Bicuculline methiodide is a potent GABA(A) receptors blocker. Bicuculline methiodide alters membrane properties and firing pattern. Bicuculline methiodide reduces the Apamin-sensitive afterhyperpolarization, while Apamin is a toxin isolated from bee venom to block small conductance Ca2+ -activated K+ channels. Bicuculline methiodide facilitates burst firing via blocking apamin-sensitive Ca2+ -activated K+ current[1].
Nonivamide is a agonist, which exhibits 4d-EC50 value of 5.1 mg/L in static toxicity tests.
Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2[3]. Olivetol also inhibits CYP2C19 and CYP2D6 activity, with IC50s of 15.3 μM, 7.21 μM and Kis of 2.71 μM, 2.87 μM, respectively[1][2].
Osthenol (Ostenol), a prenylated coumarin isolated from the dried roots of Angelica pubescens, is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM). Osthenol potently inhibits recombinant hMAO-A with an IC50 of 0.74 µM and shows a high selectivity index for hMAO-A versus hMAO-B[1].
11-O-Galloylbergenin is a compound isolated from ethanolic extract of Mallotus philippinensis. 11-O-Galloylbergenin has analgesic and anti-inflammatory activities. 11-O-Galloylbergenin is a lead compound for management of pain and inflammation[1].
Moxonidine-d4 (BDF5895-d4) is the deuterium labeled Moxonidine. Moxonidine(BDF5895) is a selective agonist at the imidazoline receptor subtype 1, used as antihypertensive agent[1][2].
IDO1/TDO-IN-4 is a potent IDO1/TDO dual inhibitor, with IC50 values of 3.53 μM (IDO1) and 1.15 μM (TDO). IDO1/TDO-IN-4 forms hydrogen bond with IDO1, and π−π stacking interaction with TDO. IDO1/TDO-IN-4 can be used in the research of depression, and depression-induced infectious, metabolic, and autoimmune disorders[1].
L-AP5 (L-APV; L-2-Amino-5-phosphonovaleric acid) is an NMDA antagonist and is the isomer of D-AP5 (HY-100714A).L-AP5 shows a relatively weak amino acid and synaptic blocking activity[1].
Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
FKGK11 is a potent and selective inhibitor of GVIA iPLA2 (Group VIA calcium-independent phospholipase A2). FKGK11 can be used for the research of ovarian cancer and neurological disorders such as peripheral nerve injury and multiple sclerosis[1][2].
Pressinoic Acid is a synthetic hexapeptide with potent corticotrophin-releasing activity. Pressinoic Acid is also an oxytocin inhibitor; it induces maternal behavior.
LSN2814617 is an orally active, potent, brain-penetrant, and selective mGlu5 (metabotropic glutamate 5) positive allosteric modulator (PAM), with EC50 values of 52 nM (Human mGlu5) and 42 nM (rat mGlu5). LSN2814617 shows wake-promoting effect. LSN2814617 can be used for schizophrenia research[1].
SEP-363856 hydrochloride（SEP-856 hydrochloride）, an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 hydrochloride（SEP-856 hydrochloride） has the potential for the treatment of schizophrenia[1].
NPY5RA-972 is an orally active, central nervous system (CNS) penetrating, potent and selective NPY Y5 receptor antagonist that prevents feeding driven by activation of this receptor[1].
FSB is a fluorescent dye that can be used to detect filamentous tau and to label human amyloid lesions with high sensitivity and specificity (excitation: 390 nm, emission: 520 nm)[1][2].
PSB-06126 is a selective nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitor, with the Ki values of 0.33 μM for rat NTPDase 1, 19.1 μM for NTPDase 2 and 2.22 μM for NTPDase 3, respectively. PSB-06126 acts on human NTPDase 3 with an IC50 value of 7.76 μM and a Ki value of 4.39 μM[1][2].
F 11440 is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.Target: 5-HT1AThe affinity of F 11440 for 5-HT1Abinding sites (pKi, 8.33) was higher than that of buspirone (pKi , 7.50), and somewhat lower than that of flesinoxan (pKi , 8.91).In vivo, F 11440 was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone, in exerting 5-HT1A agonist activity at pre- and postsynaptic receptors in rats (measured by, for example, its ability to decrease hippocampal extracellular serotonin (5-HT) levels and to increase plasma corticosterone levels, respectively). F 11440, shown here to be a potent, selective, high efficacy 5-HT1Areceptor agonist, appears to have the potential to exert marked anxiolytic and antidepressant activity in humans.[1]
Heterocyclyl carbamate derivative 1 is a heterocyclyl carbamate derivative that may be used for the research of inflammatory and neurological diseases.
T761-0184 is a potent α7 nicotinic receptor (nAChR) antagonist[1].
Oct-1-en-3-ol, a fatty acid fragrant, is a self-stimulating oxylipin messenger. Oct-1-en-3-ol serves as a signaling molecule in plant cellular responses, plant-herbivore interactions, and plant-plant interactions. Oct-1-en-3-ol causes dopamine neuron degeneration through disruption of dopamine handling[1][2].
Joro spider toxin 3 is a GABA agonist. Joro spidertoxin 3 blocks the binding of muscle-stimulating diazepam. Joro spider toxin 3can be used to study the inactivation mechanism of inhibitory GABA receptor[1].
Dichlorphenamide disodium is an orally active, specific, carbonic anhydrase inhibitor. Dichlorphenamide can reduce intraocular pressure by inhibiting the secretion of water from the eye. Dichlorphenamide can be used for glaucoma research[1].
Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic drug candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor[1].
Cefazolin sodium pentahydrate is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research[1]. Cefazolin sodium pentahydrate has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD)[2].
L-Tyrosine-d2 is the deuterium labeled L-Tyrosine. L-Tyrosine is a non-essential amino acid which can inhibit citrate synthase activity in the posterior cortex.
Mca-SEVKMDAEFRK(Dnp)RR-NH2, containing the wild-type amyloid precursor protein (APP) beta-secretase cleavage site, is the substrate of thimet oligopeptidase (TOP). It is used for Alzheimer's disease research[1].
Cenobamate, a sodium channel blocker, enhances GABAergic transmission and has the potential to be a versatile CNS drug.
3-Methyl-2-oxovaleric acid-d8 sodium is the deuterium labeled 3-Methyl-2-oxovaleric acid. 3-Methyl-2-oxovaleric acid is a neurotoxin, an acidogen, and a metabotoxin, and also an abnormal metabolite that arises from the incomplete breakdown of branched-chain amino acids[1].
ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM.
Remimazolam benzenesulfonate is a GABA agonist。Target: GABA ReceptorRemimazolam acts on GABA receptor, specifically GABA-alpha. Remimazolam is a new drug innovation in anesthesia. Remimazolam combines the properties of two unique drugs already established in anesthesia - Midazolam and remifentanil. Remimazolam acts on GABA receptors like midazolam and has organ-independent metabolism like remifentanil. Remimazolam is likely to be the sedative of the future, as preliminary phase II trials have shown minimal residual effects on prolonged infusions. Remimazolam has potential to be used as a sedative in ICU and as a novel agent for procedural sedation.