synaptic plasticity

PDE2 inhibitor6 (Compound 1) is an orally active phosphodiesterase (PDE) inhibitor, effectively inhibiting PDE2A, PDE3B, and PDE10A2 with IC50 values of 0.95 nM, 6.17 μM (pIC50=5.21), and 87.1 nM (pIC50=7.06), respectively. It modulates AMPA receptor activity, enhances synaptic plasticity, and improves learning and memory in rat models. Furthermore, PDE2 inhibitor6 possesses blood-brain barrier permeability.

Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. It enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy [1].

Highly potent and selective group II metabotropic glutamate receptor antagonist. Disodium salt of LY 341495 Fitzjohn et al (1998) The potent mGlu receptor antagonist LY341495 identifies roles for both cloned and novel mGlu receptors in hippocampal synaptic plasticity. Neuropharmacology 37 1445 PMID:9886667 |Ornstein et al (1998) 2-Substituted (2SR)-2-amino-2-((1SR,2SR)-2-carboxycycloprop-1-yl) glycines as potent and selective antagonists of group II metabotropic glutamate receptors. 2. Effects of aromatic substitution, pharmacological characterization, and bioav J.Med.Chem. 41 358 PMID:9464367 |Johnson et al (1999) [3H]-LY341495 as a novel antagonist radioligand for group II metabotropic glutamate receptors: characterization of binding to membranes of mGlu receptor subtype expressing cells. Neuropharmacology 38 1519 PMID:10530814

AMPA-IN-1 is a potent inhibitor of AMPA receptors, widely expressed in the brain and central to the regulation of rapid excitatory synaptic transmission and synaptic plasticity. [14]

ZD7288 (ICI D7288), a selective hyperpolarization-activated cyclic nucleotide-gated channel blocker, inhibits hippocampal synaptic plasticity.

Neurogranin (48-76), mouse, is a peptide comprising residues 48-76 of Neurogranin, a post-synaptically exclusive calmodulin-binding protein that mediates NMDAR-driven synaptic plasticity by regulating the calcium-calmodulin (Ca2+-CaM) pathway [1].

Leptin (116-130), a bioactive fragment of leptin, enhances synaptic plasticity in the hippocampus by promoting AMPA receptor trafficking to synapses. It preserves hippocampal synapse integrity and prevents neuronal cell death in amyloid toxicity models, showing promise for Alzheimer's disease (AD) research [1].

DU-14, a powerful steroid sulfatase inhibitor, has an IC 50 of 55.8 nM and effectively inhibits MCF-7 cell proliferation with an IC 50 of 38.7 nM. It exhibits neuroprotective properties against neurotoxic Aβ, indicating that by increasing endogenous DHEAS, DU-14 could help alleviate Aβ-induced issues in spatial memory and synaptic plasticity [1] [2] [3].

Sp-8-pCPT-cGMPS is a potent agonist for cyclic guanosine monophosphate-gated (CNG) channels and serves as a lipophilic activator for PKG (types I α, I β, and II) and PKA II. It exhibits excellent cell membrane permeability and stability against phosphodiesterases. This compound is utilized in studying the role of cGMP in synaptic transmission and neural plasticity.

Pep63, a neuroprotective peptide (VFQVRARTVA), enhances synaptic plasticity and memory. It competitively binds with Aβ1-42 oligomers, thereby inhibiting the formation of Aβ fibrils. Pep63 is employed in research focused on Alzheimer's disease (AD).