Neurological Disease

Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3 receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2L receptors, with an inhibition constant (K_i) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC₅₀) of 3.72 nM in functional activity experiments.

TIPP is a potent and selective δ-opioid antagonist with a K_i value of 1.22 nM.

MSK-9 is a positive allosteric modulator of the P2X4 receptor with dual activities of enhancing ion conductance and delaying receptor inactivation. MSK-9 stabilizes the open state of the P2X4 receptor through rigid 3-piperidinyl and hydrophobic menthyl substituents. MSK-9 can be used in the study of multiple sclerosis (MS).

Lp-PLA2-IN-9 (compound 17), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC₅₀ of 10.1 for rhLp-PLA2. Lp-PLA2-IN-9 has the potential for neurodegenerative related diseases research.

Calebin A is a PI3K/Akt/mTOR, MAPK, and NF-κB inhibitor with oral effectiveness. Calebin A can block the autophagy-repressive, inhibiting apoptosis. Calebin A has anti-tumor activity by epigenetic regulation. Calebin A suppresses adipogenesis, modulates thermogenesis, and enriches gut probiotics. Calebin A can be used in research on osteoarthritis, Alzheimer's disease, type 2 diabetes, malignant peripheral nerve sheath tumors, and colorectal cancer.

(D-Arg1,D-Pro2,D-Phe7,D-His9)-Substance P is a selective NK₁ receptor antagonist.

HHL-6 can regulate the overexpression of c-Fos and BDNF proteins. HHL-6 has potent anticonvulsant and antiepileptogenic effects.

TDHL-d₁₀ (Tergurid-d₁₀; Terguride-d₁₀; trans-Dihydrolisuride-d₁₀) is the deuterium labeled TDHL (HY-12714). TDHL (Tergurid) is a dopamine receptor agonist with a Kd of 0.39 nM for D2 receptor and an orally available 5-HT-2 receptor antagonist.

Neramexane mesylate is an α9α10 cholinergic nicotinic receptors and N-methyl-D-aspartate receptors(NMDA) antagonist. Neramexane mesylate can improve moderate to severe tinnitus, and also shows neuroprotective effects.

Cannabidiolic acid methyl ester (HU-580) is an orally active cannabidiolic acid analogue. Cannabidiolic acid methyl ester can enhance the activation of 5-HT_1A receptor and increase the expression of c-Fos and NeuN in specific hypothalamic nuclei of rats. Cannabidiolic acid methyl ester has anti-nausea, anti-anxiety and anti-injury effects.

MAO-B-IN-45 is a dual inhibitor of ferroptosis and MAO-B. MAO-B-IN-45 shows selectivity towards MAO-B with an IC₅₀ of 87.47 nM and selectivity exceeding 229-fold for MAO-B over MAO-A. MAO-B-IN-45 has excellent antiferroptosis activity through modulation of the iron metabolic pathway and GSH-GPX4 axis in vitro. MAO-B-IN-45 improves cognitive and behavioral impairments in 3×Tg (APP/Tau/Ps1) AD mouse and significantly reduced the levels of ferritin heavy chain 1 (FTH1), APP, and Tau phosphorylation (p-Tau) proteins in the brain.

N-PTyrosine PA (N-Palmitoyl-tyrosine phosphoric acid) ammonium is a lysophosphatidic acid (LPA) receptor modulator, which exhibits weak inhibitory activity against LPA1 and partial agonist properties towards LPA5. N-PTyrosine PA ammonium inhibits the activation of LPA receptors and downstream responses by competing with agonists for binding sites. N-PTyrosine PA ammonium can induce morphological changes and aggregation, and also inhibit LPA-induced morphological changes through receptor desensitization caused by pre-incubation. N-PTyrosine PA ammonium can be used in the research of related diseases such as atherosclerosis and acute ischemic syndromes (e.g., unstable angina, myocardial infarction, stroke).

2002-H20 is an inhibitor of Aβ42-induced cytotoxicity, with the activity of reducing the cytotoxicity of Alzheimer's disease Aβ peptide by binding to it. 2002-H20 protects cells and reduces Aβ toxicity by promoting fibril formation, possibly by accelerating Aβ aggregation. The screening method of 2002-H20 effectively identifies compounds that reduce Aβ toxicity and presents potential inhibitory leads.

Sercloremine hydrochloride (CGP 4718A) is a selective and reversible MAO-A and 5-HT-uptake inhibitor. Sercloremine hydrochloride can be used in the research of depression.

URB754 is a potent inhibitor of the endocannabinoid-deactivating enzyme monoacylglycerol lipase (MGL) with an IC₅₀ of 200 nM.

Indeloxazine hydrochloride is a 5-HT receptor and norepinephrine (NE) reuptake inhibitor. Indeloxazine hydrochloride is an antidepressant and cerebral activator.

Risdiplam-hydroxylate-d₃ is a Risdiplam-hydroxylate tritium substitute. Risdiplam (RG7916) is an orally administered, centrally and peripherally distributed SMN2 pre-mRNA splicing modifier that increases survival motor neuron (SMN) protein levels.

Pep4c is an inactive control peptide for Pep2m (HY-P1058). Pep4c lacks functional activity to disrupt Protein Interacting with C Kinase 1 (PICK1)-AMPA receptor (GluA2) or N-ethylmaleimide-sensitive factor (NSF)-GluA2 interactions. Pep4c is used as a negative control in experiments to validate the specificity of Pep2m's effects on AMPA receptor trafficking and synaptic plasticity^{[1][2][3][4][5][6]}.

Anhydro-Ouabain (compound 20) is a cardiotonic steroid which shows anti-inflammatory and neuroprotective activities and thus can be used in neurological research.

Anabasine ((S)-Anabasine) hydrochloride is an alkaloid that found as a minor component in tobacco (Nicotiana). Anabasine is a botanical pesticide nicotine, acts as a full agonist of nicotinic acetylcholine receptors (nAChRs). Anabasine induces depolarization of TE671 cells endogenously expressing human fetal muscle-type nAChRs (EC₅₀=0.7 µM).