Tebufelone (NE-11740), a nonsteroidal anti-inflammatory drug (NSAID), is a selective dual COX-2/5-lipoxygenase inhibitor. Tebufelone displays potent anti-inflammatory, analgesic and anti-pyretic properties[1][2].
AP102 is a dual SSTR2/SSTR5-specific somatostatin analog (SSA). AP102 is a disulfide-bridged octapeptide SSA containing synthetic iodinated amino acids. AP102 binds with subnanomolar affinity to SSTR2 and SSTR5 (IC50: 0.63 and 0.65 nM, respectively). AP102 does not bind to SSTR1 or SSTR3. AP102 can be used for acromegaly and neuroendocrine tumors research[1].
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor[1].
Ac-Leu-Arg-AMC is a fluorogenic peptide substrate.
Fmoc-1,6-diaminohexane is an analog of Osw-1 which can be used to treat Alzheimer's disease and cancer, extracted from patent US 20140135279 A1.
NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with high affinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively[1].
N-Arachidonoyl-GABA is one member of a new class of lipoamino acids related to anandamide identified in bovine brain. N-Arachidonoyl-GABA displays analgesic activity[1].
A novel potent, selective, allosteric and orally active dopamine D1 receptor potentiator with Kb of 26 nM; induces a 21-fold leftward shift in the cAMP response to dopamine in HEK293 cells, 30-fold less potent at rat and mouse D1 receptors and is inactive at the human D5 receptor; robustly (∼10-fold) increases locomotor activity in habituated hD1 mice (3-20 mg/kg), also acts synergistically with L-DOPA to reverse the strong hypokinesia caused by reserpine.
Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias[1].
SKF 38393 hydrobromide is a selective agonist of the dopamine D1 receptor (D1DR) with an IC50 of 110 nM[1].
Perphenazine sulfoxide is a sulphoxide metabolite of Perphenazine, formed by the oxidation of Perphenazine[1].
5-HT3 antagonist 1 is a potent and selective antagonist of serotonin 3 (5-HT3) receptor.
Isoasiaticoside is a pentacyclic triterpene saponin that can be isolated from Centella asiatica. Isoasiaticoside has potential neuroprotective effects in the 6-OHDA (HY-B1081)-induced PC12 cell model[1].
Quetiapine (hemifumarate)-d8 is the deuterium labeled Quetiapine hemifumarate[1]. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[2].
Prolactin-Releasing Peptide (12-31), bovine is a peptide fragment of prolactin-releasing peptide (PrRP). PrRP is RF-amide peptides expressed in brain areas involved inpain modulation. Prolactin-Releasing Peptide (12-31), bovine can be used for the research of nervous system disease[1].
CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells[1]. CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways.[2].
Irampanel (BIIR 561) is an AMPA receptor and voltage-dependent sodium channel blocker. Irampanel inhibits kainate-induced currents in rat cortical neurons[1].
PEPA is an allosteric modulator of AMPA receptors; binds to the GluA2o and GluA3o LBDs and can be utilized as an indicator of AMPA receptor heterogeneity.IC50 value:Target: AMPAR modulatorin vitro: PEPA dose-dependently potentiated AMPA-induced increase of [Ca2+]i. In 90% (72 out of 80) of the cells in which cyclothiazide acts, PEPA potentiated the increased [Ca2+]i induced by AMPA with pronounced cell-to-cell variation in rat hippocampal cultures [1]. PEPA bound to the binding domains of the GluA2 and GluA3 flop isoforms of AMPA receptors [2]. coapplication of AMPA with PEPA protected hippocampal CA1 neurons from brain ischemia-induced death. Coapplication of AMPA with PEPA could prevent downregulated expression of GluR2 subunit caused by ischemia and increase BDNF expression via Lyn-ERK1/2-CREB signaling [4].in vivo: PEPA (3, 10, 30mg/kg body weight) or vehicle was intraperitoneally administered into stressed mice once before the first extinction session. The significant decrease of the freezing response in the extinction sessions was only seen in the 30mg/kg PEPA-administered stressed mice, compared with vehicle-administered stressed mice [3].
nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research[1].
