ganglion

Pempidine (1,2,2,6,6-Pentamethylpiperidine) is a nicotinic antagonist and has been used as a ganglionic blocker for treating hypertension.

Dermorphin is agonist of μ-opioid receptor (MOR) agonist.

Sulbutiamine (Bisibuthiamine) is an antioxidant that act by inhibiting oxidative stress induced retinal ganglion cell death.

CYM5442 is an S1P agonist, targeting to Sphingosine.

VIP(6-28)(human, rat, porcine, bovine) acetate is an antagonist of the actions of exogenous vasoactive intestinal peptide (VIP) receptor on cAMP in the superior cervical ganglion (SCG).

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.

MRS 1523 can exert an antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons. MRS 1523 is an effective and selective adenosine A3 receptor antagonist Ki: 18.9 nM and 113 n

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.

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

AS1069562 is an inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake which acts by notably restoring reduced insulin-like growth factor 1 and fibroblast growth factor 2 mRNA levels in dorsal root ganglion and spinal cord, respectively.

PNU109291, a potent and selective agonist of the 5-HT1D receptor, effectively mitigates dural plasma extravasation induced by trigeminal ganglion stimulation.

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.

Amifostine Hydrate is a radiation protective agent that induces splenic vasodilation and blocks autonomic ganglion.

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].

PDDHV is a resiniferatoxin-type phorboid vanilloid with capsaicin-like selectivity for the cloned rat transient receptor potential cation channel subfamily V member 1 (TRPV1), formerly known as vanilloid receptor 1. It induces Ca2+-uptake by rat dorsal root ganglion neurons with an EC50 value of 70 nM.

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

C16 3'-sulfo Galactosylceramide (d18:1 16:0) is a sulfated glycolipid.C16 3'-sulfo Galactosylceramide (d18:1 16:0) is a relatively abundant sulfide found in porcine brain and plasma that decreases throughout development in mice.C16 3'-sulfo Galactosylceramide is a relatively abundant sulfide found in porcine brain and plasma that decreases throughout development in mice.C16 3'-sulfo Galactosylceramide is a relatively abundant sulfide found in porcine brain and plasma that decreases throughout development in mice. C16 3'-sulfo Galactosylceramide (d18:1 16:0) inhibits retinal ganglion cell growth in vitro.C16 3'-sulfo Galactosylceramide (d18:1 16:0) has been used as an internal standard for quantifying C16 3'-sulfo Galactosylceramide (d18:1 16:0) in rat cerebellum and white matter isolated from patients with multiple sclerosis. reference for sulphides.

(+)-Sparteine (sulfate pentahydrate) is a ganglion blocker that competitively inhibits nicotinic acetylcholine receptors in neurons.

Trimetaphan camsilate is a drug that counteracts cholinergic transmission at the ganglion type of nicotinic receptors of the autonomic ganglia and therefore blocks both the sympathetic nervous system and the parasympathetic nervous system. It acts as a non-depolarizing competitive antagonist at the nicotinic acetylcholine receptor, is short-acting, and is given intravenously.

NMDAR TRPM4-IN-2 is a potent interfacial inhibitor of NMDAR TRPM4 interaction.NMDAR TRPM4-IN-2 protects against MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss in mice.NMDAR TRPM4-IN-2 has neuroprotective activity against NMDA-induced hippocampal neuronal cell death and mitochondrial dysfunction. NMDAR TRPM4-IN-2 showed neuroprotective activity against NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons with an IC50 value of 2.1 μM.

α-Conotoxin Vc1.1 TFA is a peptide isolated from Conus victoriae and a selective nAChR antagonist that inhibits α3α5β2, α3β2 and α3β4, reversing mechanical allodynia in neuropathic pain models and can be used to study neuropathic chronic pain. α-Conotoxin Vc1.1 TFA inhibits human dorsal root ganglion nerve excitability and mouse colon nociception via GABA(B) receptors.