is a calcium channel blocker of the dihydropyridine class.

Fasudil hydrochloride (HA-1077) is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively.

Verapamil hydrochloride (Verapamil HCl) is a calcium channel blocker that is a class IV anti-arrhythmia agent.

Lacidipine (SN-305) is a lipophilic dihydropyridine calcium antagonist with an intrinsically slow onset of activity. Due to its long duration of action, lacidipine does not lead to reflex tachycardia. It displays specificity in the vascular smooth muscle, where it acts as an antihypertensive agent to dilate peripheral arterioles and reduce blood pressure.

Flunarizine dihydrochloride (R14950) is a selective calcium entry blocker with calmodulin binding properties and histamine H1 blocking activity. Flunarizine dihydrochloride (R14950) is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of epilepsy.

Ethacrynic acid (Edecrin) is a nonsulfonamide loop diuretic that inhibits the activity of the Na+/K+/2Cl- cotransporter NKCC2 in the thick ascending limb of the loop of Henle. It also inhibits glutathione S-transferase and Wnt signalling, producing cytotoxicity in chronic lymphocytic leukaemia cells and other tumour cells.

Isradipine (PN 200-110) is a dihydropyridine calcium channel blocker with antihypertensive and vasodilator activities. Isradipine blocks calcium entry through calcium ion channels in coronary and peripheral vascular smooth muscle, dilating coronary arteries and peripheral arterioles. This action increases oxygen delivery by enhancing blood flow and decreases oxygen requirements by reducing total peripheral resistance.

Gabapentin (Neurontin) is an Anti-epileptic Agent. The physiologic effect of gabapentin is by means of Decreased Central Nervous System Disorganized Electrical Activity.

Niflumic acid (Nifluril) is a Ca2+-activated Cl- channel blocker and an analgesic and anti-inflammatory agent used in the therapy of rheumatoid arthritis.

Dantrolene depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor 1 and decreasing intracellular calcium concentration. Ryanodine receptors mediate the release of calcium from the sarcoplasmic reticulum, an essential step in muscle contraction. Dantrolene sodium hemiheptahydrate (Sodium dantrolene) is the sodium salt form of dantrolene, a hydantoin derivative, and direct-acting skeletal muscle relaxant.

Acetylcholine Chloride is the chloride salt form of acetylcholine, a synthetic, quaternary amino alcohol with cholinergic properties. Acetylcholine chloride (Pilofrin) mimics the parasympathomimetic effect of the endogenous compound acetylcholine. Administered as an ophthalmic solution, this drug stimulates the cholinoceptors in the sphincter muscle of the iris, causing the pupil to constrict.

Tanshinone IIA sulfonate sodium (Tanshinone IIA sodium sulfonate) is a water-soluble derivative of tanshinone IIA extracted from Savia miltiorrhiza; a potent negative allosteric modulator of the human purinergic receptor P2X7. Tanshinone IIA sulfonate sodium (12.5 μM) inhibits hypoxia-induced PKG and PPAR-γ downregulation in PASMCs and distal pulmonary arteries of rats.

Nisoldipine (BAY-k 5552) is a dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent.

Benidipine hydrochloride (Coniel) , a hydrochloride salt form of benidipine, is used as a blocker of dihydropyridine calcium channel.

Amifampridine (3,4-Diaminopyridine) is primarily used to treat rare muscle diseases. It blocks potassium channel efflux in nerve terminals, increasing action potential duration, which allows Ca2+ channels to remain open longer and enhances acetylcholine release to stimulate muscles at the end plate.

Gallopamil hydrochloride (Methoxyverapamil hydrochloride) is an antagonist of phenylalkylamine calcium. Gallopamil hydrochloride can be used in antiarrhythmic and vasodilator studies.

L-Ascorbic acid (Vitamin C) is a natural product that is a potent reducing agent and antioxidant. L-Ascorbic acid functions in fighting bacterial infections, in detoxifying reactions, and in the formation of collagen. L-Ascorbic acid is used in the treatment of scurvy.

Ethosuximide (Zarontin) is an anticonvulsant, blocks the low voltage-activated T-type calcium channel used in the treatment of absence seizures unaccompanied by other types of seizures.

L-Phenylalanine (3-Phenyl-L-alanine) is an essential amino acid and the precursor of the amino acid tyrosine, acts as an antagonist at α2δ calcium channels.

Diltiazem hydrochloride (RG 83606 HCl) is a benzothiazepine calcium channel blocking agent with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.

Bupivacaine hydrochloride (Vivacaine) is a long-acting, amide-type local anesthetic. Bupivacaine hydrochloride reversibly binds to specific sodium ion channels in the neuronal membrane, resulting in a decrease in the voltage-dependent membrane permeability to sodium ions and membrane stabilization; inhibition of depolarization and nerve impulse conduction; and a reversible loss of sensation.

Butamben (Butyl 4-aminobenzoate) is a long-duration local anesthetic used for the treatment of chronic pain.

Drotaverine hydrochloride is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor，and is an antispasmodic drug, used to enhance cervical dilation during childbirth. Drotaverine hydrochloride is structurally related to papaverine

Cilnidipine (FRC-8653)(FRC8653) is a dual L- and N-type calcium channel blocker and displays antihypertensive, sympatholytic and neuroprotective activity.

Tetrandrine (Sinomenine A) is a naturally occurring biphenylisoquinoline alkaloid, a calcium channel inhibitor. Tetrandrine inhibits voltage-gated calcium channels (ICa) and Ca2+-activated potassium channels.

Strontium ranelate (S12911), a strontium (II) salt of the ranelic acid, is a medication for osteoporosis. Studies indicate it can also slow the course of osteoarthritis of the knee. The drug is unusual in that it both increases deposition of new bone by osteoblasts and reduces the resorption of bone by osteoclasts. It is therefore promoted as a dual action bone agent (DABA) indicated for use in the treatment of severe osteoporosis.