(E/Z)-Sulindac sulfide is a potent γ-secretase modulator (GSM). (E/Z)-Sulindac sulfide selectively reduces Aβ42 production in favor of shorter Aβ species. (E/Z)-Sulindac sulfide can be used for researching Alzheimer’s disease[1].
Notopterol is a coumarin extracted from N. incisum. Notopterol induces apoptosis and has antipyretic, analgesic and anti-inflammatory effects. Notopterol is used for acute myeloid leukemia (AML)[1].
Itopride hydrochloride is an AChE inhibitor (acetylcholinesterase) and D2DR inhibitor.Target: AChEItopride is a gastroprokinetic benzamide derivative. The IC50 of itopride with AChE (2.04 +/- 0.27 microM) was, however, 100-fold less than that with BuChE, whereas in the case of neostigmine with AChE (11.3 +/- 3.4 nM), it was 10-fold less. The inhibitory effect of itopride on cholinesterase (ChE) activity in guinea pig gastrointestine was much weaker than that on pure AChE. the IC50s of itopride against ChE activities were found to be about 0.5 microM. The IC50 of itopride for electric eel and guinea pig gastrointestinal AChE inhibition was 200 times and 50 times as large as that of neostigmine, respectively [1].
5-HT7 agonist 2 is a potent 5-HT7 receptor agonist with an IC50 value of 28.7 nM. 5-HT7 agonist 2 can be used for research of central nervous system (CNS) disorders[1].
Fibronectin Type III Connecting Segment Fragment 1-25 is a peptide that is responsible for melanoma cell adhesion, and plays an important role in development of the peripheral nervous system in chicken[1][2].
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control[1].
RS-5773 is a calcium channel inhibitor and a diltiazem congener. RS-5773 has antianginal effect and does not cause excessive hypotension or depression of atrioventricular conduction [1].
BChE-IN-7 (compound 13) is a potent, selective, BBB-penetrated and reversible AChE and BChE inhibitor, with an IC50 of 0.06 μM (BChE). BChE-IN-7 can protect neuronal-like cells from toxic Aβ-species[1].
Immepip is a H3 agonist. Immepip can reduce cortical histamine release. Immepip can be used for the research of neurological diseases[1].
L-Alanine-13C2 (L-2-Aminopropionic acid-13C2) is the 13C-labeled L-Alanine. L-Alanine is a non-essential amino acid, involved in sugar and acid metabolism, increases immunity, and provides energy for muscle tissue, brain, and central nervous system.
μ-Conotoxin SIIIA is a tetrodotoxin (TTX)-resistant sodium channel blocker. μ-Conotoxin SIIIA is a toxic peptide that can be obtained from the venom of Conus snails. μ-Conotoxin SIIIA can be used in the study of neurological diseases, such as neuropathic pain[1].
Propioxatin A, a secondly metabolite produced in microorganism, and is an enkephalinase B inhibitor[1].
GT-2016 is a potent, selective, and brain penetrant histamine H3 receptor antagonist with a Ki of 43.8 nM. GT-2016 displays selectivity against H1 and H2 receptors, and has non-active against histamine methyltransferase[1].
RORγt modulator 2 (Compound 21) is a modulator of retinoid-related orphan receptor γt (RORγt) with the IC50 of <50 nM. RORγt modulator 2 can be used for the research of RORyt mediated diseases such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer[1].
Gly-Leu-Met-NH2 is a C-terminal tripeptide of Substance P (Substance P (HY-P0201)). Substance P is a neuropeptide[1].
AZD-6280 is a selective GABAA(α2/3) receptor modulator, used for treatment of generalized anxiety disorder.
S-(-)-N-trans-Feruloyl normetanephrine is a nature product with weak anti-acetylcholinesterase activity. S-(-)-N-trans-Feruloyl normetanephrine can be isolated from the aerial parts of Bassia indica Wight[1].
