dorsal

AP-18 is a potent and selective TRPA1 inhibitor. AP-18 inhibits activation of TRPA1 induced by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 could reverse complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 could attenuate Yo-Pro uptake induced by 30 μM AITC in a concentration-dependent manner (IC50= 10.3 μM).

Sulfoxaflor (GF 2032) is an agonist of nAChR1 and nAChR2 subtypes and a systemic insecticide that acts on the insect central nervous system. Sulfoxaflor was found to have some effects on peripheral blood lymphocytes and is used to control sap-feeding insects such as brown planthopper, whitefly, peach aphid, and cotton aphid.

SKF-83566 is a blood-brain permeable and orally active antagonist of D1-like dopamine receptor and a weaker competitive 5-HT2 receptor antagonist with Ki of 11 nM

CGP 29030A is a new piperazine derivative with analgesic activity and significant inhibitory effect on potentially nociceptive dorsal horn neurons, which can be used to study painful disorders.

Zoliprofen is a potent and orally available non-steroidal anti-inflammatory agent with anti-inflammatory, antipyretic and analgesic activity, and inhibits carobolin, mycobacterium, and knife-ball protein A-induced rat paw oedema, as well as anti-rat serum-induced fracture or dorsal skin oedema. Zoliprofen is 20 times more effective than ibuprofen and fenoprofen against collagen- or arachidonic acid-induced platelet aggregation in rats and rabbits. Zoliprofen was 20 times more effective than ibuprofen and fenoprofen in inhibiting endotoxin-induced diarrhoea in mice and arachidonic acid-induced acute mortality in rabbits.

ZZL-7 is a fast-onset antidepressant agent that disrupts the interaction between neuronal nitric oxide synthase (nNOS) and the serotonin transporter (SERT) in the dorsal raphe nucleus (DRN). It easily crosses the blood-brain barrier and has research value in major depressive disorder (MDD).

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

LY-266097, a selective 5-HT2BR antagonist, effectively reduces tactile hypersensitivity and demonstrates potential therapeutic effects in alleviating pain caused by nerve injury. Additionally, it decreases the upregulation of 5-HT2B receptors in the dorsal root ganglia and spinal cord following nerve damage. Research indicates that LY-266097 may play a potential role in the development of neuropathic pain pathways.

Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active activator of Kv7.2/Kv7.3 channels and the TSPO. It activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). This compound protects motor neurons from degeneration caused by exposure to astrocyte-conditioned media from mice and humans with amyotrophic lateral sclerosis/frontotemporal dementia. Additionally, Kv7.2/Kv7.3 activator-3 stimulates axonal growth in dorsal root ganglia through TSPO and Kv7.2/3 activation and exhibits anticonvulsant effects in epilepsy models. It alleviates hyperalgesia in diabetic neuropathy patients, enhances the survival and regeneration of neurons after cervical neuropathy in rats, and accelerates the recovery of normal function in sensory and motor neurons.

1-Deoxyceramide (m18:1/20:0) is a type of ceramide. Its levels increase in the dorsal root ganglia of mice treated with Docetaxel.

OT-7100 is an orally active analgesic that may inhibit hyperalgesia by enhancing adenosine neurotransmission in the dorsal horn. This compound can be utilized in research related to inflammatory, neurological, and metabolic diseases such as diabetes.

LI-633 is a selective orally bioactive GABAA receptor positive allosteric modulator (PAM) with a Ki value of 21 nM. It significantly enhances GABA-induced inward currents, with EC50 values ranging from 8 nM (α5β2γ2) to 128 nM (α3β2γ2). LI-633 also increases muscimol-induced GABAergic currents in rat dorsal root ganglion (DRG) neurons, with an EC50 of 70.4 nM. LI-633 is useful for studying visceral pain.

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.

