Nizubaglustat is an inhibitor of Ceramide Glucosyltransferase or Glucosylceramide Synthase (GCS). Nizubaglustat also inhibits GBA2, involving in neuropathological lysosomal storage disorders[1][2].
MDL-29951 is a novel glycine antagonist of NMDA receptor activation, with Ki of 0.14 μM for [3H]glycine binding in vitro and in vivo.
Ikshusterol 3-O-glucoside is a phytochemical that inhibits PLA2 from snake venoms[1].
5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABAA receptors.
Lupanine (D-Lupanine) hydrochloride is a natural ketonic derivative of Sparteine ((+)-Sparteine (HY-W008350)) with a ganglioplegic activity. Lupanine hydrochloride shows binding affinity for nicotinic receptor (nAChR) with a Ki value of 500 nM[1].
ML193 (CID 1261822) is a potent, selective GPR55 antagonist with IC50 of 221 nM, shows >27-, >145- and >145-fold selectivity for GPR55 over CB1, GPR35 and CB2, respectively; reduces neuronal differentiation in vitro, increases anxiety-like behaviors while causing locomotor impairment by i.c.v. injection at the doses of 0.1 and 1 μg/rat.
L-Glutamic acid-13C5 is the 13C-labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
Piperidolate is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs).
Withaphysalin D is a selective antagonist against the N-methyl-D-aspartate receptor (NMDAR) containing GluN2B. Withaphysalin D can be isolated from water lilies and has neuroprotective properties. Withaphysalin D is able to cross the blood-brain barrier[1].
Phytic acid dodecasodium salt hydrate is a phosphorus storage compound of seeds and cereal grains. Phytic acid has the strong ability to chelate multivalent metal ions, especially zinc, calcium, and iron.
Leptin (116-130) is a bioactive leptin fragment. Leptin (116-130) promotes AMPA receptor trafficking to synapses and facilitate activity-dependent hippocampal synaptic plasticity. Leptin (116-130) prevents hippocampal synaptic disruption and neuronal cell death in models of amyloid toxicity. Leptin (116-130) has the potential for the research of Alzheimer's disease (AD)[1].
Rp-cAMPS triethylammonium salt is an analog of cAMP which acts as a potent, competitive and cell-permeable antagonist of cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 6.05 µM and 9.75 µM, respectively). Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases[1][2][3][4][5].
Rutin hydrate is a flavonol glycoside, able to cross the blood-brain barrier, and acts by inhibiting JNK and ERK1/2 activation and activating mTOR signalling.
3'-Methoxypuerarin (3'-MOP) is an isoflavone extracted from radix puerariae that shows neuron protection activity.
K 01-162 (K162) binds and destabilizes AβO (β-amyloid), with an EC50 of 80 nM. IC50 value: 80 nM (EC50)Target: Amyloid-βin vitro: The active drug candidate K162 (EC50 = 0.080 μM), stabilizes hydrophobic core I of Aβ42 peptide (residues 17-21) to its α-helical conformation by interacting specifically in this region. [1] K01-162 shows full MC65 protection at 125 nM, an EC50 of 80 nM, and no cytotoxicity up to 50 μM. [2]in vivo：K01-162 can reduce the brain amyloid burden that exists in both fibrillar and RIPA-soluble, non-fibrillar forms.[2]
NEP-IN-1 is a neutral endopeptidase (NEP) inhibitor with IC50 of 2 nM for dNEP.
IACS-52825 is a potent and selective DLK inhibitor with Kd of 1.3 nM, useful for the study of chemotherapy-induced peripheral neuropathy[1].
IEM-1460 blocks both AMPA and NMDA glutamate receptor with anticonvulsant effect in vivo[1].
Glycyl-L-histidyl-L-lysine is a tripeptide consisting of glycine, L-histidine and L-lysine residues joined in sequence. Glycyl-L-histidyl-L-lysine is a hepatotropic immunosuppressor and shows anxiolytic effect. Glycyl-L-histidyl-L-lysine and its copper complexes show good skin tolerance[1][2][3].
ANR94 is a potent and selective adenosine A2A receptor (AA2AR) antagonist with an Ki of 46 nM for hAA2AR. ANR94 has the potential for the research of Parkinson's disease[1][2].
Spinorphin is an inhibitor of enkephalin-degrading enzymes. Spinorphin inhibits aminopeptidase, dipeptidyl aminopeptidase III, angiotensin-converting enzyme and enkephalinase. Spinorphin possesses an antinociceptive effect[1].
Riminkefon is a kappa opioid receptor agonist[1].
Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC50s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).
LDN 91946 is a selective, uncompetitive ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitor with Ki of 2.8 uM, exhibits no activity against other cysteine hydrolase (UCH-L3, TGase 2, papain and caspase-3).
Small Cardioactive Peptide B (SCPB), a neurally active peptide, stimulates adenylate cyclase activity in particulate fractions of both heart and gill tissues with EC50s of 0.1 and 1.0 μM, respectively.
Nardosinonediol (Tetrahydronardosinon) is a serotonin transporter (SERT) inhibitor[1].
Guvacine, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively[1].
Baccatin VI is a natural taxoid with antinociceptive activities. Baccatin VI possesses significant antinociceptive activity against p-Benzoquinone-induced abdominal contractions[1].
Chikusetsusaponin Ib has anti-Alzheimer's disease activity and is a potent AChE inhibitor[1].
Vinpocetine(Cavinton; Ethyl apovincaminate) is a selective for PDE1 (IC50 = 21 μM). Also blocks voltage-gated Na+ channels.IC50 value:Target: PDE1; Na+ channel