ca1

Bucladesine sodium (DC2797) is a cAMP analog with cell-permeable properties. Bucladesine sodium is also a cAMP-dependent protein kinase (PKA) activator and a phosphodiester (PDE) inhibitor. Bucladesine sodium has anti-inflammatory activity.

Methocarbamol (AHR 85) is a centrally acting muscle relaxant whose mode of action has not been established. It is used as an adjunct in the symptomatic treatment of musculoskeletal conditions associated with painful muscle spasm.

MEDICA16 is a selective agonist for GPR40 as well as a partial agonist for GPR120. MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle with an increase in insulin sensitivity.

BRCA1-IN-1 is a novel small-molecule-like inhibitor of BRCA1 with an IC50 of 0.53 μM and a Ki of 0.71 μM.

BRCA1-IN-2 is a cell membrane-crossing BRCA1 protein-protein interaction (PPI) inhibitor with antitumor activity that acts by disrupting the interaction of BRCA1 (BRCT)2 with proteins.

ABCA1 inducer 1, a non-lipid inducer of ABCA1, enhances ABCA1 expression in E3 4FAD mice expressing human APOE 3 4, augments the lipidation of apolipoprotein (APOE), and reverses various Alzheimer's disease (AD) phenotypes without increasing triglycerides.

MCA17-1 exhibits superior bioactivity compared to the positive control, obeticholic acid (OCA), in the treatment of liver fibrosis.

TCA1 (TCA 1) is a small molecule with activity against drug-resistant and persistent tuberculosis.

KCa1.1 Channel Activator-1, a hybrid derivative of Quercetin, selectively stimulates the vascular KCa1.1 channels while also blocking CaV1.2 channels. Additionally, it demonstrates weak myorelaxant activity.

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

The Anti-BRCA1 Antibody (BR64) is a mouse IgG1, κ chimeric antibody that specifically targets human BRCA1. The recommended isotype control for the Anti-BRCA1 Antibody (BR64) is the Mouse IgG1 kappa, Isotype Control.

Anti-CA19-9 Antibody (1116-NS-19-9) is a mouse IgG1, κ chimeric antibody designed to target human CA19-9. The recommended isotype control for this antibody is Mouse IgG1 kappa, Isotype Control.

Benzthiazide (Lemazide) is used in the therapy of edema and hypertension. Like other thiazides, benzthiazide accelerates water loss from the body (diuretics). They inhibit Na+ Cl- reabsorption from the distal convoluted tubules in the kidneys. Thiazides also cause loss of potassium and an increase in serum uric acid. Thiazides are often used to treat hypertension, but their hypotensive effects are not necessarily due to their diuretic activity. Thiazides have been shown to prevent hypertension-related morbidity and mortality although the mechanism is not fully understood. Thiazides cause vasodilation by activating calcium-activated potassium channels (large conductance) in vascular smooth muscles and inhibiting various carbonic anhydrases in vascular tissue.

Unifiram is a nootropic agent.1It increases acetylcholine (ACh) release in the rat cerebral cortexin vivoand induces a long-lasting increase in the amplitude of field excitatory postsynaptic potentials (fEPSPs) in the rat hippocampal CA1 region (EC50= 27 nM). It does not bind to serotonin (5-HT), dopamine, muscarinic, nicotinic, adrenergic, glutamate, histamine, opioid, or GABA receptors at 1 μM. Unifiram (0.1 mg kg) improves memory in non-memory-impaired rats in a social learning test.2It also prevents memory deficits induced by the anticholinergic agent scopolamine, nicotinic receptor antagonist mecamylamine, GABABreceptor agonist baclofen, or α2-adrenergic receptor agonist clonidine in the passive avoidance test in mice when administered at a dose of 0.01 mg kg and prevents memory deficits induced by the AMPA kainate glutamate receptor antagonist NBQX at 0.1 mg kg.1 1.Romanelli, M.N., Galeotti, N., Ghelardini, C., et al.Pharmacological characterization of DM232 (unifiram) and DM235 (sunifiram), new potent cognition enhancersCNS Drug Rev.12(1)39-52(2006) 2.Ghelardini, C., Galeotti, N., Gualtieri, F., et al.The novel nootropic compound DM232 (unifiram) ameliorates memory impairment in mice and ratsDrug Develop. Res.56(1)23-32(2002)

In the central nervous system, 2-Arachidonoylglycerol is a second endogenous cannabinoid ligand

N-Stearoyltyrosine (N-(1-Oxooctadecyl)-L-tyrosine) is an analog of Anandamide. It exhibits neuroprotective effects by safeguarding the CA1 region of the hippocampus in a gerbil ischemia-reperfusion model. Additionally, N-Stearoyltyrosine inhibits free radical generation, enhances antioxidant capacity, and reduces IR-induced apoptosis (cell apoptosis).

