ganglion cells

DL-AP5 is the racemic form of a selective N-methyl-D-aspartate (NMDA) receptor antagonist with anticonvulsant effects.

Y-33075 (Y-39983 free base) is a ROCK inhibitor that lowers intraocular pressure (IOP), increases blood flow to the optic nerve head (ONH), and increases the number of RGCs (retinal ganglion cells) in the body with regenerating axons.

Tonabersat (SB-220453) is a novel and orally available gap-junction modulator and CSD (Cortical spreading depression) inhibitor that regulates cellular communication between trigeminal ganglion neuronal cells and glial cells and inhibits neurogenic inflammation for the treatment of migraine and epilepsy.

TN-871 is a potassium and calcium channel antagonist. TN-871 modulates transmitter release from preganglionic nerve terminals without changing the postsynaptic sensitivity of the ganglion cells to ACh.

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].

CAY10787 is an oxysterol and a negative allosteric modulator of GABAAreceptors.1,2It reduces GABA-induced currents in HEK cells expressing α1β1γ2or α4β3γ2subunit-containing GABAAreceptors (IC50s = 1.5 and 1 μM, respectively).2CAY10787 (500 nM) reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.In vivo, CAY10787 (2, 10, and 50 mg/kg) increases latency to nocifensive behaviors in the hot plate test in mice. 1.Hahn, M., Tang, M., and Subbiah, M.T.Cholest-3,5-dien-7-one formation in peroxidized human plasma as an indicator of lipoprotein cholesterol peroxidation potentialBiochim. Biophys. Acta1255(3)341-343(1995) 2.Niu, C., Leavitt, L.S., Lin, Z., et al.Neuroactive type-A γ-aminobutyric acid receptor allosteric modulator steroids from the hypobranchial gland of marine mollusk, Conus geographusJ. Med. Chem.64(10)7033-7043(2021)

The acyl amides are a family of endogenous lipids that act as potent modulators of pain and inflammation. The best characterized members of this family are the arachidonoyl amides, which includes N-arachidonoyl ethanolamide (AEA; anandamide). N-palmitoyl glycine (PalGly) contains an 18-carbon saturated fatty acid that is amide-linked to glycine and is structurally similar to the phospholipid-derived N-acyl ethanolamines. Endogenously produced in rat skin and spinal cord, PalGly is present in 100-fold greater amounts in skin and 3-fold greater in brain compared to AEA. Injection of 0.43 μg PalGly in rat hindpaw inhibits heat-induced firing of nociceptive neurons in rat dorsal horn. PalGly treatment induces transient calcium influx in native dorsal root ganglion (DRG) cells and in the PTX-sensitive, DRG-like cell line F-11 (EC50 = 5.5 μM).

TREK1 and TREK2 channel activator (EC50 = 0.76 μM in Rb efflux assay in TREK1-expressing CHO cells). Exhibits selectivity for TREK1/2 over TRAAK, TASK3 and a range of other potassium channels. Hyperpolarizes membrane potential of dorsal root ganglion neurons and depresses neuronal activity in vitro. Loucif et al (2018) GI-530159, a novel, selective, mechanosensitive two-pore-domain potassium (K2P) channel opener, reduces rat dorsal root ganglion neuron excitability. Br.J.Pharmacol. 175 2272 PMID:29150838

ω-Conotoxin MVIID (SNX-238) is a peptide from the Conus genus that inhibits the ω-Conotoxin-GVIA-sensitive, high-threshold calcium (Ca 2+) current in fish retinal ganglion cells [1].

Neurotensin-related hexapeptide exists in retinal ganglion cells and in their central projections in pigeons and may be utilized as a neuroactive substance by the central terminals of numerous retinal ganglion cells in birds.