GluN2B receptor modulator-1 is a selective GluN2B negative allosteric modulator with an IC50 value of 31 nM.
Notoginsenoside Fa, a protopanaxadiol (ppd)-type saponin isolated from P. notoginseng, could possibly activate and recover the function of degenerated brain[1][2].
MRS 1523 is a potent and selective adenosine A3 receptor antagonist with Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. In rat this corresponds to selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. MRS 1523 can exert antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons[1][2].
AChE-IN-20 (compound M26) is a potent AChE inhibitor with IC50 value of 397.32 nM and with Ki value of 335.76 nM. AChE-IN-20 shows inhibition potency against hCA I , hCA II and α-GLY with IC50 values of 84.14, 69.24 and 52.08 nM and with Ki values of 97.86, 76.23 and 57.93 nM, respectively[1].
Xilmenolone is a GABAA receptor positive allosteric modulator[1].
BD-1047 dihydrobromide is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia. IC50 value: Target: sigma receptorin vitro: Moreover, Progesterone and BD 1047 (a sigma 1 receptor antagonist) counteracted the antidepressant-like effect induced by co-administration of Pramipexole and Sertraline (but not Pramipexole and Fluoxetine). [2] This increased pNR1 expression is significantly reduced by pretreatment with the specific Sig-1 R antagonist, BD-1047. In another set of experiments Sig-1 R agonists further potentiated NMDA-induced pain behaviour and pNR1 immunoreactivity and this is also reversed with BD-1047. [3]in vivo: BD 1047 does not decrease amphetamine-induced hyperactivity in mice in a statistically significant manner. BD 1047 does not modify the hyperactivity induced by NMDA receptor antagonists. BD 1047 shows a moderate activity in models used in this study suggesting that its usefulness as an antipsychtic drug is doubtful. [1]
Mesdopetam (IRL790) hemitartrate is a dopamine D3 receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3 receptor) with psychomotor stabilizing properties. Mesdopetam hemitartrate is used for the research of motor and psychiatric complications in Parkinson disease[1][2].
Foslevcromakalim (QLS-101) is a ATP-sensitive potassium channel opener. Foslevcromakalim is the prodrug used for ocular hypotensive effect[1][2].
S26131 (compound 5) is a potent and selective MT1 melatoninergic ligand, and the Ki values are 0.5 and 112 nM for MT1 and MT2, respectively. S26131 behaves as an MT1 and MT2 antagonist[1].
Baclofen is a gamma-amino-butyric acid (GABA) derivative used as a skeletal muscle relaxant.Target: GABA ReceptorBaclofen, a lipophilic analog of gamma-aminobutyric acid, is clinically used to control spasticity. Baclofen pretreatment (3 mg/kg) not only prolonged the time taken for animals to reach a core body temperature of 40 degrees C (P < 0.001), but also reduced the percentage of rats attaining a core body temperature of 40 degrees C [1]. Baclofen overdose may result in coma, apnea, autonomic disturbances, cardiac conduction abnormalities, and seizures. Levels obtained shortly after overdose correlate with length of mechanical ventilation [2].
BCATc Inhibitor 2 is a selective branched-chain aminotransferase (BCAT) inhibitor for research of neurodegenerative diseases. The IC50s of 0.2 μM, 0.8 μM and 3.0 μM for rat cytosolic isoenzyme rBCATc, human cytosolic isoenzyme hBCATc and rat mitochondrial isoenzyme rBCATm, respectively[1].
JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.
Melitracen (Melitracene) is an orally active tricyclic antidepressant and it is also a bipolar thymoleptic with activating properties. Melitracen inhibits 3H-5-HT and 14H-5-HT with IC50s of 670 nM and 5500 nM, respectively. Melitracen can be used for the research of depression and anxiety[1][2].
FGF acidic I (102-111) (bovine brain) (aFGF (102-111)) is the 102-111 fragment of acidic FGF that can be used as a potential neurotrophic agent[1].
