Cyclobenzaprine-13C,d3 (hydrochloride) is the 13C- and deuterium labeled.
PEAQX(NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/2B(29,600 nM).IC50 value: 270 nM(hNMDA A1/A2) [1]Target: NR2A antagonistin vitro: PEAQX has a high binding affinity for NMDA receptors (IC50=8 nM), and a functional preference in excess of 100-fold for hNMDA 1A/2A (IC50=of 270 nM) over 1A/2B receptors (IC50=29,600 nM) [1].in vivo: PEAQX is practically inactive in Xenopus oocytes expressing hNMDA 1A/2B receptors, displays an ED50 value of 23 mg/kg in the MES test [1]. Sprague-Dawley rats were treated on PN7, PN9, and PN11 with PCP (10 mg/kg), PEAQX (NR2A-preferring antagonist; 10, 20, or 40 mg/kg), or ifenprodil (selective NR2B antagonist; 1, 5, or 10 mg/kg) and sacrificed for measurement of caspase-3 activity (an index of apoptosis) or allowed to age and tested for locomotor sensitization to PCP challenge on PN28-PN35. PCP or PEAQX on PN7, PN9, and PN11 markedly elevated caspase-3 activity in the cortex; ifenprodil showed no effect. Striatal apoptosis was evident only after subchronic treatment with a high dose of PEAQX (20 mg/kg). Animals treated with PCP or PEAQX on PN7, PN9, and PN11 showed a sensitized locomotor response to PCP challenge on PN28-PN35 [2].
Crocin is a nutraceutical and the main constituent isolated from the stigmas of Crocus sativus with immense pharmacological properties as anti-inflammatory, anticancer, antidepressant and anticonvulsant[1].
YM-08 (Compounds 7a) is a brain-penetrant inhibitors of SIRT2,with the IC50 of 19.9 μM. YM-08 also is inhibitor of Hsp70[1].
DOV-216,303 (Free Base) is a potent triple serotonin, norepinephrine, and dopamine reuptake inhibitor, with IC50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively[1]. Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats[2].
Irbesartan (SR-47436) hydrochloride is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan hydrochloride can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan hydrochloride can be used for the research of high blood pressure, heart failure, and diabetic kidney disease[1].
L-Glutamic acid-13C5,d5,15N is the deuterium, 13C-, and 15-labeled L-Glutamic acid. L-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA). L-Glutamic acid shows a direct activating effect on the release of DA from dopaminergic terminals.
MTEP Hcl is a potent, selective and non-competitive mGlu5 antagonist with IC50 and Ki of 5 nM and 16 nM, respectively. IC50 Value: 5 nM [1]Target: mGluR5MTEP occupied mGlu5 receptors in a dose-dependent manner with essentially full receptor occupancy at the highest dose tested (10 mg/kg, i.p.). At doses appropriate for mGlu5 receptor-mediated effects, MTEP significantly reduced fear-potentiated startle and increased punished responding in a modified Geller-Seifter conflict model consistent with an anxiolytic-like profile. MTEP decreased unpunished responding to a lesser extent than diazepam and had no effect on rotarod performance when administered either alone or in combination with ethanol. Repeated dosing with MTEP in this model eliminated the increase in punished responding observed with acute dosing.
mGAT3/4-IN-2 (compound 27b) is a potent mGAT3/mGAT4 inhibitor, with pIC50 values of 5.44 and 5.25, respectively[1].
Gelsemiol is the main active ingredient in Verbena littoralis H. B. K.. Gelsemiol enhanced nerve growth factor (NGF) -induced axonal elongation in PC12D cells[1].
Alirinetide (GM604) is an oligopeptide containing 6 amino acids. Alirinetide can cross the blood-brain barrier and can be used for the research of multiple neurodegenerative diseases[1].
