PNU-96415E is a selective D4/5-HT2A antagonist. PNU-96415E may have potential antipsychotic efficacy[1].
6'-Iodoresiniferatoxin (6'-IRTX) is a TRPV1 agonist used in the study of neuropathic pain[1].
Echitovenidine is an alkaloid that can be isolated from Alstonia yunnanensis. Echitovenidine is an inhibitor of monoamine oxidase (MAO)[1].
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca2+ flux [1][2][3].
Mebanazine is a potent monoamine oxidase (MAO) inhibitor. Mebanazine can be used in research of depression[1].
Bocconoline is a potent early endosome antigen 1 (EEA1) inhibitor. Bocconoline can be isolated from Macleaya cordata. Bocconoline can be used for the research of Parkinson’s disease (PD)[1].
Methyl citrate is a Monoamine oxidase B (MAO-B) inhibitor (IC50=0.23 mM). Methyl citrate is isolated from the fruits of Opuntia ficus-indica var. saboten Makino[1].
Carassin is a 21 amino acid tachykinin-related peptide, it can be isolated from the goldfish brain. Carassin has moderate affinity for rat tachykinin binding sites[1][2].
Protocatechuic acid is a phenolic compound which exhibits neuroprotective effect.
Indole-3-pyruvic acid, a keto analogue of tryptophan, is an orally active AHR agonist. Indole-3-pyruvic acid has antioxidant properties, and can be used in the research of inflammation, anxiety[1][2][3].
ALX-1393, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model[1].
Isopropyl dodec-11-enylfluorophosphonate (IDEFP) is an organophosphorus ester that antagonizes the central cannabinoid receptor (CB1) and inhibits FAAH with similar potencies (IC50 = 2 nM)[1].
δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research[1].
Selfotel (CGS 19755) is a selective and competitive antagonist at N-methyl-D-aspartate (NMDA)-preferring receptor. CGS 19755 inhibits the binding of [3H]-3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid to NMDA-type receptors with an IC50 of 50 nM[1][2].
Miglustat hydrochloride is an inhibitor of glucosylceramide synthase, primarily to treat Type I Gaucher disease (GD1).Target: OthersMiglustat is an inhibitor of the ceramide-specific glycosyltransferase, which catalyzes the first step of glycosphingolipid biosynthesis and is currently approved for the oral treatment of type 1 GD [1]. Consumption of a standard high-fat breakfast within 30 minutes before administration of miglustat significantly reduced peak exposure but did not significantly affect the extent of systemic exposure to miglustat. The peak plasma concentration (C(max)) decreased by 36% on average following administration with food. Area under the plasma concentration-time curve (AUC(0-infinity)) showed a modest (14%) decrease with food, but the 90% confidence interval was within the acceptance limit of 80% to 125%. The median (min-max) time to C(max) (t(max)) was prolonged from 2.5 (1.0-4.0) hours in the fasted state to 4.5 (1.5-8.0) hours in the fed state, whereas the apparent terminal half-life was approximately 8 hours and not affected by food [2].
Diapocynin (Dehydrodiacetovanillone), a dimeric derivative of Apocynin, is an orally active NADPH oxidase inhibitor. Diapocynin has anti-inflammatory, neuroprotection and antioxidant activities[1].
(rel)-Eglumegad ((rel)-LY354740) is the racemic isomer of Eglumegad (HY-18941). Eglumegad is a highly potent and selective group II (mGlu2/3) receptor agonist with EC50s of 5 and 24 nM for transfected human mGlu2 and mGlu3 receptors, respectively[1].
ZSET1446 is a novel cognitive enhancer that significantly improves learning deficits in various types of Alzheimer disease (AD) models.
WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM)[1][2].
[Ala11,D-Leu15]-Orexin B(human) is a potent and selective orexin-2 receptor (OX2) agonist. [Ala11,D-Leu15]-Orexin B(human) shows a 400-fold selectivity for the OX2 (EC50=0.13 nM) over OX1 (52 nM)[1].
N-Acetyl-5-hydroxytryptamine is a Melatonin precursor, and that it can potently activate TrkB receptor.
Methocarbamol-13C,d3 is the 13C- and deuterium labeled. Methocarbamol is an orally active central muscle relaxant and blocks muscular Nav1.4 channel. Methocarbamol reversibly affects voltage dependence of inactivation of Nav1.4 channel. Methocarbamol has the potential for muscle spasms and pain syndromes research[1][2][3].
ML218 hydrochloride is a potent, selective and orally active T-type Ca2+ channels (Cav3.1, Cav3.2, Cav3.3) inhibitor with IC50s of 310 nM and 270 nM for Cav3.2 and Cav3.3, respectively. ML218 hydrochloride inhibits the burst activity in subthalamic nucleus (STN) neurons. ML218 hydrochloride has no significant inhibition of L- or N-type calcium channels, KATP or hERG potassium channels. ML218 hydrochloride can penetrate the blood-brain barrier[1].
Psychosine (Galactosylsphingosine), a substrate of the galactocerebrosidase (GALC) enzyme, is a potential biomarker for Krabbe disease[1]. Psychosine is a highly cytotoxic lipid, capable of inducing cell death in a wide variety of cell types including, most relevantly to globoid cell leukodystrophy (GLD), oligodendrocytes. Psychosine causes cell death at least in part via apoptosis. Psychosine also is an inhibitor of PKC[1].
Isocitric acid is an endogenous metabolite present in Saliva and Cellular_Cytoplasm that can be used for the research of Alzheimer's Disease, Lewy Body Dementia and Anoxia[1][2][3].
ONO-8713 is a selective prostaglandin E receptor subtype EP1 antagonist.
(S)-Osanetant is the S-enantiomer of Osanetant. Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia[1].
Substance P (2-11) is a substance P (SP) fragment peptide. Substance P (2-11) has contracting activities on guinea pig ileum. Substance P (2-11) inhibits the permeation of 3H SP in BBMEC monolayers[1][2].
AChE/Nrf2 modulator 1 is an orally active acetylcholinesterase (AChE)/nuclear factor erythroid 2-related factor 2 (Nrf2) modulator. AChE/Nrf2 modulator 1 has Nrf2 inductive activity and AChE inhibitory activity for eeAChE and hAChE with IC50 values of 0.07 μM and 0.38 μM, respectively. AChE/Nrf2 modulator 1 can be used for the research of Alzheimer's disease[1].
(+)-KCC2 blocker 1 is a selective K+-Cl- cotransporter KCC2 blocker with an IC50 of 0.4 μM. (+)-KCC2 blocker 1 is a benzyl prolinate and a enantiomer of KCC2 blocker 1[1].