Loperamide phenyl is an impurity of Loperamide (HY-B0418A). Loperamide is an opioid receptor agonist[1].
VU0529331 is a modestly selective non-GIRK1-containing G protein-gated, inwardly-rectifying, potassium channel (non-GIRK1/X) activator, with EC50s of 5.1 µM and 5.2 µM for GIRK2 and GIRK1/2 in HEK293 cells, respectively, also effective on GIRK4 homomeric channel[1].
S-22153 is a potent melatonin receptor antagonist with EC50 values of 19 nM, 4.6 nM for hMT1 and hMT2 melatonin receptor, respectively. S-22153 has Ki values of 8.6 nM (CHO cells) and 16.3 nM (HEK cells) for hMT1, and 6.0 nM (CHO cells) and 8.2 nM (HEK cells) for hMT2. S-22153 is a specific ligand of MT1 and MT2 melatonin receptors subtypes[1][2].
Tiospirone is a 5-HT2 receptor antagonist with affinity for D2, 5-HT1a, and 5-HT7, and sigma receptors. Tiospirone decreases consumption of ethanol while increasing food intake of rats. Tiospirone can also reduce the reinforcing properties of Cocaine exhibited in the conditioned place preference paradigm[1][2].
ML-184 (ML184) is a potent, selective GPR55 agonist with EC50 of 263 nM, >120-fold, 83-fold, and 57-fold selectivity against GPR35, CB1 and CB2; shows activity in activating the downstream responses of ERK phosphorylation and PKC β II translocation.
Cyclohexanecarboxylic acid is a Valproate structural analogue with anticonvulsant action[1].
Ropivacaine-d7 hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B)[1]. Ropivacaine hydrochloride is a potent?sodium channel?blocker and blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese[2][3]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane[4]. Ropivacaine is widely used for neuropathic pain?management in vivo[2].
ADX88178 is a potent positive allosteric modulator for metabotropic glutamate receptor 4 (mGluR4) with EC50 of 4 nM for human mGluR4.
(±)13(14)-EpDPA (13,14-EpDPE) is the product of the reaction of cytochrome P-450 epoxygenase with Docosahexaenoic Acid (DHA).(±)13(14)-EpDPA has antihyperalgesic and vasorelaxative activities[1].
Acetyllycoposerramine M is a lycopodine-type alkaloid, which can be isolated from Lycopodium japonicum. But Acetyllycoposerramine M has no inhibitory effect on acetylcholinesterase[1].
Capsiconiate (Coniferyl (E)-8-methyl-6-nonenoate) is a TRPV1 agonist (EC50= 3.2 μM). Capsiconiate can be used to study TRPV1-mediated diseases such as pain, inflammation, and epilepsy(EC50= 3.2 μM)[1].
Velusetrag (TD-5108) is a potent, selective and oral 5-HT4 receptor agonist with pKi of 7.7, shows >500-fold selectivity over other 5-HT receptors; displays >25-fold selectivity over other biogenic amine receptors, and no effect on hERG channels; increases the contractility of the canine antrum, duodenum and jejunum with higher potency than tegaserod, demonstrates robust in vivo activity in the guinea pig, rat and dog gastrointestinal tracts. Other Indication Phase 2 Clinical
Rivastigmine, an cholinesterase inhibitor(IC50= 5.5 uM), inhibits both butyrylcholinesterase and acetylcholinesteraseIC50 value: 5.5 uMTarget: AChERivastigmine is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type and dementia due to Parkinson's disease. The drug can be administered orally or via a transdermal patch; the latter form reduces the prevalence of side effects, which typically include nausea and vomiting. The drug is eliminated through the urine, and appears to have relatively few drug-drug interactions. Rivastigmine, a cholinesterase inhibitor, inhibits both butyrylcholinesterase and acetylcholinesterase. It is thought to work by inhibiting these cholinesterase enzymes, which would otherwise break down the brain chemical acetylcholine.
Deoxysappanone B (3-Deoxysappanone B) is a homoisoflavone compound isolated from Caesalpinia sappan L (Lignum Sappan). Deoxysappanone B has anti-neuroinflammatory and neuroprotective effects and inhibits the production of neuroinflammatory mediators by blocking the IκB kinase (IKK)-NF-κB and p38/ERK MAPK pathways. Deoxysappanone B can be used in disease studies of neuritis and inflammation-related neurological damage[1].