WAY-100635 is a potent 5-HT 1A receptor antagonist with an IC50 = 0.91 nM that abrogates the reduction in hippocampal CA1 pyramidal neuron firing frequency during conditioned reflexes; it also acts as a dopamine D4 receptor agonist with an affinity of 3.3 nM.

UBP714 is a derivative of the NMDA receptor negative allosteric modulator UBP608. It also enhanced NMDAR mediated field EPSPs in the CA1 region of the hippocampus. UBP714 is a novel template for the development of potent and subunit selective NMDAR potent

S-8510 is a GABA-A receptor inverse agonist. S-8510 selectively potentiated pentylenetetrazol-induced convulsion without affecting minimal electroconvulsive shock- or strychnine-induced convulsion in ddY mice. S-8510 ameliorated memory impairment induced

(E)-Ajoene is a disulfide that has been found inA. sativumand has diverse biological activities.1,2,3,4It is active against Gram-positive and Gram-negative bacteria (MICs = 10-250 and 150->500 μg/ml, respectively) and fungi (MICs = 15-50 μg/ml).1(E)-Ajoene inhibits proliferation of a variety of cancer cells, including MDA-MB-231 breast, HeLa cervical, and WHCO1 esophageal cancer cells (IC50s = 18.6, 61, and 39.2 μM, respectively).2It also inhibits human glutathione reductase andT. cruzitrypanothione reductase when used at a concentration of 200 μM.3(E)-Ajoene (25 mg/kg) is neuroprotective in a gerbil model of ischemia-reperfusion injury, reducing reactive astrocytosis and microgliosis in the hippocampal CA1 region.4 1.Yoshida, H., Iwata, N., Katsuzaki, H., et al.Antimicrobial activity of a compound isolated from an oil-macerated garlic extractBiosci. Biotechnol. Biochem.62(5)1014-1017(1998) 2.Kaschula, C.H., Hunter, R., Hassan, H.T., et al.Anti-proliferation activity of synthetic ajoene analogues on cancer cell-linesAnticancer Agents Med. Chem.11(3)260-266(2011) 3.Gallwitz, H., Bonse, S., Martinez-Cruz, A., et al.Ajoene is an inhibitor and subversive substrate of human glutathione reductase and Trypanosoma cruzi trypanothione reductase: Crystallographic, kinetic, and spectroscopic studiesJ. Med. Chem.42(3)364-372(1999) 4.Yoo, D.Y., Kim, W., Nam, S.M., et al.Neuroprotective effects of Z-ajoene, an organosulfur compound derived from oil-macerated garlic, in the gerbil hippocampal CA1 region after transient forebrain ischemiaFood Chem. Toxicol.721-7(2014)

NAP-1 is a compound with anesthetic activity.1 It increases paired-pulse inhibition in the CA1 region of rat hippocampal brain slices when used at a concentration of 100 μM. NAP-1 also induces loss of righting reflex in tadpoles (EC50 = 0.53 μM).References NAP-1 is a compound with anesthetic activity.1 It increases paired-pulse inhibition in the CA1 region of rat hippocampal brain slices when used at a concentration of 100 μM. NAP-1 also induces loss of righting reflex in tadpoles (EC50 = 0.53 μM). References

Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. It enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy [1].

Ginkgolide J (BN 52024) has neuroprotective activity, it can prevent A beta(1-42) induced inhibition of long-term potentiation in the CA1 region of mouse hippocampal slices.

GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of generalized tonic-clonic seizures induced by 4-aminopyridine (4-AP) when administered at doses of 25 and 50 mg kg. GYKI 52466 (30 mg kg) prevents neuronal damage in the CA1 region of the hippocampus in a rat model of global ischemia-reperfusion injury induced by four-vessel occlusion.