Noxiustoxin is a toxin from the venom of the Mexican scorpion Centruroides noxius which block voltage-dependent potassium channel (Kv1.3, IC50 = 360 nM), and calcium-activated potassium channel. Noxiustoxin plays an important role in neuroinflammatory disease[1][2].
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect[1].
Benactyzine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with a Ki of 0.010 mM.
Pargyline is an irreversible non-selective monoamine oxidase (MAO) inhibitor drug (IC50 for MAO-A is 11.52 nM and for MAO-B is 8.2 nM) .
7-Nitroindazole is a selective nNOS inhibitor with antinociceptive and cardiovascular effects. 7-Nitroindazole is a useful tool to evaluate the biological roles of nitric oxide in the central nervous system[1][2].
TACA (trans-4-Aminocrotonic acid) is a potent agonist of GABAA and GABAC receptors (KD= 0.6 μM). TACA also is GABA uptake inhibitor and substrate for GABA-T. TACA produces late biphasic responses in the MPG neurons[1][2][3].
N-Acetylputrescine (NAP) is an endogenous metabolite widely present in animals and plants. N-Acetylputrescine can be used as a biomarker for lung squamous cell carcinoma (SCCL) and Parkinson's disease (PD) for disease diagnosis[1][2][3].
GNE 0723 is a brain permeable positive allosteric modulator of NMDAR, with an EC50 of 21 nM for GluN2A, 7.4 and 6.2 μM for GluN2C and GluN2D, respectively.
Rosavin is isolated from R. rosea, Rosavin shows antidepressant-like, adaptogenic, anxiolytic-like effects in mice model[1].
MM 77 dihydrochloride is a potent postsynaptic antagonist of the 5-HT1A receptor. MM 77 dihydrochloride exhibits anxiolytic-like activity[1][2].
L-Glutamic acid-13C5,15N is the 13C- and 15N-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.
Herkinorin is a potent and selective agonist of µ opioid receptor with a Ki of 45 nM Herkinorin is widely used for pain research[1].
ZM39923 is a JAK3 inhibitor, with a pIC50 of 7.1; ZM39923 also potently inhibits tissue transglutaminase (TGM2) with an IC50 of 10 nM.
BML-259 is a potent cyclin-dependent kinase 5 (Cdk5) inhibitor, with IC50s of 64 and 98 nM for Cdk5 and Cdk2, respectively[1].
β-Spaglumic acid (β-NAAG) is a competitive NAAG peptidase inhibitor (Ki=1 µM) that protects spinal cord neurons from excitotoxicity and hypoxic damage. β-Spaglumic acid is also a selective mGluR3 antagonist (mGluR3 receptor functions to regulate activity-dependent synaptic potentiation in the hippocampus). β-Spaglumic acid can be used in neuroprotection-related studies[1][2].
α-Conotoxin BuIA is a paralytic peptide neurotoxin and a competitive nAChR antagonist, with IC50s of 0.258 nM (α6/α3β2), 1.54 nM (α6/α3β4), 5.72 nM (α3β2), respectively. α-Conotoxin BuIA can be used to distinguish nAChRs containing β2- and β4-subunit, respectively. α-Conotoxin BuIA distinguishes among αxβ2 nAChRs with a rank order potency of α6>α3>α2>α4[1].
Phenibut (β-Phenyl-GABA) hydrochloride is an orally active GABA-B agonist[1]. Phenibut hydrochloride acts as a GABA-mimetic, primarily at GABAB receptors. Phenibut hydrochloride has anxiolytic and nootropic (cognition enhancing) effects[2].
Methiothepin maleate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
Eplontersen is a triantennary N-acetyl galactosamine (GalNAc3-7a)-conjugated antisense oligonucleotide targeting transthyretin (TTR) mRNA to inhibit production of both variant and wild-type TTR protein. Misfolded TTR induces amyloid fibrils formation in the heart and peripheral nerves, leads to amyloid TTR (ATTR) amyloidosis diseases[1][2][3].
Etoposide phosphate disodium (BMY-40481 disodium) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate disodium is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate disodium induces cell cycle arrest, apoptosis, and autophagy[1][2].
Bifemelane hydrochloride is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with a Ki of 4.20 μM, and it also inhibits MAO-B noncompetitively with a Ki of 46.0 μM. Bifemelane hydrochloride has a potent antidepressant activity and can be used for the research of cognitive and emotional disturbances related to cerebrovascular disease[1][2].
1(10)-Aristolen-2-one is an agent with sedative effect[1].
Mesembrine-d3 ((+)-Mesembrine-d3) is the deuterium labeled Mesembrine. Mesembrine ((+)-Mesembrine) a main alkaloid that features an aryloctahydroindole skeleton. Mesembrine is a 5-HT transporter inhibitor with a Ki of 1.4 nM. Mesembrine also inhibits phosphodiesterase 4B (PDE4B) with an IC50 of 7.8 μM[1][2].
Neuromedin S(rat) is a 34-amino acids peptide from rat Neuromedin S. Neuromedin S. Neuromedin S is a neuropeptide isolated from rat brain, acts as ligand for the G protein-coupled receptor FM4/TGR-1[1]
Selurampanel (BGG 492) is an orally active and competitive AMPA receptor antagonist with an IC50 of 190 nM. Selurampanel has reasonable blood-brain barrier penetration. Selurampanel can be used for epilepsy research[1][2].
(S)-Willardiine is a potent agonist of AMPA/kainate receptors with EC50 of 44.8 uM.IC50 value: 44.8 uM(EC50) [1]Target: AMPA/kainate receptor agonistin vitro: The (S)- but not (R)-isomers of willardiine and 5-bromowillardiine were potent agonists, producing rapidly but incompletely desensitizing responses [1]. At a concentration of 1.8 mM, Ca2+ inhibited the currents induced by 100 microM willardiine by approximately 50% [2].in vivo: In newborn mice (P5, histopathology at P10), local injection of the AMPA receptor agonist S-bromo-willardiine at day 5 after birth induced cortical damage and white matter damage, which was reduced in a dose-dependent manner by the AMPA receptor antagonists [3].
BRD6688 is a selective HDAC2 inhibitor. BRD6688 increases H4K12 and H3K9 histone acetylation in primary mouse neuronal cells. BRD6688 crosses the blood brain barrier and rescues the memory defects associated with p25 induced neurodegeneration in contextual fear conditioning in a CK-p25 mouse model[1].
ELOVL6-IN-1 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-1 dose-dependently inhibits mouse ELOVL6 activities, with an IC50 value of 0.350 μM. ELOVL6-IN-1 inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (Ki=994 nM) and palmitoyl-CoA[1].
HEAT (BE2254) hydrochloride is a selective alpha 1 adrenergic receptor antagonist. HEAT hydrochloride, a phenethylamine derivative, shows pKis of 9, 9.1, and 8.57 for alpha 1a, alpha 1b and alpha 1c, respectively[1][2].