Aleplasinin is an orally active, potent, BBB-penetrated and selectiveSERPINE1 (PAI-1, Plasminogen activator inhibitor-1) inhibitor. Aleplasinin increases amyloid-β (Aβ) catabolism and ameliorates amyloid-related pathology. Aleplasinin improves memory deficiency. Aleplasinin can be used for Alzheimer's disease research[1][2].
7(8)-Dehydroschisandrol A (Compound 4a) is a lignan can be isolated from Schizandra chinensis Baill. 7(8)-Dehydroschisandrol A has a weak inhibitory effect on stress-induced gastric ulcer[1].
RLH-033 is a potent and selective ligand for the sigma 1 recognition site. RLH-033 has high affinity for sigma 1 sites labeled by [3H](+)-pentazocine with a Ki of 50 pM[1].
GR103545 is a potent and selective agonist of the κ-opioid receptor (κ-OR). 11GR103545 is a radiotracer for imaging κ-OR in vivo[1][2].
β-Sheet Breaker Peptide iAβ5 is a potent degrader of cerebral amyloid-beta (Abeta). Abeta deposition is associatied with the Alzheimer disease (AD), due to its related toxicity linked to its beta-sheet conformation and/or aggregation. β-Sheet Breaker Peptide iAβ5 reproducibly induces in vivo disassembly of fibrillar amyloid deposits. Thus, β-Sheet Breaker Peptide iAβ5 prevents and/or reverses neuronal shrinkage caused by Abeta, and reduces the extent of interleukin-1beta positive microglia-like cells that surround the Abeta deposits. β-Sheet Breaker Peptide iAβ5 reduces the size and/or number of cerebral amyloid plaques in AD. β-Sheet Breaker Peptide iAβ5 labeled by hydrophobic benzyl alcohol (HBA) tag, can be used for quantitative assay by showing vivid blue color under acidic conditions[1][2][3].
γ-Aminobutyric acid (4-Aminobutyric acid) is a major inhibitory neurotransmitter in the adult mammalian brain[1][2], binding to the ionotropic GABA receptors (GABAA receptors) and metabotropic receptors (GABAB receptors)[2].
POP-IN-1 (Compound 12h) is a potent inhibitor of POP with an Ki of 0.009 μM. POP-IN-1 has the potential for the research of neurodegenerative diseases and cancer progression[1].
Deserpidine (Harmonyl) is an alkaloid isolated from the root of Rauwolfia canescens related to Reserpine. Deserpidine is used as an antihypertensive agent and a tranquilizer. Deserpidine is a competitive angiotensin converting enzyme (ACE) inhibitor. Deserpidine also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex[1][2][3].
[Sar9] Substance P is a potent and selective neurokinin (NK)-1 receptor agonist[1].
Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
Propoxycaine hydrochloride is the hydrochloride salt form of Propoxycaine, a para-aminobenzoic acid ester with local anesthetic activity.Target: sodium channelPropoxycaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses. This results in a loss of sensation.
Dynorphin B 29 (Leumorphin) (pig) is a petide. Dynorphin B 29 (pig) can interact with multiple receptors in the brain, as well as in isolated tissue systems. Dynorphin B 29 (pig) can be used for the research of immunoreaction[1].
Sigma-2 receptor antagonist 1 is a sigma-2 (σ-2) receptor antagonist.
4-tert-Octylphenol, a endocrine-disrupting chemical, is an estrogenic drug. 4-tert-Octylphenol induces apoptosis in neuronal progenitor cells in offspring mouse brain. 4-tert-Octylphenol reduces bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), resulting in a reduction of neuronal progenitor proliferation. 4-tert-Octylphenol disrupts brain development and behavior in mice[1].
Bupivacaine hydrochloride monohydrate is a NMDA receptor inhibitor. Bupivacaine hydrochloride monohydrate can block sodium, L-calcium, and potassium channels. Bupivacaine hydrochloride monohydrate potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine hydrochloride monohydrate can be used for the research of chronic pain[1][2][3].
