cis-ACPD is a potent agonist of NMDA receptor, with an IC50 of 3.3 μM. And it is also a selective agonist of group II mGluR, with EC50s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively[1][2].
SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.
ML169 (VU0405652) is a potent, selective and brain penetrant positive allosteric modulator (PAM) of M1 mAChR, with an EC50 of 1.38 µM. ML169 is a MLPCN probe and can be used for Alzheimer’s disease[1].
Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties[1].
α-Synuclein inhibitor 4 (compound 3gh) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 0.98 μM and inhibition ratio at 30 μM of 91.2%[1].
Levobetaxolol hydrochloride is a beta-adrenergic receptor inhibitor (beta blocker), used to lower the pressure in the eye in treating conditions such as glaucoma.
(±)-HIP-A is a non-competitive excitatory amino acid transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). (±)-HIP-A is also a lead compound against ischemia-induced neuronal degeneration. (±)-HIP-A can be used in the study of neurological diseases[1].
Paspalinine is a tremorgenic metabolite that can be found in Aspergillus flavus[1].
Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease[2].
Tiotropium Bromide (BA679 BR) is a muscarinic acetylcholine receptor (mAChR) antagonist that blocks the binding of the acetylcholine ligand and subsequent opening of the ligand-gated ion channel.
Kainic acid hydrate is a potent excitotoxic agent. Kainic acid hydrate also is an agonist for a subtype of ionotropic glutamate receptor. Kainic acid hydrate induces seizures[1][2].
Aloisine RP106 (compound 38) is a potent inhibitor of Cdk1/cyclin B, Cdk5/p25, and GSK3 with IC50s of 0.70µM, 1.5µM, 0.92 µM, respectively[1].
5-HT3-In-1 is extracted from patent EP0748807A1, compound example 8. It shows 5-HT3 inhibition activity.
RO5028442 is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).
D-Isoleucine ((R)-Isoleucine), an isoleucine stereoisomer, is a selective activator of Asc-1 antiporter, which enhances long-term potentiation at the hippocampal CA1-CA3 via release of endogenous D-serine[1].
Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
B-HT 920(Talipexole 2Hcl) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.IC50 Value: 25 nM(Adrenergic receptor α-2, rat)Target: Adrenergic Receptor; 5-HT Receptor; Dopamine Receptorin vitro: N/Ain vivo: Intravenous injection of 30 micrograms/kg of B-HT 920 into cats lead initially to an increase in blood pressure and then to a long-lasting decrease in blood pressure and heart rate. Vagally mediated reflex bradycardia elicited by angiotensin injection in beta-adrenoceptor-blocked dogs was facilitated by intracisternal injection of 10 micrograms/kg B-HT 920.
S-Allyl-L-cysteine, one of the organosulfur compounds found in AGE, possess various biological effects including neurotrophic activity, anti-cancer activity, anti-inflammatory activity.
Olcegepant is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.
Felbamate-d4 (W-554-d4) is the deuterium labeled Felbamate. Felbamate (W-554) is a potent nonsedative anticonvulsant whose clinical effect may be related to the inhibition of N-methyl-D-aspartate (NMDA).
AEF0117 a signaling-specific inhibitor of the cannabinoid receptor 1 (CB1-SSi). AEF0117 plays an important role in Cannabis use disorder (CUD)[1].
Xanthine amine congener (XAC) hydrochloride is a non-selective adenosine receptor antagonist. Xanthine amine congener hydrochloride induces convulsions in mice[1].
Sodium Houttuyfonate is a natural compound extracted from Houttuynia cordata, with anti-inflammatory and anti-fibrotic effects. Sodium Houttuyfonate ameliorates LPS induced mastitis by inhibiting the NF κB pathway[1][2].
13-Hydroxylupanine Hydroxylupanine is the typical alkaloid profile of sweet lupins. 13-Hydroxylupanine Hydroxylupanine blocks ganglionic transmission, decreases cardiac contractility and contracts uterine smooth muscle[1].
Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity[1].
Inosine-2,8-d2 is the deuterium labeled Inosine. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors[1][2][3].
TNIK-IN-6 (Compound 9) is an inhibitor of Traf2 and Nck-interacting kinase (TNIK) and , with IC50 of 0.93 μM, that plays important roles in neurological and psychiatric disorders[1][2].
[MePhe8,Sar9] Substance P ([MePhe8-MeGly9] Substance P) is an analog of Substance P (Substance P (HY-P0201)).Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator in the CNS[1].
Cl-HIBO is a highly subtype-selective GluR1/2 agonist (EC50=4.7 and 1.7 μM, respectively). Cl-HIBO is a potent AMPA receptor agonist (IC50=0.22 μM). Cl-HIBO has desensitizing properties[1].
LX-1031 is a potent, orally available tryptophan 5-hydroxylase (TPH) inhibitor that reduces serotonin (5-HT) synthesis peripherally.