IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2[1].
Pitolisant oxalate is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
Butanedioic acid-13C2 is the 13C labeled Succinic acid[1]. Succinic acid is a potent and orally active anxiolytic agent. Succinic acid is an intermediate product of the tricarboxylic acid cycle. Succinic acid can be used as a precursor of many industrially important chemicals in food, chemical and pharmaceutical industries[2][3].
α-Synuclein (61-75) is the 61-75 fragment of α-Synuclein. α-Synuclein is an abundant neuronal protein that is highly enriched in presynaptic nerve terminals. α-Synuclein is a potential biomarker for Parkinson's disease (PD)[1][2].
TCRS-417 (T417) is a small molecule compound capable of docking to the interface between PBX1 and its cognate DNA target sequence, effectively interfering with PBX1-DNA interaction. TCRS-417 can be used in the research of cancer, developmental disorders, inflammatory disorders, autoimmune diseases or neurodegenerative diseases[1].
HTL22562 is a calcitonin gene-related peptide (CGRP) receptor antagonist for acute treatment of migraine.
MPP+-d3(iodide) is deuterium labeled MPP+ (iodide). MPP+ iodide, a toxic metabolite of the neurotoxin MPTP, causes symptom of Parkinson's disease in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ iodide is taken up by the dopamine transporter into dopaminergic neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain. MPP+ iodide is also a high affinity substrate for the serotonin transporter (SERT)[1][2].
SAMe-1,4-Butanedisulfonate, a natural compound, is a methyl donor in the central nervous system. SAMe-1,4-Butanedisulfonate has antidepressant activity. SAMe-1,4-Butanedisulfonate can be used for research of CNS disorders[1][2][3][4].
OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity[1][2].
Ipratropium bromide (Sch 1000) hydrate is a muscarinic receptor antagonist, with IC50s of 2.9 nM, 2 nM, and 1.7 nM for M1, M2, and M3 receptors, respectively. Ipratropium bromide hydrate relaxes smooth muscle, can be used in the research for COPD (chronic obstructive pulmonary disease) and asthma[1][2][3][4][5].
MARK-IN-2 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 5 nM.
Acetylcholinesterase (ACHE; EC 3.1.1.7) is a cholinergic enzyme mainly found in neuromuscular junctions and cholinergic type chemical synapses, and is often used in biochemical research. Acetylcholinesterase catalyzes the breakdown or hydrolysis of acetylcholine and some other choline esters that act as neurotransmitters into acetate and choline. Acetylcholinesterase's main role is to terminate neuronal transmission and signaling between synapses to prevent ACh spread and activation of nearby receptors[1].
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca2+-activated K+ (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca2+ and stimulates transmitter release[1][2].
LY108742 is a 5-HT2 receptor antagonist, with IC50 values of 9.3 nM (Rat), 57.2 nM (Pig), 56.8 nM (Monkey)[1].
Phoenixin-20 (PNX-20) is a bioactive peptide with hormone-like actions in vertebrates, and can stimulates hypothalamo-pituitary-gonadal hormones and regulate reproductive processes in mammals. Phoenixin-20 promotes neuronal mitochondrial biogenesis via CREB-PGC-1α pathway. Phoenixin-20 has anxiolytic effect[1][2][3].
Propionylpromazine hydrochloride (Propiopromazine hydrochloride), a dopamine receptor D2 (DRD2) antagonist, can be used in the research of Parkinson disease[1].
Rocuronium (Org-9426) is an aminosteroid non-depolarizing neuromuscular blocker or muscle relaxant used in modern anaesthesia.
PSB-12062 is a potent and selective P2X4 antagonist with an IC50 of 1.38 μM for human P2X4.
Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively[1].
Crocin II is isolated from the fruit of Gardenia jasminoides with antioxidant, anticancer, and antidepressant activity.Crocin II inhibits NO production with an IC50 value of 31.1 μM.Crocin II suppresses the expressions of protein and m-RNA of iNOS and COX-2[1].
HexylHIBO is a potent group I mGluR antagonist with Kbs of 140 and 110 μM at mGlu1a and mGlu5a receptors, respectively. HexylHIBO decreased sEPSC in rat[1].
IPN-60090 dihydrochloride is an orally bioavailable and selective inhibitor of GLS1 (the kidney-type glutaminase), an important enzyme for metabolic energy production. IPN-60090 dihydrochloride can be used in the research of GLS1-mediated diseases[1][2].
Dalargin is a potent δ-opioid receptor agonist. Dalargin mitigates Gentamicin (HY-A0276)-induced cell death. Dalargin shows nephroprotective effects on Gentamicin-induced kidney injury. Dalargin shows antiulcer activity[1][2][3].
Acamprosate is an orally active prototypic neuromodulator. Acamprosate can be used for the research of alcohol dependence and alcoholism[1].
Verazine ((-)-Verazine) is an anti-Fungal Agent that can be found in the dried roots and rhizoma of Veratrum maackii Regel. Verazine causes DNA damage in the cerebellum and cerebral cortex of mice in a dose-dependent manner. Verazine can be used in the study of fungal infections and neurological diseases[1][2].
MK-3328 is a β-Amyloid PET ligand, which exhibits high binding potency with an IC50 of 10.5 nM.
Doxapram hydrochloride hydrate inhibits TASK-1, TASK-3, TASK-1/TASK-3 heterodimeric channel function with EC50 of 410 nM, 37 μM, 9 μM, respectively.Target: Potassium ChannelDoxapram is a respiratory stimulant. Doxapram (15-150 microM) also evoked 3H overflow in a concentration dependent manner, and doxapram-evoked release was inhibited by the Ca2+ channel blocker nifedipine (5 microM). Analysis of released tritiated compounds suggested that doxapram preferentially stimulated the release of dopamine. Our results indicate that the mechanism of action of doxapram shares similarities with that of hypoxia in the carotid body [1]. Doxapram (1-100 microM) caused rapid, reversible and dose-dependent inhibitions of K+ currents recorded in type I cells (IC50 approximately 13 microM). doxapram was also seen to directly inhibit Ca(2+)-independent K+ currents. Doxapram was a more potent inhibitor of the Ca(2+)-activated K+ currents recorded under control conditions. Doxapram (10 microM) was without effect on L-type Ca2+ channel currents recorded under conditions where K+ channel activity was minimized and was also without significant effect on K+ currents recorded in the neuronal cell line NG-108 15, suggesting a selective effect on carotid body type I cells. The effects of doxapram on type I cells show similarities to those of the physiological stimuli of the carotid body, suggesting that doxapram may share a similar mechanism of action in stimulating the intact organ [2].
D[LEU4,LYS8]-VP is a selective agonist of vasopressin V1b receptor, with the Kis of 0.16 nM, 0.52 nM, and 0.1.38 nM for rat, human and mouse V1b receptor, respectively. D[LEU4,LYS8]-VP has weak antidiuretic, vasopressor, and in vitro oxytocic activities[1][2].
Ipalbidine is an alkaloid extracted from ipomoea Hardwickki Hemsl. Ipalbidine has dose-dependent analgesic effects[1].
4-Butyl-alpha-agarofuran (AF 5) is an anxiolytic and antidepressant agent. 4-Butyl-alpha-agarofuran a α-agarofuran derivative that can be isolated from Gharu-wood. 4-Butyl-alpha-agarofuran can be used for the research of neurological disease research[1].