CV-159 is a unique dihydropyridine Ca2+ antagonist with an anti-calmodulin (CaM) action, and has antiinflammatory activities.
Levamlodipine besylate ((S)-Amlodipine besylate) is a powerful dihydropyridine calcium channel blocker, possessing vasodilation properties and used in the treatment of hypertension and angina[1].
Amlodipine mesylate, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine mesylate can be used for the research of high blood pressure and cancer[1][2][3].
Calcium channel-modulator-1 is a calcium channel modulator; blocks aortic contraction with an IC50 of 0.8 μM.
ILS-920 is a nonimmunosuppressive Rapamycin analog with reduced immunosuppressive activity and potent neuroprotective activity. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 shows 200-fold selectivity for FKBP52 versus FKBP12[1].
Ranolazine is an antianginal medication.Target: Sodium ChannelRanolazine is believed to have its effects via altering the transcellular late sodium current. It affects the sodium-dependent calcium channels during myocardial ischemia in rabbits by altering the intracellular sodium level [1]. Thus, ranolazine indirectly prevents the calcium overload that causes cardiac ischemia in rats [2]. The effects of ranolazine on the NaV 1.7 and NaV 1.8 sodium channels also make it potentially useful in the treatment of neuropathic pain. Ranolazine produced dose-dependant analgesia on mechanical allodynia induced by CFA injection, but had no effect on thermal hyperalgesia [3, 4].
(-)-Denudatin B is an antiplatelet agent. (-)-Denudatin B relaxed vascular smooth muscle by inhibiting the Ca2+ influx through voltage-gated and receptor-operated Ca2+ channels[1]. And (-)-Denudatin B has nonspecific antiplatelet action
Agelenin is a polypeptide composed of 35 amino acids. Agelenin could be isolated from the Agelenidae spider Agelena opulenta. Agelenin has structural similarity to insect-specific calcium channel inhibitor[1].
Darodipine (PY 108-068, PY-108068) is a potent calcium channel antagonist.
(R)-Lercanidipine hydrochloride is the R-enantiomer of Lercanidipine. (R)-lercanidipine hydrochloride is a calcium channel blocker[1].
Etripamil (MSP-2017) is a short-acting L-type calcium-channel antagonist with a rapid onset of action designed for intranasal administration, used to treat Paroxysmal Supraventricular Tachycardia (PSVT). Etripamil (MSP-2017) slows atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells[1][2].
Cavα2δ1&NET-IN-3 (example 216) is an inhibitor of the subunit α2δ of voltage-gated calcium channels (VGCC) and noradrenaline transporter (NET). Cavα2δ1&NET-IN-3 has Kis of 100-500 nM for human α2δ-1 subunit of Cav2.2 calcium channel and NET, respectively[1].
MMK1 is a potent and selective human formyl peptide receptor like-1 (FPRL-1/FPR2) agonist with EC50s of <2 nM and >10000 nM for FPRL-1 and FPR1, respectively. MMK1 is a potent chemotactic and calcium-mobilizing agonist. MMK-1 potently activated phagocytic leukocytes and could enhance Pertussis Toxin (HY-112779)-sensitive production by human monocytes of proinflammatory cytokines IL-1b and IL-6. MMK1 exerts anxiolytic-like activity[1][2][3][4].
Rp-8-Br-cGMPS (Rp-8-bromo-Cyclic GMPS) sodium salt is a potent Ca2+-ATPase activator. Rp-8-Br-cGMPS sodium salt mediates cytosolic Ca2+ reduction by activating Ca2+-ATPase and subsequently removing Ca2+ from the cell[1].
Lacidipine-d10 is the deuterium labeled Lacidipine. Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker[1][2].
Maurocalcine is an agonist of ryanodine receptor (RyR) channel types 1, 2 and 3 with cellular permeability. Maurocalcine induces [3H]ryanodine binding on RyR1 with an EC50 value of 2558 nM. Maurocalcine exhibits a apparent affinity of 14 nM for RyR2. Maurocalcine can be applied to in vivo cell tracking or other cell imaging techniques[1][2][3].
RyRs activator 3 (compound A4) is an effective insecticide against diamondback moths (M. separata) and diamondback moths (P. xylostella). The LC50 value of RyRs activator 3 against diamondback moth is 3.27 mg/L. RyRs activator 3 can bind to ryanodine receptor, increase cytoplasmic Ca2+ concentration, and produce biological toxicity[1].
Ibutilide Fumarate is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm.Target: Calcium ChannelIbutilide is the first 'pure' class III antiarrhythmic drug to become available. Its predominant action is prolongation of the myocardial action potential duration. Intravenous ibutilide 0.01 to 0.025 mg/kg or 1 to 2 mg successfully converted atrial flutter or fibrillation to sinus rhythm in 33 to 49% of patients in 2 placebo-controlled trials involving 439 patients with sustained arrhythmia [1]. Ibutilide appears to be an effective alternative method for rapid conversion of recent-onset AF or AFl. The drug may be particularly useful in patients who have undergone recent cardiac surgery or those who are not ideal candidates for DCC [2].