Isofuranodiene is a neuritogenic compound isolated from wild celery (Smyrnium olusatrum L., Apiaceae)[1].
2-Arachidonoylglycerol-d11 is deuterium labeled 2-Arachidonoylglycerol.2-Arachidonoylglycerol is a second endogenous cannabinoid ligand in the central nervous system[1].
CAY10614 is a potent TLR4 antagonist. CAY10614 inhibits the lipid A-induced activation of TLR4, with an IC50 of 1.675 μM. CAY10614 can improve survival of mice in lethal endotoxin shock model[1][2].
Ethyl 7-(diethylamino)-2-oxo-2H-chromene-3-carboxylate is a potent and selective inhibitor of hMAO-B with an IC50 of 45.52 μM[1].
Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with an IC50 of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity[1][2][3].
ABT-418 hydrochloride is a potent and selective agonist of nAChRs with cognitive enhancing and anxiolytic activities. ABT-418 hydrochloride activates cholinergic channel and can be used for research of Alzheimer's disease[1][2].
CX614 is a positive variant modulator of AMPA receptors that enhances excitatory postsynaptic potentials (amplitude and duration) by blocking and slowing the inactivation of responses to glutamate and automatically evokes excitatory postsynaptic currents in neuronal cultures. CX614 can be used in the study of psychiatric disorders such as depression[1][2].
2BAct (eIF2B activator 2BAct) is a novel, highly selective, CNS-permeable small molecule eIF2B activator with EC50 of 33 nM in cell-based reporter assays; 2BAct normalized body weight gain and prevented motor deficits in male R191H mice, prevented myelin loss and reactive gliosis in the brain and spinal cord of R191H mice; also prevented ISR induction in the cerebellum and spinal cord of Eif2b5R132H/R132H mice, prevented all measures of pathology and normalizes the transcriptome and proteome of Vanishing White Matter (VWM) mice.
Y-29794 (Compound 2) is a potent, covalent prolyl oligopeptidase (POP) inhibitor with a Ki of 0.95 nM. Y-29794 can be used for studying neurodegenerative diseases and cancer[1].
Amoxapine is a tetracyclic antidepressant of the dibenzoxazepine family, though it is often classified as a secondary amine tricyclic antidepressant.
[Pro9]-Substance P is a potent, reversible and selective agonist of NK-1 tachykinin receptors with an EC50 of 0.93 nM[1].
Hydrangenol 8-O-glucoside (Hydrangenol 8-O-β-D-glucopyranoside) can be isolated from Hydrangea macrophyllu. Hydrangenol 8-O-glucoside is an AChE inhibitor (IC50: 22.66 μM). Hydrangenol 8-O-glucoside inhibits passive cutaneous anaphylaxis (PCA) reaction[1][2].
SYM 2206 is a novel, potent, non-competitive AMPA receptor antagonist (IC50= 2.8 μM).IC50 value: 2.8 μMTarget: AMPA receptorSYM 2206 exerts anticonvulsant effects, elevates the threshold for maximal electroshock-induced seizures in mice. TID20 and TID50(threshold increasing doses by 20% and 50%) values for SYM 2206 are 4.25 and 10.56 mg/kg in the MEST test in mice, respectively.
(S)-4C3HPG ((S)-4-Carboxy-3-hydroxyphenylglycine) is an antagonist of metabotropic glutamate receptor 1a (mGluR 1a) and an agonist of GluR2. (S)-4C3HPG has the anticonvulsant activity and protects against audiogenic seizures in DBA/2 mice[1].
Antidepressant agent 5 (Compound 3i) is a 7-substituted tetrahydroisoquinolines derivatives. Antidepressant agent 5 exhibits almost equal antidepressant activity compared with magnoflorine. ntidepressant agent 5 can be used for depressive disorder research[1].
Vasicinone is a quinazoline alkaloid isolated from the Adhatoda vasica plant. Vasicinone is a potential agent for Parkinson's disease and possibly other oxidative stress-related neurodegenerative disorders[1].