Carbamoylcholine chloride is used to study responses mediated by nAChR and mAChR, including smooth muscle contraction, gut motility, and neuronal signaling.IC50 value: 10 to 10,000 nM (Ki)Target: nAChR, mAChRCarbamoylcholine is an analog of acetylcholine that activates acetylcholine receptors (AChR). Carbamoylcholine is an agonist of both nicotinic (nAChR) and muscarinic (mAChR) receptors, with reported Ki values ranging from 10 to 10,000 nM for different receptors and different preparations.
ML252 is a selective inhibitor of potassium channel, targeting to KCNQ2 channel (Kv7.2) (IC50=69 nM). ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively[1][2].
Benzoctamine is an orally active and potent psychoactive agent which possesses tranquillizing properties. Benzoctamine increases the turnover rate of catecholamines. Benzoctamine enhances the [3H]noradrenaline uptake in the rat heart. Benzoctamine also accelerated the disappearance of intracisternally injected [3H]noradrenaline[1].
AMPA receptor modulator-5 (Example 217) is an AMPA receptor modulator. AMPA receptor modulator-5 can be used for research of neurological disease[1].
J-147 is a broad spectrum neuroprotective phenyl hydrazide compound(EC50=60-115 nM) with significant neurotrophic properties related to the induction of brain-derived neurotrophic factor (BDNF).IC50 value: 60-115 nM in vitro assay [1]Target: J-147 has been shown to promotes HT22 and primary cell survival in a dose-dependent manner (EC50 value range of 0.06 – 0.115 μM) when applied to cell exposed to the mitochondrial neurotoxin, iodoacetic acid (IAA), toxicity mediated by the excitatory amino acid glutamate, which causes HT22 cell death by an oxytosis mechanism. In the preclinical in vitro development assays, the EC50 value for J-147-induced cell survival is 25 nM. J-147 was metabolically unstable (highly metabolized) with only 12% of parent remaining after incubation with rat microsomes (phase 1 metabolism).
Corydalmine (L-Corydalmine), an alkaloid isolated from roots of Corydalis Chaerophylla, inhibits spore germination of some plant pathogenic as well as saprophytic fungi[1]. Corydalmine acts as an oral analgesic agent, exhibiting potent analgesic activity[2]. Corydalmine alleviates Vincristine-induced neuropathic pain in mice by inhibiting an NF-κB-dependent CXCL1/CXCR2 signaling pathway[3].
TRPA1 Antagonist 1 is a methylene phosphate prodrug which converts to its active parent drug, a TRPA1 antagonist with an IC50 of 8 nM.
2-Hexyl-4-pentynoic acid ((±)-2-Hexyl-4-pentynoic acid), valproic acid (VPA) derivative, exhibits potential roles of HDAC inhibition (IC50=13 µM) and HSP70 induction. Potent neuroprotective effects. 2-Hexyl-4-pentynoic acid causes histone hyperacetylation and protect against glutamate-induced excitotoxicity in cultured neurons[1].
Phrixotoxin 1, from the venom of the theraphosid spider Phrixotrichus auratus, is a specific peptide inhibitor of Kv4 potassium channel[1][2].
MK-0952 is a selective and orally active PDE4 inhibitor, with an IC50 of 0.53 nM. MK-0952 has the potential for Alzheimer’s disease study[1][2].
DMNPE-4 AM-caged-calcium, photolabile analogues of EGTA, is an extremely effective Ca2+ selective cage, with a Kd for Ca2+ of 48 nM and 19 nM at pH 7.2 and pH 7.4, respectively. DMNPE-4 AM-caged-calcium has a lower affinity for Ca2+ (Kd=~2 nM) after photolysis[1][2].
D-glutamic acid, an enantiomer of L- glutamic acid, is widely used in pharmaceuticals and foods.
alpha-Cobratoxin is a neurotoxin, which can be isolated from the venom of the Thailand cobra. alpha-Cobratoxin exhibits neuromodulatory, antiviral, and analgesic activity. alpha-Cobratoxin also shows potent immunosuppressive activity for acute and chronic multiple sclerosis. alpha-Cobratoxin is further on research in adrenomyeloneuropathy[1].