Flunarizine is a potent dual Na+/Ca2+ channel (T-type) blocker. Flunarizine is a D2 dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects[1][2][3][4][5].
SM-6586 is a calcium channel antagonist and inhibitor of Na+/H+ and Na+/Ca2+ exchange transport, potentially for the treatment of cerebrovasular diseases and hypertension.
Zonisamide sodium is a 1,2 benzisoxazole derivative and the first agent of this chemical class to be developed as an antiepileptic drug.Target: Calcium channel inhibitor; Sodium channel inhibitorZonisamide sodium is a sulfonamide anticonvulsant approved for use as an adjunctive therapy in adults with partial-onset seizures for adults; infantile spasm, mixed seizure types of Lennox-Gastaut syndrome, myoclonic, and generalized tonic clonic seizure. Zonisamide sodium is a 1,2 benzisoxazole derivative and the first agent of this chemical class to be developed as an antiepileptic drug. It has shown activity in various animal models of epilepsy, and although a detailed mode of action awaits clarification it appears to block the propagation/spread of seizure discharges and to suppress the epileptogenic focus [1].Zonisamide sodium 500 mg/day was significantly superior to placebo in reducing the frequency of complex partial seizures (-51% versus -16%), all partial seizures and all seizures, with dose-dependent benefit provided over a 100-500 mg/day dose range. Supporting trials have confirmed significant increases in reduction in median seizure frequency (up to 41%) and responder rates (35-42%) compared with placebo following zonisamide sodium 400-600 mg/day, enabling 20-27% of patients to attain >or=75% reduction in seizure frequency [2].Clinical indications: Epilepsy; Lewy body dementia; Parkinsons diseaseToxicity: Anorexia; Somnolence; Dizziness; Irritability; Confusional state; Depression; Diplopia; Memory impairment
CHF-6366 is a potent M3 muscarinic antagonist and β2-adrenergic receptors agonist with pKi values of 10.4 and 11.4, respectively. CHF-6366 is also a weak calcium channel inhibitor (IC50~50 μM). CHF-6366 inhibits bronchoconstriction in guinea pigs. CHF-6366 can be used to research chronic obstructive pulmonary disease (COPD)[1].
Sipatrigine, a neuroprotective agent, is a glutamate release inhibitor, voltage-dependent sodium channel and calcium channel inhibitor, penetrating the central nervous system. Has potential to treat focal cerebral ischemia and stroke[1][2].
Cav 2.2 blocker 2 is a Cav2.2 calcium channel blocker extracted from patent WO2017046581A1, compound 1. Cav 2.2 blocker 2 can reverses hyperalgesia associated with an injury or inflammation in conjunction with the opioid[1].
Neomycin sulfate is an aminoglycoside antibiotic used for preventing or treating bacterial infections.
N-type calcium channel blocker-1 is an orally active analgesic agent which shows high affinity to functionally block N-type calcium channels with an IC50 of 0.7 μM in the IMR32 assay.
Calciseptine, a natural?neurotoxin?isolated from the black mamba Dendroaspis p. polylepis venom. Calciseptine consists of 60 amino acids with four disulfide bonds. Calciseptine specifically blocks L-type?calcium channel[1].
TTA-Q6 is a selective T-type Ca2+ channel antagonist, used in the neurological disease.
Zonisamide is a 1,2 benzisoxazole derivative and the first agent of this chemical class to be developed as an antiepileptic drug.Target: Calcium channel inhibitor; Sodium channel inhibitorZonisamide is a sulfonamide anticonvulsant approved for use as an adjunctive therapy in adults with partial-onset seizures for adults; infantile spasm, mixed seizure types of Lennox-Gastaut syndrome, myoclonic, and generalized tonic clonic seizure. Zonisamide is a 1,2 benzisoxazole derivative and the first agent of this chemical class to be developed as an antiepileptic drug. It has shown activity in various animal models of epilepsy, and although a detailed mode of action awaits clarification it appears to block the propagation/spread of seizure discharges and to suppress the epileptogenic focus [1].Zonisamide 500 mg/day was significantly superior to placebo in reducing the frequency of complex partial seizures (-51% versus -16%), all partial seizures and all seizures, with dose-dependent benefit provided over a 100-500 mg/day dose range. Supporting trials have confirmed significant increases in reduction in median seizure frequency (up to 41%) and responder rates (35-42%) compared with placebo following zonisamide 400-600 mg/day, enabling 20-27% of patients to attain >or=75% reduction in seizure frequency [2].Clinical indications: Epilepsy; Lewy body dementia; Parkinsons diseaseToxicity: Anorexia; Somnolence; Dizziness; Irritability; Confusional state; Depression; Diplopia; Memory impairment
TMB-8 is a novel Ca 2+ antagonist. TMB-8 may exert inhibitory effects in smooth muscle by blocking Ca 2+ release from intracellular bound stores.