ca 5

CA-5f is a potent late-stage macroautophagy autophagy inhibitor that works by inhibiting autophagosome-lysosome fusion.

1. Cornuside (Comuside) has immunomodulatory activity . 2. Cornuside suppresses expression levels of cytokine-induced proinflammatory and adhesion molecules in the human endothelial cells. 3. Cornuside can treat myocardial I/R and protect the liver from CCl4-induced acute hepatotoxicity, by reducing oxidative stress and suppressing inflammatory responses. 4. Cornuside has anti-inflammatory activity by downregulations of iNOS and COX-2 due to NF-κB inhibition as well as the negative regulation of ERK1/2, p38, and JNK1/2 phosphorylations in RAW 264.7 cells. 5. Cornuside has protective potential against cerebral ischemic injury, may be due to the suppression of intracellular Ca(2+) elevation and caspase-3 activity, and improvements in mitochondrial energy metabolism and antioxidant properties.

Barnidipine hydrochloride (YM-09730-5 hydrochloride) is a dihydropyridine calcium channel blocker that has an IC50 value of 0.35 nM in potassium-induced tonic contraction of pig coronary artery

Barnidipine (YM-09730-5(Free base)) is a calcium channel blocker.

TGR5 is a potent TGR5(GPCR19) agonist.

Norfluoxetine Hydrochloride (Norfluoxetine HCl) is an active metabolite of fluoxetine. Fluoxetine is an antidepressant drug.

Nantenine is an acetylcholinesterase inhibitor, it functions as an effective antagonist against a wide range of MDMA-induced effects in mice. Nantenine has anticonvulsant effect, which seems attributable to its stimulation and the resultant decrease of Ca

CA 074 is a potent inhibitor of cathepsin B with a Ki value of 2 to 5 nM.CA 074 inhibits ischemic hippocampal neuronal death in primates and attenuates retinopathy and optic neuritis in experimental autoimmune encephalomyelitis induced by SJL/J mice.

Ginsenoside Ro (Chikusetsusaponin V) can reduce TXA2 production, weakly reduce COX-1 and TXAS activities, and has antiplatelet effects as a Ca2+ antagonist with an IC50 of 155 μM.

hCAIX XII-IN-5 (Coumarin 9a) is an inhibitor of carbonic anhydrase (CA) with excellent selectivity for hCA IX XII, displaying Kis of 93.3 nM and 85.7 nM over hCA I and hCA II, respectively. It exhibits anti-proliferative activities in cancer cells, delaying the cell cycle and inducing apoptosis [1].

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg/kg, respectively). Zonisamide (40 mg/kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).

PPADS tetrasodiuma is a potent P2X receptor antagonist and inhibitor of the inverse mode of Na Ca²⁺ exchange in guinea pig airway smooth muscle and is neuroprotective against glutamate NMDA toxicity.PPADS tetrasodiuma inhibits P2X1, P2X-2, P2X-3, and P2X- 5. 5.

DPX-3778 is the triethanolamine salt of 3-(p-chlorophenyl)-6-methoxy-s-triazine-2,4(1H,3H) dione, at concentrations of 0.124-2.48 μM enhanced ca. 4-5-fold the proliferation of tobacco (Nicotiana tabacum L. cv. Wisconsin 38) callus cultured in the presence

COX-2-IN-30, a benzenesulfonamide derivative, is an orally active, dual inhibitor of cyclooxygenase-2 (COX-2; IC50 = 49 nM) and cyclooxygenase-1 (COX-1; IC50 = 10.4 μM), as well as 5-lipoxygenase (5-LOX; IC50 = 2.4 μM). Additionally, it inhibits the transmembrane isoforms of human carbonic anhydrase IX and XII with nanomolar class Ki values. Demonstrating analgesic and anti-inflammatory properties, COX-2-IN-30 is devoid of acute gastric effects, avoiding ulcerogenic activity [1].

AC-264613 is an agonist of the GPCR protease-activated receptor 2 (PAR2). AC-264613(AC264613) suppresses interferon regulatory factor 5 and decreases interleukin-12p40 production by lipopolysaccharide-stimulated macrophages. AC-264613(AC264613) activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 30 to 100 nM.

N-Salicyloyltryptamine(STP) is a tryptamine analogue with anticonvulsant, anti-inflammatory, analgesic, and vasorelaxation effect. N-Salicyloyltryptamine acts as the voltage-dependent Na +, Ca 2+, and K + ion channels inhibitor which inhibits K + currents with an IC 50 value of 34.6 μM ( /to) [1] - [5].

RS-93522 is an antagonist of calcium channel. RS-93522 had the additional property of inhibiting phosphodiesterase activity in myocardial homogenates (IC50 = 1.6 x 10(-5)M), the potency and efficacy of phosphodiesterase inhibition was similar to that for

YK-5-252 is a dual action combretastatin A-4 (CA-4) prodrug which releases CA-4 through a disulfide bond cleavage mechanism and contains a near-infrared (NIR) fluorophore.

Efonidipine HCl (NZ-105) serves as both a T-type and L-type calcium channel blocker. This compound, distinct from other calcium channel blockers, notably increases N(6), 2'-O-dibutyryladenosine 3',5'-cyclic monophosphate (dbcAMP)-induced StAR mRNA and DHEA-S production in NCI-H295R adrenocortical carcinoma cells, actions reflective of adrenocorticotropic hormone. Efonidipine uniquely inhibits calcium channels by merging tonic and use-dependent blocking methods. Its inhibitory concentrations (IC50) for I(Ca(T)) and I(Ca(L)) are 0.35 micromol/l and 1.8 nmol/l, respectively. Clinically, efonidipine administered to hypertensive patients undergoing chronic hemodialysis (20-60 mg, twice daily) demonstrated comparable blood pressure control to amlodipine (2.5-7.5 mg, once daily) over a 12-week period without significantly altering pulse rate. Furthermore, efonidipine significantly improved left ventricular ejection fraction in heart failure models without affecting blood pressure, in addition to lowering the heart rate by about 10%.

Acetylshikonin can effectively inhibit tumor cells, it can be used to treat hepatocellular carcinoma cells expressing hepatitis B virus X protein (HBX) by inducing ER stress , an oncoprotein from hepatitis B virus. Acetylshikonin inhibits the production of eicosanoid, is due to the attenuation of cytosolic phospholipase A(2) membrane recruitment via the decrease in [Ca(2+)](i) and to the blockade of cyclooxygenase and 5-lipoxygenase activity.

(+)-5-Methoxyisolariciresinol displays significant antioxidant activities, with the IC(50) value in the range of ca. 42 to 49 microg/ml.

Zonisamide (AD 810), a sulfonamide anticonvulsant, is approved for use as an adjunctive treatment in adults with partial-onset seizures. It may inhibit a carbonic anhydrase although this is not one of the main mechanisms of action. Zonisamide may act by blocking repetitive firing of voltage-gated sodium channels results in a reduction of T-type calcium channel currents, or by binding allosterically to GABA receptors. This latter action may lower the uptake of the inhibitory neurotransmitter GABA while increasing the uptake of the excitatory neurotransmitter glutamate.

Zonisamide sodium is a 1,2 benzisoxazole derivative. It is the first agent of this chemical class to be developed as an antiepileptic drug.