Neurological Disease

Brompheniramine (maleate) (Standard) is the analytical standard of Brompheniramine (maleate). This product is intended for research and analytical applications. Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC₅₀s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.

VGSCs-IN-1 (compound 14), a 2-piperazine analog of Riluzole (HY-B0211), is a human voltage-gated sodium channels (VGSCs) inhibitor. VGSCs-IN-1 shows great Nav1.4 blocking activity. VGSCs-IN-1 has a pKa of 7.6 and a cLog P of 2.4. VGSCs-IN-1 can be used for cell excitability disorders research.

Carbenoxolone-d₄ is the d₄ labeled Carbenoxolone (HY-B1588). Carbenoxolone is a blood-brain barrier-permeable Pannexin1 inhibitor, gap junction (Gap junction) blocker, and β-amyloid 42 inhibitor. Carbenoxolone modulates voltage-gated currents of wild-type and mutant Panx1, and inhibits stimulus-activated Panx1 channel function. Carbenoxolone interacts with stable residues of β-amyloid 42 peptides, fibrils and oligomers, thereby inhibiting their aggregation. Carbenoxolone alleviates liver fibrosis. Carbenoxolone exerts neuroprotective and nootropic effects. Carbenoxolone can be used in studies related to Alzheimer's disease and liver fibrosis.

Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC₅₀=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation.

Atomoxetine-d₅ (hydrochloride) is the deuterium labeled Atomoxetine hydrochloride. Atomoxetine hydrochloride is a potent and selective noradrenalin re-uptake inhibitor (Ki values are 5, 77 and 1451 nM for inhibition of radioligand binding to human NET, SERT and DAT respectively).

D-Heptamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Heptamannuronic acid can be used for the research of pain and vascular dementia.

α-synuclein-IN-16 (Compound H1) is a α-synuclein inhibitor. α-synuclein-IN-16 significantly inhibits the secondary nucleation in α-synuclein aggregation. α-synuclein-IN-16 can be used for Parkinson’s disease research.

A-1048400 is an orally active and selective calcium channel inhibitor with an IC₅₀ value of 1.4 μM for N-type channels, 1.2 μM for T-type channel. A-1048400 inhibits neurotransmitter release and reduces membrane hyperexcitability, exerting potent analgesic activity. A-1048400 is promising for research of neuropathic pain (e.g., pain induced by spinal nerve ligation and chronic constriction injury).

KBR 2822 is an inhibitor of neurological target esterase (NTE) and has an inhibitory effect on AChE. KBR 2822 can aggravate neurological damage under certain conditions, but does not cause neurological disease when used alone in the absence of direct neurotoxicity or biochemical damage.

Eslicarbazepine-d₃ (BIA 2-194-d₃) is the deuterium labeled Eslicarbazepine (HY-114703). Eslicarbazepine is an oral anticonvulsant indicated for the adjunctive treatment of partial seizures.

25I-NBF hydrochloride is a highly potent partial agonist for the 5-HT2A receptors receptor with a K_i value of 0.26 nM and an EC₅₀ value of 1.6 nM.

N-Desmethylolanzapine-d8 hydrochloride (N-Demethylolanzapine-d8 hydrochloride) is the deuterium labeled N-Desmethylolanzapine (HY-W009247). N-Desmethylolanzapine is an antipsychotic drug. The formation of N-Desmethylolanzapine correlates with the level and activity of human liver flavin-containing monooxygenase (FMO3). N-Desmethylolanzapine can be used in the study of antipsychotic drugs .

Phlo1a (μ-TrTx-Phlo1a) is a peptide toxin contains 35-amino acid residues. Phlo1b is a selective Nav1.7 inhibitor. Phlo1a has a weak inhibitory effect on Nav1.2 and Nav1.5.

GABAA receptor modulator-12 (Compound 5) is a GABA_A receptor modulator. GABAA receptor modulator-12 inhibits anesthetic-induced desensitization of GABA_A α3β3γ2 receptors with an IC₅₀ of 0.2 μM. GABAA receptor modulator-12 can be used in the research of central nervous system disorders.

Lexanopadol (GRT-6006) is a μ-opioid receptor and nociceptor receptor (ORL-1 receptor) agonist. Lexanopadol can be used to study pain.

TAT-QFNP12 is a peptide that blocks the NDRG2-PPM1A binding and reduces Smad2/3 phosphorylation, decreases astrocytic MMP-9 production and BBB disruption after subarachnoid hemorrhage (SAH).

GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagonist with an IC₅₀ value of 74.01, nM. GluN2B-NMDAR antagonist-2 shows mild cytotoxicity. GluN2B-NMDAR antagonist-2 decreases the cerebral infarction rates and neurologic deficit scores. GluN2B-NMDAR antagonist-2 has the potential for the research of stroke.

F992 is an antidiuretic peptide and vasopressin (antidiuretic hormone) analogue.

2-MeSADP is a P2Y receptor agonist, with an EC₅₀ of 5 nM for human P2Y12, EC₅₀ values of 19 nM and 13 nM for human P2Y13, and an EC₅₀ of 6.2 nM for mouse P2Y13. It shows slightly higher selectivity for P2Y12 over human P2Y13. 2-MeSADP triggers increases in intracellular calcium levels, Gi-mediated cAMP inhibition, adenylate cyclase inhibition and downstream signal transduction. 2-MeSADP can be used in research related to glaucoma.

DR/5-HT7AR Ligand-1 is a ligand with a K_i value of 1.24 nM against human D2R, 5.78 nM against human D3R, 0.67 nM against human 5-HT1AR, and 19.9 nM against human 5-HT7AR. DR/5-HT7AR Ligand-1 can be used for the research of schizophrenia.