Neuroscienza

13,14-dihydro-15-keto Prostaglandin E2 (13,14-dihydro-15-keto PGE2) serves as the predominant metabolite of PGE2 in plasma, created through a 15-keto PGE2 intermediate by the action of 15-oxo-PG Δ13 reductase. Unlike its precursor PGE2, this compound exhibits poor binding affinity towards EP2 and EP4 PGE2 receptors (Ki values of 12 and 57 µM, respectively) in CHO cells and fails to stimulate adenylate cyclase activity therein (EC50s >18 and >38 µM, respectively). Concentrations of 13,14-dihydro-15-keto PGE2 are notably higher in the plasma of pregnant women during their third trimester and at labor and delivery stages, whereas its levels are found to be reduced in the tumor tissues of patients with non-small cell lung cancer (NSCLC) compared to adjacent healthy tissue.

Facinicline hydrochloride (RG3487) is both a novel nicotinic alpha-7 receptor (alpha7nAChR) partial agonist (Ki = 6 nM) and an antagonist of 5-HT3(Ki = 1.2 nM).

3β-Hydroxy-lup-20(29)-en-16-one (compound 9) serves as a dual inhibitor of both AChE and BChE, displaying a preference for BChE with an IC50 of 28.9 μM [1].

AAK1-IN-2, a potent (IC50=5.8 nM) AAK1 inhibitor, selective & brain-penetrant, is used for neuropathic pain studies.

CGP 55845: potent, selective GABAB blocker, IC50=5 nM, hinders agonist binding, reduces GABA/glutamate release.

AChE-IN-30 is an acetylcholinesterase inhibitor (IC50 4.4 μM) that reduces oxidative stress and apoptosis, useful for Alzheimer’s disease research models.

MAO-B-IN-13: a potent, reversible MAO-B inhibitor with BBB penetration, neuroprotective effects; used in Parkinson’s research (IC50=10nM).

QM-FN-SO3 is a blood-brain barrier (BBB)-penetrable, near-infrared (NIR) probe with aggregation-induced emission (AIE) activity, specifically designed for the detection of Aβ plaques. It exhibits ultra-high signal-to-noise (S/N) ratio, binding affinity, and high-performance NIR emission, making it suitable for in vivo detection of Aβ plaques [1].

Quinolactacin A1, a strong AChE inhibitor from Penicillium citrinum, aids Alzheimer's research.

AAK1-IN-5: Potent, selective AAK1 inhibitor; CNS-penetrant; oral; IC50: 1.2 nM; Ki: 0.05 nM; cell IC50: 0.5 nM. Useful in neuropathic pain research.

mGAT3/4-IN-2 are potent inhibitors of mGAT3/mGAT4 with their pIC50 values of 5.44 and 5.25, respectively.

AAK1-IN-4 selectively inhibits AAK1 with IC50 of 4.6 nM; penetrates CNS, oral bioactive, potential for studying neuropathic pain.

AChE-IN-31 (compound 1), a non-competitive acetylcholinesterase (AChE) inhibitor, exhibits potential for Alzheimer's disease research [1].

AAK1-IN-3: Brain-penetrant AAK1 inhibitor for neuropathic pain research; IC50=11 nM.

VU0029251 serves as a partial antagonist of mGluR5, exhibiting a binding affinity with a K i of 1.07 μM.

Robalzotan is a selective 5-HT1A receptor antagonist.

Fosthiazate is a broad-spectrum nematicide that combats a range of plant parasitic nematodes such as Meloidogyne spp., Globodera spp., and Pratylenchus spp., by

SDZ-216525, a 5-HT1A receptor antagonist, inhibits the tracheal contractions induced both by NKA (10 nM-3 microM) and 5-HT (10 nM-10 microM) (n=4-10).

(R)-4-Amino-3-hydroxybutyric acid, also known as (R)-GABOB, acts as a modulator of GABA receptors, specifically binding to both GABAA and GABAB receptors and blocking GABA reuptake in rat brain synaptosomes. Additionally, it serves as a GABAC receptor agonist, triggering currents in patch-clamp assays with Xenopus oocytes that express the human receptor. In vivo studies reveal its capability to suppress electrical discharges in the amygdala in cats undergoing N-amidinobenzamide-triggered seizures, indicating its potential therapeutic application in managing seizure disorders.

COR659: suppresses alcohol/chocolate intake in rats; enhances GABAB receptor, blocks CB1 receptor.