Neurological Disease

Brofoxine is a progesterone receptor modulator with anti-anxiety properties.

LY86057 is an ergoline derivative without N1 substituents. It has higher affinity for porcine, squirrel monkey and human 5-HT2 receptors than rats and is an antagonist of 5-HT2 receptors. When studying the differences in recognition of a series of ergolines between species, LY86057 was found to be more selective for 5-HT2 receptors. Compared with LY53857, LY108742 resulted in a higher affinity for rat 5-HT2 receptors even when the N1 substituent was only methyl.

MAX8 is a synthetic β-hairpin peptide that folds rapidly and self-assembles into a β-sheet-rich fibrous hydrogel network via non-covalent crosslinking. MAX8 hydrogel exhibits excellent shear-thinning and self-healing properties, enabling precise delivery via syringe and maintaining local retention after implantation. MAX8 hydrogel can uniformly encapsulate cells while preserving their viability and morphology, and protect growth factors (e.g., NGF) and chemotherapeutic drugs from degradation. MAX8 is applicable for spinal cord injury repair, medulloblastoma treatment, and three-dimensional high-throughput drug screening.

LY310762 free base is a selective 5-HT_1D receptor antagonist with a K_i value of 249 nM for the guinea pig receptor. LY310762 free base blocks presynaptic 5-HT_1D autoreceptors and enhances potassium-stimulated [³H]5-HT outflow from guinea pig cortical slices. LY310762 free base abolishes the inhibitory effect of 5-CT (HY-135555)/L-694,247 (HY-101208) on sympathetic nerve-induced renal vasoconstriction mediated by prejunctional 5-HT_1D receptors. LY310762 free base potentiates the increase in extracellular 5-HT concentration induced by Fluoxetine (HY-B0102). LY310762 free base is used in research related to depression and diabetic nephropathy.

NO-711ME is a prodrug of NO-711. NO-711 is a potent and selective GABA uptake inhibitor.

Butabindide (UCL-1397) is a potent, selective tripeptidvl peptidase II (TPP II) inhibitor with K_i values of 7 nM and 10 μM for TPP II and TPP I, respectively. Butabindide inhibits TPP II to protect CCK-8 against inactivation.

Phazr-N3 is a near-infrared (NIR) environment-sensitive fluorescent probe used to monitor the entire aggregation process of Aβ42 (amyloid-β42) from monomers/early aggregates to mature fibrils and plaques. Phazr-N3 binds Aβ42 in a structure-independent manner, exhibits low micromolar affinity (K_d = 6.6 μM) for free, disordered Aβ42 under non-aggregating conditions, and produces a solvatochromic fluorescence shift driven by local polarity changes during aggregation. Phazr-N3 uses a 580/680 nm excitation/emission setting in Aβ aggregation^[1].

sFTX-3.3 is a Ca²⁺ channel antagonist with IC₅₀s of approximately 0.24 mM and 0.70 mM against P-type and N-type channels.

Japonipene G is a bisabolane-type sesquiterpene that exhibits no significant cytotoxicity toward neuronal cells at the tested concentrations, but shows no inhibitory activity against cobalt CoCl₂-induced neuronal cell death. Japonipene G can serve as a negative control or a mechanistic research tool for neuroprotection-related studies.

Senktide TFA is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC₅₀=0.5-3 nM). Senktide TFA less potently agonizes the NK1 receptor (EC₅₀=35 µM). Senktide TFA is promising for research of neurological disease.

AZD3783 is an orally active, blood-brain barrier-penetrant 5-HT₁B receptor antagonist. AZD3783 reverses agonist-induced hypothermia, inhibits separation-induced vocalizations in guinea pig pups, and acts as a moderately permeable glycoprotein substrate with moderate clearance. AZD3783 inhibits hERG channel activity. AZD3783 is applicable for research on depression, anxiety disorders, and other psychiatric diseases associated with serotonergic neurotransmission.

Sp-8-CPT-cAMPS, a cAMP analog, is a potent and selective activator of the cAMP-dependent protein kinas A (PKA I and PKA II). Sp-8-CPT-cAMPS selects site A of RI compares to site A of RII by 153-fold and site B of RII compares to site B of RI by 59-fold.

TISCH is a potent and selective iodinated ligand with high affinity and selectivity for CNS D1 dopamine receptors. TISCH showed a K_d value of 0.205 nM in rat striatal tissue, indicating its effectiveness in biological activity. TISCH is able to easily cross the blood-brain barrier and show distribution in specific areas with D1 receptor density. TISCH is considered to be useful as a pharmacological tool for characterizing D1 dopamine receptors. When labeled with I-123, TISCH has the potential to be used as an in vivo imaging agent for CNS D1 dopamine receptors.

L-Aspartic acid-1,4-¹³C₂,¹⁵N is the ¹⁵N, ¹³C-labeled L-Aspartic acid (HY-N0666). L-Aspartic acid is a NMDA receptor agonist and acidic amino acid. L-Aspartic acid has no independent analgesic activity. L-Aspartic acid can antagonize the analgesic effects of D-Aspartic acid and Morphine. L-Aspartic acid regulates polymorph transformation, crystal growth/aggregation and nucleation processes of calcium carbonate, and can serve as a biomineralization template. L-Aspartic acid promotes burst firing of central neurons. L-Aspartic acid can be used in studies related to cerebral ischemia and epilepsy.

[D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) is a potent neurokinin NK1 antagonist. [D-Pro4,D-Trp7,9,Nle11] Substance P (4-11) inhibits the effects of gold-protein-substance P (GPSP) and substance P (SP).

Neurofilament, U-¹⁵N is the ¹⁵N-labeled Neurofilament.

Rufutalkib is an orally active ALK modulator. It possesses thermodynamic and chemical stability, and can be used in research related to anaplastic large cell lymphoma, non-Hodgkin's lymphoma, inflammatory myofibroblastic tumor, neuroblastoma, glioblastoma, and ALK-positive malignancies.

Tasipimidine is an orally active and selective α_2A-adrenoceptor agonist with a pEC₅₀ of 7.57 for human α_2A-adrenoceptors and an EC₅₀ of 5.7 nM for rat α₂-adrenoceptor. Tasipimidine can be utilized in research related to situational anxiety and fear.

AChE/MAO-B-IN-6 (compound 3a) is a dual inhibitor of AChE and h-MAO-B with potential to inhibit Alzheimer's disease.

α1b-AR antagonist 1 (Compound Cpd1) is a selective α₁B-AR antagonist. Alpha1b-ar antagonist 1 can be used in the study of cardiovascular and central nervous system diseases.