retinal permeability

BNN27 is an agonist of the TrkA receptor (TrkAreceptor) and the p75NTR receptor (p75NTR receptor), exhibiting neurotrophic and anti-apoptotic properties. It enhances levels of glutamate, GABA, and glutamine in the hippocampus and prefrontal cortex of rats, improving glutamate turnover. In a mouse model of amyotrophic lateral sclerosis (ALS), BNN27 demonstrates neuroprotective effects, shows anti-inflammatory properties in an experimental autoimmune encephalomyelitis (EAE) model, and exhibits retinal protection in a rat diabetes model. BNN27 also possesses blood-brain barrier permeability.

PB1 is a highly-effective intracellular disulfide reducing agent with notable attributes such as excellent cell permeability, the capacity to generate a substantial intracellular concentration gradient, and remarkable stability. It serves as a borane-protected TCEP (tris(2-carboxyethyl)phosphine) analogue. PB1 demonstrates the potential to enhance the survival of retinal ganglion cells following axotomy in vitro at concentrations in the nanomolar and picomolar range. Consequently, PB1 has proven instrumental in the study of neuroprotective properties[1][2][3].

PB2, a tris(2-carboxyethyl)phosphine (TCEP) analogue, enhances the survival of retinal ganglion cells (RGCs) following axotomy in vitro. Even at nanomolar and picomolar concentrations, PB2 demonstrates pronounced efficacy in promoting RGC survival. Notably, PB2 exhibits superior permeability compared to TCEP. Serving as a potent reducing agent, PB2 provides robust neuroprotection for RGCs[1].

SPHINX31 is a potent inhibitor of serine arginine-rich protein kinase 1 (SRPK1; IC50: 5.9 nM).

PKC-IN-4 (compound 7l) is a highly potent and orally active inhibitor of atypical protein kinase C (aPKC), with an IC 50 value of 0.52 µM. In vitro studies show that PKC-IN-4 effectively suppresses NF-κB activity induced by TNF-α and impedes retinal vasculature permeability induced by both VEGF and TNF-α. [1]

Angiogenesis inhibitor BT2 is a novel inhibitor of angiogenesis and vascular permeability, inhibiting ERK phosphorylation and the expression of FosB ΔFosB, VCAM-1, and many genes involved in proliferation, migration, angiogenesis, and inflammation, interacting with MEK1, suppressing retinal CD31, pERK, VCAM-1, and VEGF-A165 expression.

Abicipar pegol (AGN-150998, MP0112), an anti-VEGF DARPin molecule, is a novel class of small ankyrin repeat domain-containing proteins designed for high specificity and affinity targeting. This compound effectively inhibits angiogenesis and vascular permeability, and has been applied in ocular inflammation-related disease studies through intravitreal injections, significantly reducing mean retinal thickness and leakage area [1] [2].

Sp-8-Br-PET-cGMPS is a membrane-permeable PKG activator and an inhibitor of the membrane-permeable retinal cGMP-gated ion channels (cGMP-gated ion channel). It also serves as an activator for cGMP-dependent protein kinase I α and β. Resistant to mammalian cyclic nucleotide-dependent phosphodiesterases, Sp-8-Br-PET-cGMPS does not undergo metabolic side effects and exhibits stronger lipophilicity and permeability compared to Sp-8-pCPT-cGMPS. This compound is useful for investigating the role of the cGMP signaling pathway in the nervous system.