Lofexidine is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal[1][2].
Unifiram (DM232) is acts as a potent cognition enhancer through the activation of the AMPA-mediated neurotransmission system. Unifiram (DM232) has the potential for amnesia prevention and neurodegenerative disorder research[1][2].
Yohimbine-d3 is the deuterium labeled Yohimbine (HY-12715)[1].
Anle138b is a novel oligomer modulator.
PE 22-28 is a TREK-1 inhibitor with IC50 value of 0.12 nM. PE 22-28 also is a 7 amino-acid peptide that is used as a core sequence for preparing analogs by chemical modifications and also by substitution of amino-acids. PE 22-28 can be used for the research of depression[1].
DL-Laudanosine, an Atracurium and Cisatracurium metabolite, crosses the blood–brain barrier and may cause excitement and seizure activity[1].
2-PAT, an analogue of Rasagiline and Selegiline, a reversible MAO-A inhibitor with an IC50 of 0.721 µM. 2-PAT is an inactivator of MAO-B with an IC50 of 14.6 µM. 2-PAT has the potential for Parkinson’s disease and depression research[1].
UPF-648 sodium salt is a potent kynurenine 3-monooxygenase (KMO) inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO inhibition); ineffective at blocking KAT activity.IC50 value: 1 uM(81 ± 10 % inhibition) [1]Target: KMO inhibitorin vitro: BFF 122 inhibited KAT activity almost completely at both 1 and 0.1 mM. The effect was still remarkable at 0.01 mM (70 ± 1 % inhibition). At the same three concentrations, BFF 122 did not affect KMO activity significantly. In contrast, UPF 648 totally blocked KMO at 0.1 and 0.01 mM and was still highly active at 0.001 mM (81 ± 10 % inhibition), but the compound was essentially ineffective at blocking KAT activity [1]. UPF 648 binds close to the FAD cofactor and perturbs the local active-site structure, preventing productive binding of the substrate l-kynurenine. Functional assays and targeted mutagenesis reveal that the active-site architecture and UPF 648 binding are essentially identical in human KMO, validating the yeast KMO-UPF 648 structure as a template for structure-based drug design [3].in vivo: Applying an identical experimental design, separate rats were used to study the effect of KMO inhibition on the de novo synthesis of KP metabolites in the lesioned striatum. These animals were bilaterally injected with 0.1 mM UPF 648 and 3H-kynurenine in PBS. 0.1 mM UPF 648 significantly reduced the neosynthesis of 3-HK and QUIN in the lesioned striatum (by 77 % and 66%, respectively) and moderately (27%) but significantly increased the de novo formation of KYNA [1]. Administered to pregnant rats or mice on the last day of gestation, UPF 648 (50 mg/kg, i.p.) produced qualitatively similar changes (i.e., large increases in kynurenine and KYNA and reductions in 3-HK and QUIN) in the brain and liver of the offspring. Rat pups delivered by UPF 648-treated mothers and immediately exposed to neonatal asphyxia showed further enhanced brain KYNA levels [2]. UPF 648, has an IC50 of 20 nM and provides protection against intrastriatal QUIN injections in kynurenine aminotransferase (KAT II) deficient mice. UPF 648 treatment also shifts KP metabolism towards enhanced neuroprotective KYNA formation [3].
Cimetropium Bromide is a mAChR antagonist for long-term treatment of irritable bowel syndrome.
Oxethazaine-d6 (Oxetacaine-d6) is the deuterium labeled Oxethazaine. Oxethazaine (Oxetacaine), a precursor of phentermine acidic, is an acid-resistent and orally active analgesic agent. Oxethazaine (Oxetacaine) has the potential for the relief of pain associated with peptic ulcer disease or esophagitis[1][2].