Neurological Disease

Levomepromazine (Standard) is the analytical standard of Levomepromazine. This product is intended for research and analytical applications. Levomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca²⁺ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca²⁺ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting.

GSK189254A hydrochloride is a novel, potent and selective histamine H3 receptor antagonist with pK_i values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.

UBP618 is a non-selective N-methyl-D-aspartate inhibitor.

Unconjugated/naked Etedesiran (without SMCC linker) is a small interfering RNA (siRNA) targeting DMPK, and also represents the unconjugated, non-SMCC linker-bound component of delpacibart etedesiran. Unconjugated/naked Etedesiran (without SMCC linker) corrects pathogenic mRNA aberrant splicing by targeting and degrading mutant DMPK mRNA, thereby releasing sequestered MBNL splicing factors. Unconjugated/naked Etedesiran (without SMCC linker) can be used in studies of myotonic dystrophy type 1.

Mebeverine acid-d₃ (Mebeverine metabolite Mebeverine acid-d₃) is the deuterium labeled Mebeverine Acid (HY-12769). Mebeverine acid is a secondary metabolite of the intestinal antispasmodic agent Mebeverine (HY-A0078). Mebeverine acid is generated by the hydrolysis of Mebeverine in the body and is considered a key circulating metabolite. Mebeverine acid is an important marker for oral Mebeverine.

Vasopressin (Standard) is the analytical standard of Vasopressin. This product is intended for research and analytical applications. Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis, and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of corticotropin releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors.

COX-2-IN-57 is an orally active COX-2 inhibitor with an IC₅₀ value of 0.02 μM. COX-2-IN-57 reduces MyD88 expression and decreases serum levels of COX-2, PGE2, and COX-1 in Cisplatin (HY-17394)/radiation-induced neuropathy rat model. COX-2-IN-57 demonstrates superior antinociceptive efficacy in hot plate, cold allodynia, and Randall-Selitto tests, along with hepato-/renal protection. COX-2-IN-57 can be used for the study of inflammation.

CCPA (2-Chloro-N6-cyclopentyladenosine (Standard)) is the analytical standard of CCPA (HY-103185). This product is intended for research and analytical applications. CCPA (2-Chloro-N6-cyclopentyladenosine) a highly selective A1 adenosine receptors agonist with a K_i of 0.4 nM. CCPA inhibits adenylate cyclase with an IC₅₀ of 33 nM. CCPA exhibits anti-seizure and cardiacprotective activity. CCPA can be used for the research of seizure and myocardial infarction.

ONO-2952 (Standard) is the analytical standard of ONO-2952 (HY-111191). This product is intended for research and analytical applications. ONO-2952 is a potent, selective and orally active translocator protein 18 K_da (TSPO) antagonist with K_i of 0.33-9.30 nM for rat and human TSPO. ONO-2952 is more selective for TSPO than other receptors, transporters, ion channels and enzymes. ONO-2952 exerts its anti-stress effects through inhibition of excessive activation of noradrenergic system in the brain without the amnesic effect. ONO-2952 has the potential for irritable bowel syndrome treatment.

Suzetrigine N-oxide (the third compound in P57) is a derivative of Suzetrigine (HY-148800). Suzetrigine N-oxide is an inhibitor of voltage-gated sodium channels (Nav1.8) and can be used for research on the treatment of pain, especially neuropathic pain.

3-O-Methyltolcapone (Standard) (Ro 40-7591 (Standard)) is the analytical standard of 3-O-Methyltolcapone (HY-174062). 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone (HY-17406). Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor with an IC₅₀of 773 nM. Tolcapone can inhibits α-syn and Aβ₄₂ oligomerization and fibrillogenesis. Tolcapone can cause oxidative stress and induce cancer cells apoptosis and ROS production. Tolcapone can be used for the researches of cancer and neurological disease, such as Parkinson disease and neuroblastoma.

Dihydromunduletone (Standard) is the analytical standard of Dihydromunduletone (HY-101483). This product is intended for research and analytical applications. Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent adhesion G protein-coupled receptor (aGPCR) (GPR56 and GPR114/ADGRG5) antagonist with an IC 50 of 20.9 μM for GPR56, but not inhibit GPR110 or class A GPCRs.

(1S,2S)-2-PCCA (hydrochloride) (Standard) is the analytical standard of (1S,2S)-2-PCCA (hydrochloride) (HY-100013B1). This product is intended for research and analytical applications. (1S,2S)-2-PCCA hydrochloride is a less active diastereomer of 2-PCCA. 2-PCCA is a GPR88 receptor agonist, and inhibits GPR88-mediated cAMP production, with an EC50 of 116 nM in HEK293 cells.

Lys-psi(CH2NH)-Trp(Nps)-OMe is a lysine-tryptophan (Nps) pseudodipeptide analog. It is obtained by replacing the peptide bond in the Lys-Trp(Nps) molecule with an aminomethylene bond and has analgesic activity. Lys-psi(CH2NH)-Trp(Nps)-OMe induces a dose-dependent and naloxone-reversible analgesia after intracerebroventricular administration in mice, and its analgesic effect lasts longer than that of the original compound. It protects methionine enkephalin from degradation in rat striatal slices and binds to low-dose opioid peptides to produce analgesia. Lys-psi(CH2NH)-Trp(Nps)-OMe effectively inhibits brain aminopeptidase activity both in vitro and in vivo. The enhanced resistance of this pseudodipeptide to proteolysis may explain its prolonged analgesic activity.

Gabaculine is an amino acid neurotoxin and blood-brain barrier-permeable GABA transaminase inhibitor, with an IC₅₀ of 1 μM in beef and Pseudomonas ovalis. Gabaculine elevates endogenous synaptic and brain GABA levels and enhances GABA activity. Gabaculine induces sedation, hypothermia, loss of righting reflex, and prevents convulsions in mice. Gabaculine is applicable to research related to neurological disorders.

Atomoxetine-d₅ (Tomoxetine-d₅) is deuterium labeled Atomoxetine. Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with K_i values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DA_EX and NE_EX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na⁺ channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research.

TTR stabilizer L6 (L6) binds to the T4 binding pocket of transthyretin (TTR), which can prevent the dissociation of TTR to monomer. TTR stabilizer L6 is promising for research of familial amyloid polyneuropathy.

PBT 1033 (Standard) is the analytical standard of PBT 1033. This product is intended for research and analytical applications. PBT 1033 (PBT 2) is an orally active copper/zinc ionophore. PBT 1033 restores cognition in mouse models of Alzheimer's disease (AD). PB 1033 also has antibacterial activity against Gram-positive bacteria.

Methylspinazarin is a potent inhibitor of catechol O-methyltransferase (COMT, IC₅₀ = 0.8 μg/ml) that can be isolated from Streptomyces. Methylspinazarin is selective for COMT over tyrosine hydroxylase.