Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties[1][2][4].
Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects[1][2][3].
Nitroxazepine is a tricyclic antidepressant (TCA) for the treatment of depression. Nitroxazepine acts as a serotonin-norepinephrine reuptake inhibitor.
Alizapride hydrochloride is a dopamine receptor antagonist with prokinetic and antiemetic effects which can also be used in the treatment of nausea and vomiting, including postoperative nausea and vomiting.
L-DOPA-2,5,6-d3 (Levodopa-2,5,6-d3) is the deuterium labeled L-DOPA. L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain[1][2][3].
JNJ-42165279 is a FAAH inhibitor with IC50 of 70 ± 8 nM and 313 ± 28 nM for hFAAH and rFAAH, respectively.IC50 value: 70 ± 8 nM (for hFAAH), 313 ± 28 nM (for rFAAH )Target：FAAHJNJ-42165279 covalently inactivates the FAAH enzyme, but is highly selective with regard to other enzymes, ion channels, transporters, and receptors. JNJ-42165279 exhibits high selectivity against a panel of 50 receptors, enzymes, transporters, and ion-channels at 10 μM, at which concentration it does not produce >50% inhibition of binding to any of the targets. Fortunately, JNJ-42165279 also does not inhibit CYPS (1A2, 2C8, 2C9, 2C19, 2D6, 3A4) or hERG when tested at a 10 μM compound concentration. [1]in vivo: JNJ-42165279 exhibits excellent ADME and pharmacodynamic properties as evidenced by its ability to block FAAH in the brain and periphery of rats and thereby cause an elevation of the concentrations of anandamide (AEA), oleoyl ethanolamide (OEA), and palmitoyl ethanolamide (PEA). The compound was also efficacious in the spinal nerve ligation (SNL) model of neuropathic pain. JNJ-42165279 exhibits relatively rapid clearance in the course of rat pharmacokinetic experiments, manifesting as a low AUC and Cmax; however, sufficiently high exposures were obtainable to support preclinical animal models. In a subsequent higher dose (20 mg/kg) oral PK experiment, compound concentrations were determined both in the plasma and brain of rats. [1]
Lesogaberan (AZD-3355) napadisylate is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptors. Binding affinity (Kis) of 5.1 nM and 1.4 μM for rat brain GABAB and GABAA receptors, respectively[1].
CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease[1].
Pirimiphos-methyl is a rapid-acting organophosphorus insecticide and acaricide, causing inhibition of AChE in target organisms. Pirimiphos-methyl is often used for prevention and control of beetles, snout beetles, moths and Ephestia cautella during storage of agricultural grains[1][2][3].
Farampator-d10 (CX-691-d10) is the deuterium labeled Farampator. Farampator (CX-691) is an AMPA receptor positive modulator.
Sinomenine, an alkaloid extracted from Sinomenium acutum, is a blocker of the NF-κB activation[1]. Sinomenine also is an activator of μ-opioid receptor[2].
CYT-1010 hydrochloride is a mu-opioid receptor agonist extracted from patent WO2013173730A2, with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively[1].
Orphenadrine-d3 (hydrochloride) is the deuterium labeled Orphenadrine hydrochloride[1]. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases[2][3].
(-)-Carvone is an insect neurotoxin and a irreversible acetylcholinesterase (AChE) inhibitor. (-)-Carvone can be used as a bird repellent, inhibits larval growth, decreases pupatation rate, and increases mortality of larvae[1][2].
Manghaslin is a flavonoid glycoside with anti-inflammatory activities. Manghaslin shows inhibitory activity against AChE with an IC50 of 94.92 µM[1][2].
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2[1].
ZZL-7 is a fast-onset antidepressant agent. ZZL-7 works by disrupting the interaction between the serotonin transporter (SERT) and neuronal nitric oxide synthase (nNOS) in the dorsal raphe nucleus (DRN). ZZL-7 can cross the blood-brain barrier readily. ZZL-7 can be used for the research of major depressive disorder (MDD)[1].
αA-Conotoxin PIVA is a selective mouse musclenAChR inhibitor with IC50 for adult and fetal mouse musclenAChR sub> values are 2.3 nM and 22 nM respectively. αA-Conotoxin PIVA can be used in the study of neurological diseases.