ADCI is an inhibitor of voltage-activated sodium channels and N-methyl-D-aspartate (NMDA)-receptor-gated channels. Inhibition of sodium channels by ADCI was voltage dependent. High doses of ADCI increased dopamine metabolism in the prefrontal cortex and/o

Globotriaosycleramides are glycosphingolipids found in mammalian cell membranes that are synthesized from lactosylceramides . They act as receptors for Shiga and Shiga-like toxins in vitro and in vivo. Globotriaosylceramides accumulate in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A. Globotriaosylceramides act as natural resistance factors to HIV infection, interacting with HIV gp120 to prevent its interaction with chemokine co-receptors and subsequent fusion of HIV to host cell membranes. This product contains a mixture of hydroxy fatty acid-containing globotriaosylceramides isolated from porcine red blood cells (RBCs).

Globotriaosycleramides are glycosphingolipids found in mammalian cell membranes that are synthesized from lactosylceramides . They act as receptors for Shiga and Shiga-like toxins in vitro and in vivo. Globotriaosylceramides accumulate in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A. Globotriaosylceramides act as natural resistance factors to HIV infection, interacting with HIV gp120 to prevent its interaction with chemokine co-receptors and subsequent fusion of HIV to host cell membranes. This product contains a mixture of hydroxy and non-hydroxy fatty acid-containing globotriaosylceramides isolated from porcine red blood cells (RBCs).

C16 globotriaosylceramide is an endogenous sphingolipid found in mammalian cell membranes that is synthesized from C16 lactosylceramide . C16 globotriaosylceramide acts as a receptor for Shiga toxin in B cell-derived Raji cells and THP-1 monocytes. It accumulates in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease. C16 globotriaosylceramide is also upregulated in plasma of patients with ovarian carcinoma compared to those with benign ovarian tumors or uterine fibroids.

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.

L-AP4 (L-APB) monohydrate is a potent and specific agonist for group III mGluRs, with EC50s of 0.13, 0.29, 1.0, and 249 μM for mGlu4, mGlu8, mGlu6, and mGlu7 receptors, respectively [1][2].

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)

N-Palmitoyl Glycine is an endogenous lipid that modulates calcium influx and nitric oxide (NO) production in sensory neurons. It is associated with an increased risk of Brugada syndrome (BrS), interacts with BrS-related proteins, and shows moderate binding affinity to molecules including DCC, CR1, CTSB, NAAA, DEFB1, EPHA1, IGF1/IGFBP3/ALS, and LTA.

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

C18 globotriaosylceramide is an endogenous sphingolipid found in mammalian cell membranes that is synthesized from lactosylceramide . It inhibits aggregation of human neutrophils induced by phorbol 12-myristate 13-acetate (PMA; 10008014) when used at a concentration of 1 μM. C18 globotriaosylceramide acts as a receptor for Shiga toxin in B cell-derived Raji cells and THP-1 monocytes. It accumulates in the brain, heart, kidney, liver, lung, and spleen in a mouse model of Fabry disease, a lysosomal storage disorder characterized by a deficiency in the enzyme α-galactosidase A. C18 globotriaosylceramide also accumulates in endothelial cells, pericytes, vascular smooth muscle cells, renal epithelial cells, dorsal ganglia neuronal cells, and myocardial cells in patients with Fabry disease.

Resolvin D4 (RvD4) is a specialized pro-resolving mediator derived from docosahexaenoic acid . [1] It has been detected in human milk, in the dorsal pouch of mice before and after infection with S. aureus, and in untreated tissues from humans, mice, and sardines.[2][3] RvD4, at 10 ng/mouse, reduces neutrophil infiltration in zymosan A-induced peritonitis and, at 200 ng/mouse, diminishes neutrophil infiltration in response to S. aureus infection. [3] With isolated cells, RvD4 promotes phagocytosis of bacteria, opsonized zymosan A, and apoptotic neutrophils by human macrophages.[3] It also promotes the clearance of apoptotic neutrophils by human fibroblasts.[3] Reference:[1]. Serhan, C.N., and Savill, J. Resolution of inflammation: The beginning programs the end. Nature Immunology 6(12), 1191-1197 (2005).[2]. Arnardottir, H., Orr, S.K., Dalli, J., et al. Human milk proresolving mediators stimulate resolution of acute inflammation. Mucosal. Immunol. 9(3), 757-766 (2016).[3]. Winkler, J.W., Orr, S.K., Dalli, J., et al. Resolvin D4 stereoassignment and its novel actions in host protection and bacterial clearance. Sci.Rep. 6, (2016).