Glufosinate, a phosphinic acid analogue of glutamic acid, is a herbicide which is converted by plant cells into PT (L-phosphinothricin). Glufosinate exerts neurotoxic activity[1][2].
Aloeresin D is a chromone glycoside isolated from Aloe vera, inhibits β-Secretase (BACE1) activity, with an IC50 of 39 μM[1].
Direct Blue 1 (Chicago Sky Blue 6B) is a counterstain for background autofluorescence in immunofluorescence histochemistry. Direct Blue 1, structurally related to glutamate, is a potent and competitive VGLUT inhibitor without affecting plasma membrane transporters. Direct Blue 1 is the first small molecule PrP ligand capable of inhibiting Aβ binding[1].
Seletracetam (Ucb 44212) is an analog of the antiepileptic agent Levetiracetam. Seletracetam is a small molecule SV2A modulator for the research of epilepsy[1][2][3].
Safinamide (EMD 1195686; FCE 26743) selectively and reversibly inhibits MAO-B with IC50 of 98 nM, exhibits 5918-fold selectivity against MAO-A.IC50 value: 98 nM [1]Target: MAO-BSafinamide (EMD 1195686; FCE 26743; ) is a highly selective and reversible monoamine oxidase type B (MAO-B) inhibitor that increases neostriatal dopamine concentration. In addition, Safinamide (EMD 1195686; FCE 26743; ) is voltage-dependent sodium and calcium channel blocker. Safinamide (EMD 1195686; FCE 26743; ) appears to bind to the batrachotoxin-sensitive site 2 of the voltage-sensitive sodium channels. Safinamide blocks N and L-type calcium channels and inhibits glutamate and aspartate release from synaptic terminals.
Farnesyl pyrophosphate, a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate is a TRPM2 (TRP Channel) agonist, activates TRPM2 opening for ion influx. Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis[1].
NBI-98854 is a potent, highly selective, VMAT2 inhibitor that is effective in regulating the levels of dopamine release during nerve communication.IC50 value:Target: VMAT2NBI-98854 completed a Phase I single ascending dose clinical trial in healthy male volunteers in Canada under an approved Clinical Trial Application with Health Canada.This trial showed NBI-98854 to be generally safe and well tolerated.
D-Hexamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Hexamannuronic acid can be used for the research of pain and vascular dementia[1][2][3][4].
AChE/BChE-IN-4 (BMC-3) is a dual AChE and BChE inhibitor with IC50 values of 792 nM and 2.2 nM against human AChE (hAChE) and human BChE (hBChE), respectively. AChE/BChE-IN-4 can cross the BBB[1].
BI-6C9 is a BH3 interacting domain (Bid) inhibitor, which prevents mitochondrial outer membrane potential (MOMP) and mitochondrial fission, and protects the cells from cell death[1].
Fenadiazole acts as a central nervous system agent to manage insomnia and dreaminess[1].
Raphin1 acetate is an orally bioavailable, selective inhibitor of the regulatory phosphatase PPP1R15B (R15B). Raphin1 acetate binds strongly to the R15B-PP1c holophosphatase (Kd=33 nM), and shows ~30-fold selective in binding R15B-PP1c over R15A-PP1c. Raphin1 acetate crosses the blood-brain barrier, and reduces organismal and molecular deficits in a mouse model of a protein misfolding disease[1].
TC-G 24 (Compound 24) is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM. TC-G 24 can cross the BBB and can be used for studying many diseases such as type 2 diabetes mellitus, stroke, Alzheimer, and other related diseases[1].
DASPEI is a fluorescent dye. DASPEI is a styryl dye that stains mitochondria of live cells. DASPEI has a large fluorescence Stokes shift and is taken up relatively slowly as a function of membrane potential[1].
Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy[1][2].
CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity[1]. CGP 39551 shows measurable inhibitory activity at both L-[3H]-glutamate (Ki=8.4 μM)[2].
GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy[1].
Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits?GABA receptor?with?IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
Manzamine A, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A targets vacuolar ATPases and inhibits Autophagy in pancreatic cancer cells. Manzamine A has antimalarial and anticancer activities. Manzamine A also shows potent activity against HSV-1[1][2][3][4].
Agathisflavone is a flavonoid with antioxidant, anti-inflammatory, antiviral, antiparasitic, cytotoxic, neuroprotective, and hepatoprotective activities. Agathisflavone can improve tissue repair in a spinal cord injury model in rats[1][2][3].
Shatavarin IV is a steroidal saponin, that can be isolated from the roots of Asparagus racemosus (Liliaceae). Shatavarin IV shows anticancer activity. Shatavarin IV elicits lifespan extension and alleviates Parkinsonism in Caenorhabditis elegans[1].
TPN729 is a novel potent, selective phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 2.28 nM, shows better selectivity profile 2.5 times higher than sildenafil against PDE6 and 500 times higher than tadalafil against PDE11; selectively inhibits PDE5 and blocks the degradation of cyclic guanosine monophosphate, and is a promising PDE5 inhibitor providing fewer side effects and better compliance.
Safinamide-d4 (FCE 26743-d4) is the deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
VU0285683 is a selective mGluR5 positive allosteric modulator (PAM). VU0285683 has anxiolytic-like activity in rodent models for anxiety[1].
CHIR 98024 (Compound L) is a glycogen synthase kinase 3 (GSK3) inhibitor with an EC50 of 0.2566 μM[1].
ω-Conotoxin CnVIIA, a 27 amino acid neuropeptide toxin, is a N-type calcium current blocker[1].
β-Amyloid (1-28) is a β-Amyloid protein fragment involved in metal binding. Beta-amyloid is a peptide that forms amyloid plaques in the brains of Alzheimer's disease (AD) patients.
Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively[1]. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase[2]. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis[3]. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway[4].
(-)-GSK598809 is an isomer of GSK598809. GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist.
CP-465022 hydrochloride is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes[1][2].