Rivastigmine carbamate impurity (3-Nitrophenyl ethyl(methyl)carbamate) is an impurity of Rivastigmine. Rivastigmine is an orally active and potent cholinesterase (ChE) inhibitor and inhibits butyrylcholinesterase (BChE) and acetylcholinesteras (AChE) with IC50s of 0.037 μM, 4.15 μM, respectively[1][2].
Z-Thioprolyl-Thiazolidine is a potent and specific prolyl endopeptidase inhibitor with an Ki value of 0.36 nM for bovine brain prolyl endopeptidase[1]
Rubrofusarin triglucoside is a glycoside compound isolated from Cassia obtusifolia Linn seeds. Rubrofusarin triglucoside inhibits human monoamine oxidase A (hMAO-A) with an IC50 of 85.5 μM[1].
Tetrabenazine (Racemate) is a selective and reversible inhibitor of vesicular monoamine transporter-2 (VMAT-2).(1) The reference for administration is 0.25-0.75 mg/kg IP(2) Injections of tetrabenazine into accumbens core also reduced FR5 lever pressing and increased chow intake. (3) Tetrabenazine (Racemate) reduced extracellular DA and altered DARPP-32 signaling in both substance-P- and enkephalin-containing accumbens neurons. (4) Tetrabenazine (Racemate) inhibits locomotor activity and produces hypothermia upon systemic administration in rats and mice.
Beta-asarone is a major ingredient of Acorus tatarinowii Schott, penetrates blood brain barrier, with the properties ofimmunosuppression, central nervous system inhibition, sedation, and hypothermy. Beta-asarone protects against Parkinson’s disease[1].
Atuzaginstat (COR388) is an effective small-molecule bacterial protease lysine gingipain inhibitor and can be used for the research of Alzheimer's disease[1][2].
PD 168568 is a orally active and potent dopamine receptor D4 (DRD4) antagonist. PD 168568 contains an isoindolinone and is selective for the D4 receptor versus D2 and D3, with Ki values of 8.8, 1842, and 2682 nM, respectively. PD 168568 can be used for glioblastoma (GBM) research[1][2].
SKF 81297 hydrobromide is a potent and selective dopamine D1 receptor agonist[1].
TWIK-1/TREK-1-IN-3 (compound 2h) is an inhibitor of TWIK-related potassium channel (Potassium Channel) TREK-1. TREK-1 contains a two-pore domain potassium (K2p) channel that dimerizes into TREK-1 homodimer and TWIK-1/TREK-1 heterodimer, and is an important antidepressant target. TWIK-1/TREK-1-IN-3 targets TREK-1 homodimer and TWIK-1/TREK-1 heterodimer with IC50s of 9.74 μM and 16.5 μM, respectively, and has antidepressant-like effects[1].
D4R agonist-1 (Compound 16f) is a D4R partial agonist (Ki: 2.2 nM). D4R agonist-1 is metabolically stable in rat and human liver microsomes. D4R agonist-1 can be used for research of neuropsychiatric disorders[1].
HSK16149 is a novel ligand of voltage-gated calcium channel (VGCC) α 2 δ subunit.
Glycine-13C2,15N is the 13C- and 15N-labeled Glycine. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors.
S 38093 hydrochloride is a brain-penetrant, orally active antagonist of H3 receptor, with Kis of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively.
Hesperetin is a natural flavanone, and acts as a potent and broad-spectrum inhibitor against human UGT activity.
Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gaucher's disease research[1].
GABAA receptor agent 6 (compound 2027) is a potent γ-GABAAR antagonist with an Ki of 0.56 µM. GABAA receptor agent 6 shows γ-GABAAR antagonist activity with low cellular membrane permeability[1].
Indibulin (ZIO 301) , an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis[1].
Sunobinop (S 117957) is a modulator of the opioid receptor-like orphan receptor (ORL1)[1].
Triheptanoin (Propane-1,2,3-triyl triheptanoate) is a synthetic medium-chain triglyceride (MCT) consisting of three odd-chain 7-carbon (heptanoate) fatty acids on a glycerol backbone. Triheptanoin can be used for the research of inherited metabolic disorders[1].