KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with Kis of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain[1].
Dimethindene is a potent, selective histamine H1 antagonist. Dimethindene impairs cutaneous wound healing (WH). Dimethindene can block K+ currents[1][2].
Pyridoxamine 5′-phosphate is the active form of vitamin B6 bound to phosphoric acid. Pyridoxamine 5′-phosphate is the aminated form of pyridoxal 5'-phosphate hydrate (HY-W011727A) and as co-factor of a variety of enzymes central metabolite, potent antioxidant, vitamin B6 vitamer and enzyme substrate. Pyridoxamine 5′-phosphate can be interconverted with pyridoxal 5'-phosphate hydrate[1].
Chlorphenesin carbamate is a centrally acting skeletal muscle relaxant. Chlorphenesin carbamate can be used for the research of pain and discomfort related to skeletal muscle trauma and inflammation[1]. Chlorphenesin carbamate is a selective blocker of polysynaptic pathways at the spinal and supra-spinal levels[2]. Antinociceptive effect[3].
Flutazolam (MS 4101; Ro 7-6102) is a medicine acts on benzodiazepine receptors of the brain and relieves anxiety or tension.
N-Desmethyl zopiclone-d8 is deuterium labeled Norzopiclone. Norzopiclone is the inactive metabolite of Zopiclone. Norzopiclone has some anxiolytic properties.
Reboxetine is an orally active, potent and selective noradrenaline uptake blocker. Reboxetine can be used for antidepressant research[1].
Isovaleramide is an active principle on central nervous system from Valeriana pavonii, as an anticonvulsant.Target：in vitro: Isovaleramide (300 μM) exhibits a 42% of inhibition of the binding of 3H-FNZ to its sites.in vivo: Isovaleramide at 100 mg/Kg, p.o, evidences a 90% index protection against the maximal electroshock seizure in mice (MES).
Ergtoxin-1 is a potassium channel blocker.Ergtoxin-1 is isolated from the venom of the Mexican scorpionCentruroides noxius. Ergtoxin 1 can blockERG-K+ channels in nerve, heart and endocrine cells[1].
RO5203648 is a potent and highly selective partial agonist of TAAR1 (Trace amine-associated receptor 1) with high affinity. RO5203648 demonstrates a novel paradigm for neuropsychiatric therapeutics[1].
BIMU 8 is a potent and selective 5-HT4 agonist with EC50s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors[1][2].
Galanin (1-30), human is a 30-amino acid neuropeptide, and acts as an agonist of GalR1 and GalR2 receptors, with Kis of both 1 nM.
Geniposide is an iridoid glucoside extracted from Gardenia jasminoides Ellis fruits; exhibits a varity of biological activities such as anti-diabetic, antioxidative, antiproliferative and neuroprotective activities.
α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier[1][2][3].
Lumateperone (ITI-007) is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia[1][2][3].
Schibitubin I is a lignin. Schibitubin I has neuroprotective activity. Schibitubin I can be isolated from the fruits of Schisandra bicolor var. tuberculata[1].
L-365260 is a potent and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance[1][2][3].
4-Chloro Trazodone hydrochloride is an isomer of Trazodone hydrochloride (HY-B0478). Trazodone hydrochloride is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders[1].
nAChR agonist 2 (compound 8) is a selective alpha4beta2 (α4β2) nAChR agonist (Kd=26 nM)[1].
NMDA receptor modulator 3 (Compound 99) is a potent NMDA receptor modulator. NMDA receptor modulator 3 can be used for neurological disorder research[1].
PrPSc-IN-1 is a fluorescent probe, binds to the misfolded protein PrPSc, inhibits its accumulation, with an IC50 of 1.6 μM. Anti-prion activity[1].
Dixyrazine, a phenothiazine derivative, can prevent brain oedema induced by intracarotid injection of protamine sulphate.
Echinacoside is a natural polyphenolic compound, has various kinds of pharmacological activities, such as antioxidative, anti-inflammatory, neuroprotective, hepatoprotective, nitric oxide radical-scavenging and vasodilative ones.IC50 value:Target:in vitro: Echinacoside(ECH) dose dependently inhibited HEWL aggregation, and this inhibition occurred in different fiber-forming stages. ECH could also scavenge the DPPH and OH free radicals in a concentration-dependent manner. ECH could increase viability of rat pheochromocytoma PC12 cells injured by Aβ and suppress the increase in intracellular reactive oxygen species (ROS) triggered by Aβ [1]. Transient treatment with echinacoside inhibits cytochrome c release and caspase-3 activation caused by ensuing rotenone exposure via activating Trk-extracellular signal-regulated kinase (ERK) pathway in neuronal cells [2]. ECH caused a significant increase in cell proliferation, ALP activity, COL I contents, OCN levels and an enhancement of mineralization in osteoblasts at the concentration range from 0.01 to 10nmol·L(-1) (p<0.05), suggesting that ECH has a stimulatory effect on osteoblastic bone formation or has potential activity against osteoporosis [4]. in vivo: In OVX rats, the increases of body weight, serum hydroxyproline (HOP) levels, and the decreases of uterus wet weight and BMD were significantly reversed by ECH treatment [3]. Echinacoside (60 mg/kg) was given intraperitoneally to mice at 1 h prior to GalN/LPS exposure. Pretreatment with echinacoside remarkably improved the survival rate of GalN/LPS-treated mice and attenuated acute hepatotoxicity, as demonstrated by decreased ALT levels and improved histological signs. Echinacoside shows both anti-apoptotic and anti-inflammatory properties, characterized by a substantial inhibition of hepatocyte apoptosis and a significant reduction in the inflammatory markers, including myeloperoxidase, extracellular nucleosomes, high-mobility group box 1, and inflammatory cytokines in the plasma of mice, which may be important mechanisms related to its protective effect [5].
Ro 64-6198 is a nonpeptidic, selective, brain-penetrant agonist of nociceptin/orphanin FQ receptor (NOP receptor/ORL1) with pKi of 9.41; displays >100-fold selectivity for ORL1 over other members of opioid receptor family; elicits dose-dependent anxiolytic-like effects in models of distinct types of anxiety states in rata, with no efficient anti-panic-like activity, absence of anticonvulsant properties, and lack of effects on motor performance and cognitive function at anxiolytic doses (0.3 to 3 mg/kg i.p.). Anxiety Discontinued
Bifeprunox mesylate is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox mesylate is an antipsychotic for the research of schizophrenia[1][2].
RO7185876 is a potent and selective gamma secretase modulator as a potential treatment for Alzheimer's disease.
CI-943 is a potential antipsychotic agent.
γ-Acetylenic GABA (4-Aminohex-5-ynoic acid) is an irreversible inhibitor of GABA-transaminase. γ-Acetylenic GABA can increase the concentration of GABA in rat brain[1][2][3].
PROT-IN-1 (Compound 2) is a proline transporter (PROT) inhibitor (IC50: 1.48 μM). PROT-IN-1 can be used for research of cognitive disorders[1].
Guvacine hydrobromide, an alkaloid found in the nut of Areca catechu, is a potent GABA uptakp inhibitor. Guvacine hydrobromide inhibits rat GAT-1, rat GAT-2 and rat GAT-3 with IC50 values of 39 μM, 58 μM and 378 μM, respectively[1].