MCH (human, mouse, rat) is a potent peptide agonist of MCH-R and exhibits binding IC50 values of 0.3nM and 1.5 nM for MCH1R and MCH2R, respectively. MCH (human, mouse, rat) is a highly sensitive to MCH-2R in a CHO cell line and monitoring mobilization of intracellular calcium with FLIPR, exhibits functional activation EC50 values of 3.9 nM and 0.1nM for human MCH-1R and MCH-2R, respectively[1].
Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (Ki=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids[1][2].
PF-06371900 is a potent and highly selective leucine rich repeat kinase 2 (LRRK2) inhibitor[1].
Padsevonil is a potent antiepileptic agent.
SALMF amide 1 is a neuropeptide[1].
RU 24969 is a selective agonist at the 5-HT1A and 5-HT1B receptors; IC50 value:Target: 5-HT1A/1B agonistRU 24969 possesses preference for the purported 5-HT1B subtype of central 5-HT1 recognition site. The reported significant linear correlation between hypotensive activity following intravenous (i.v.) administration to anesthetized rats and affinity for the central 5-HT1 binding site could only be maintained by incorporation of the affinity of RU 24969 for its low and 8-OH-DPAT for its high affinity binding site [1]. The drug RU 24969 (10 mg/kg) inhibited the rate of synthesis of 5-HT in rat brain by about 50%. Pretreatment of rats with desmethylimipramine over a longer term or clenbuterol given acutely, treatments known to enhance the behavioural responses of rats to various other 5-HT agonists, did not alter the RU 24969-induced response [2]. RU 24969 (0.03-3.0mg/kg, s.c.) dose-dependently decreased water consumption in water deprived rats [3].
Pirepemat (IRL752) is a corticalpreferring catecholamine- and cognition-promoting agent. Pirepemat (IRL752) is used for the study of Parkinson's disease[1][2].
DA-JC4 is a dual GLP-1/GIP receptor agonist and can be used for the research of neurological disease and insulin signaling pathways[1][2][3].
3β-Hydroxy-lup-20(29)-en-16-one (compound 9) is a dual inhibitor of AChE and BChE, with selectivity for BChE (IC50: 28.9 μM)[1].
Mebeverine alcohol D5 is the deuterium labeled Mebeverine alcohol, which is a metabolite of Mebeverine.
(Rac)-Mephenytoin-d3 is a labelled racemic Mephenytoin. Mephenytoin, an anticonvulsant, is the CYP2C19 and CYP2B6 substrate[1].
BMY-14802 hydrochloride (BMY-14802-1) is a selective and orally active sigma receptor antagonist with an IC50 of 112 nM. BMY-14802 hydrochloride is also a 5-HT1A and adrenergic α1 receptors agonist. BMY-14802 hydrochloride has antipsychotic effects[1][2][3].
ISX-9 is a small molecule inducer of adult neural stem cell differentiation. Target: At 2.5-20 μM, ISX-9 has been shown to dose-dependently trigger neurogenesis and block gliogenesis in adult rat hippocampal stem cells through a calcium-activated signaling pathway dependent on myocyte-enhancer factor 2-dependent gene expression.ISX-9 administered at 20 mg/kg for 12 days to mice has been reported to improve hippocampal function as evidenced by enhanced spatial memory ability in the Morris water maze test.
Levonantradol (l-Nantradol) hydrochloride is an analog of delta (9)-tetrahydrocannabinol. Levonantradol acting as a potent anti-analgesic agent[1].
Alaproclate (GEA 654) hydrochloride is a selective and orally active serotonin re-uptake inhibitor (SSRI). Alaproclate hydrochloride also acts as a potent, reversible and noncompetitive antagonist of the NMDA receptor coupled ion flow[1][2].
Mecamylamine-d3 hydrochloride is the deuterium labeled Mecamylamine hydrochloride. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier[1][2].