(1S,2R)-Tranylcypromine hydrochloride is a potent antidepressant agent. (1S,2R)-Tranylcypromine hydrochloride can inhibits MAO and LSD1[1][2].
PF 0713, a GABAA receptor agonist, is used as an intravenous sedative-hypnotic for general anaesthesia, ICU sedation, procedural sedation, chemotherapy.
Demecarium Bromide (BC-48) is a potent cholinesterase inhibitor, with an apparent affinity (Kiapp) of 0.15 μM[1]. Demecarium Bromide (BC-48) is used as a glaucoma agent[2].
(Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine is a full agonist of?dopamine receptor, a partial agonist of the?5-HT1A receptor, and an antagonist of the?α2B-adrenergic receptor, with?Kis of 0.71?nM, 4-15?nM, and 83?nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
Moclobemide(Ro111163) is a reversible monoamine oxidase inhibitor (MAOI) selective for isoform A (RIMA) used to treat major depressive disorder.Target: Monoamine OxidaseMoclobemide orally administered 2 hours before decapitation preferentially inhibits MAO-A and PEA in rat brain with ED50 of 7.6 μmol/kg and 78 μmol/kg, respectively. Moclobemide orally administered 2 hours before decapitation preferentially inhibits MAO-A and PEA in rat liver with ED50 of 8.4 μmol/kg and 6.6 μmol/kg, respectively. Moclobemide (0.1 mM), which inhibits brain MAO-A activity by over 80%, does not affect benzylamine oxidase (rat heart) and diamine oxidase (rat small intestine) activity in vitro [1]. Moclobemide (10 mM-100 mM) includes in the culture medium during anoxia or with glutamate significantly increases in a concentration-dependent manner the amount of surviving neurons compared to controls in neuronal-astroglial cultures from rat cerebral cortex [2].Moclobemide (10 mg/kg p.o.) induces a significant decrease of all monoamine metabolites measured in rat brain [1]. Moclobemide, given via the drinking water (4.5 mg/kg/day), produces significant decreases in adrenal weight of rats after 5 (-23%) and 7 weeks (-16%) of treatment. Moclobemide upregulates hippocampal mineralocorticoid receptor (MR) levels in rats by 65%, 76% and 19% at 2 weeks, 5 weeks and 7 weeks of treatment, and upregulates Glucocorticoid receptor (GR) levels in this limbic brain structure by 10% at 5 weeks. Moclobemide treatment (5 weeks, 4.5 mg/kg/day) significantly attenuates stress (30 min novel environment)-induced plasma ACTH (-35%) and corticosterone (-29%) levels [3].
TPA023B is a potent, α2/α3 subtype-selective GABAA receptor partial agonist with Ki of 2.0 and 1.8 nM, does not affect the functioning of the α1 subtype; demonstrates anxiolytic effects in rodent and primate models of anxiety, with no significant effects in ataxia and/or myorelaxation.
LAU159 is a functionally selective positive modulator of α1β3 GABA(A) receptor with an EC50 of 2.2 μM[1].
DSP-1053 is a potent Serotonin Transporter (SERT) (Ki=1.02 nM) inhibitor with partial 5-HT1A receptor (Ki=5.05 nM) agonistic activity.
Dehydroaripiprazole (OPC-14857) hydrochloride is an active metabolite of Aripiprazole. Aripiprazole is an antipsychotic agent and is metabolized by CYP3A4 and CYP2D6 forming mainly Dehydroaripiprazole hydrochloride. Dehydroaripiprazole hydrochloride has with antipsychotic activity equivalent to Aripiprazole[1][2][3][4].
BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research[1][2][3].
AChE-IN-12 is a potent and blood-brain barrier (BBB) penetrant acetylcholinesterase (AChE) with IC50s of 0.41 μM and 1.88 μM for rat AChE and electric eel AChE. AChE-IN-12 is also a good antioxidant (ORAC = 3.3 eq), selective metal chelator and huMAO-B inhibitor (IC50 = 8.8 µM). AChE-IN-12 has remarkable inhibition of self- and Cu2+-induced Aβ1-42 aggregation, as well as exhibits a good neuroprotective effect. AChE-IN-12 can be used for researching Alzheimer’s disease[1].
Amyloid β-Peptide (1-42) human is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.