NGP555 is a γ-secretase modulator.
Macranthoin G is an inhibitor of p38 MAPK. Macranthoin G protects the cytotoxicity induced by Aβ or hydrogen peroxide in neuronal cells by downregulating p38 MAPK. Macranthoin G can used in study Alzheimer’s Disease[1].
Tandospirone(SM-3997) is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM). IC50 Value: 27±5 nM(Ki) [1]Target: 5-HT1Ain vitro: Tandospirone is most potent at the 5-HT1A receptor, displaying a Ki value of 27 +/- 5 nM. The agent is approximately two to three orders of magnitude less potent at 5-HT2, 5-HT1C, alpha 1-adrenergic, alpha 2-adrenergic, and dopamine D1 and D2 receptors (Ki values ranging from 1300 to 41000 nM). Tandospirone is essentially inactive at 5-HT1B receptors; 5-HT uptake sites; beta-adrenergic, muscarinic cholinergic, and benzodiazepine receptors [1]. 3H-SM-3997 bound rapidly, reversibly and in a saturable manner with high affinity to rat brain hippocampal membranes (Kd = 9.4 nM, Bmax = 213 fmol/mg protein) [2]. in vivo: Chronic treatment with tandospirone, at 0.2 and 1.0mg/kg/day, but not 2.0mg/kg/day, attenuated footshock stress-induced eLAC elevation in the mPFC [3]. Rats were acutely administered tandospirone (0, 0.1, and 1 mg/kg, i.p.). Tandospirone decreased the number of premature responses, an index of impulsive action, in a dose-dependent manner [4].Toxicity: It is not believed to be addictive but it is known to produce mild withdrawal effects (e.g. anorexia) after abrupt discontinuation.
Sortilin antagonist 1 (compound 44) is a sortilin antagonist with an IC50 value of 20 nM for inhibiting Neurotensin (NTS) binds to sortilin. Neurotensin is a sortilin ligand. Sortilin antagonist 1 can be used for the research of neurological disease[1].
MEN11467 is a selective and orally- effective peptidomimetic tachykinin NK1 receptor antagonist.
Cedrin is a natural flavonoid that can be found in Cedrus deodara. Cedrin protects PC12 cells against neurotoxicity induced by Aβ1-42. Cedrin can reduce reactive oxygen species overproduction, increase the activity of superoxide dismutase and decrease malondialdehyde content[1].
Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.
FITC-Dextran is a marker consisting of coupling fluorescein-isothiocyanate to dextran. FITC-Dextrans are polysaccharides comprised of varying lengths of branched glucose molecules which available in molecular weights ranging from 4-70 kDa and can be used to determine solute, ion and protein permeability of the blood-brain barrier (BBB) based on the size of the dextran used[1][2][3].
Neuropeptide Y (22-36), a 15 amino acid peptide, is a fragment of Neuropeptide Y.
Tesmilifene fumarate (DPPE fumarate), an H1C receptor antagonist, potentiates a wide range of cytotoxics and even to offer some protection of normal cells[1][2].
Peripheral Myelin P0 Protein (180-199), mouse, a neuritogenic peptide, is a purified component of murine peripheral nerve myelin[1][2].
4-Aminobenzohydrazide is an irreversible MPO myeloperoxidase inhibitor with an IC50 of 0.3 µM[1]. It is used for the research of subacute stroke[2].
Pilocarpine-d3 (hydrochloride) is deuterium labeled Pilocarpine (Hydrochloride). Pilocarpine Hydrochloride is a potent M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.
Mephenesin is an NMDA receptor antagonist, is a centrally acting muscle relaxant.Target: NMDA receptor
Levitide is a neurohormone-like peptide, can be isolated from skin secretions of the South African frog Xenopus laevis. Levitide comes from preprolevitide, is 88 residues long and contains contains the levitide peptide at the C terminus (Glu-Gly-Met-Ile-Gly-Thr-Leu-Thr-Ser-Lys-Arg-Ile-Lys-Gln-NH2) and the putative signal sequence at the N terminus[1].