sensory neurons

CRMP2-Ubc9-NaV1.7 inhibitor 194, is a CRMP2-Ubc9-NaV1.7 inhibitor.

AMG-0347 (UNII-CD7L9290QR) is a small molecule inhibitor targeting TRPA1(transient receptor potential ankyrin 1) ion channels, a receptor found in sensory neurons and involved in the detection of pain and environmental stimuli. AMG-0347 acts by blocking the function of TRPA1 and has analgesic effects.

Picaridin (Lcaridin) is a topical insect repellent.

BT-13 is a selective agonist of glial cell line-derived neurotrophic factor (GDNF) receptor RET independently of GFLs. BT-13 promotes neurite growth from sensory neurons in vitro.

AUT2 is a Kv3.1 channel modulator with the potential to treat sensory hyperreactivity in patients with FXS by shifting the activation of high-threshold currents to more negative potentials. This shift reduces high-threshold K+ currents and increases low-threshold K+ currents in neurons, restoring wave IV of the ABR. Due to its ability to regulate neuronal excitability, AUT2 is also promising for the treatment of hearing impairments.

SBI-810 hydrochloride is a β-arrestin-2 (βarr2)-biased allosteric modulator of NTSR1 (neurotensin receptor 1), exerting analgesic effects through peripheral and central mechanisms by inhibiting excitatory synaptic transmission, suppressing NMDA receptor and ERK signalling in spinal nociceptive neurons, and reducing Nav1.7 expression and action potential discharge in primary sensory neurons.

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.

EG01449 is a quinoline-based neuropilin-1 (NRP1) antagonist with a Kd of 0.6 µM. It competitively inhibits the binding of VEGFA to NRP1 with an IC50 of 362 nM, preventing VEGFA-induced pain by inhibiting NRP1-dependent signaling and reducing sodium currents in sensory neurons. EG01449 can cross the blood-brain barrier, allowing for targeted actions within the central nervous system, and is utilized in pain research.

EG01449 Free acid is a quinoline-based antagonist of neuropilin-1 (NRP1), exhibiting a Kd of 0.6 µM. It competitively inhibits the binding of VEGFA to NRP1, with an IC50 of 362 nM. By inhibiting NRP1-dependent signaling and reducing sodium currents in sensory neurons, EG01449 Free acid prevents VEGFA-induced pain. Additionally, it is capable of crossing the blood-brain barrier, allowing for targeted effects within the central nervous system. EG01449 Free acid is applicable for pain research.

CN016 is a neuroprotective agent. It inhibits the elevation of pro-inflammatory cytokines G-CSF, GM-CSF, and IL-6 induced by Oxaliplatin. Additionally, CN016 suppresses the inflammatory response and the infiltration of immune cells into sensory neurons induced by Paclitaxel. Furthermore, CN016 protects neurons from neurotoxic damage induced by Paclitaxel and shields mice from Oxaliplatin-induced peripheral neuropathy.

Nav1.7-IN-22 (P58 13-2) is a selective inhibitor of the voltage-gated sodium channel Nav1.7. By blocking the activity of the Nav1.7 channel, Nav1.7-IN-22 suppresses the generation and transmission of abnormal electrical signals in sensory neurons. This compound is applicable for research related to pain.

Hh-Ag1.5 (SAG-1.5) is a potent Hedgehog (Hh) agonist (EC50: 1 nM) and Smoothened (Smo) receptor agonist, with an EC50 of 1 nM and Ki values between 0.5 and 2.3 nM for Smo. Hh-Ag1.5-mediated reprogramming breaks the quiescent state of non-injured hepatic stem cells and thus rescues liver failure. Hh-Ag1.5 induced differentiation of hiPSCs into skin precursor cells, spinal motor neurons and spinal sensory neurons.

Alosetron hydrochloride (GR 68755) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist. Alosetron blocks the actions of serotonin at 5-HT3 sites in the peripheral nervous system, particularly on enteric and nociceptive sensory neurons, thereby affecting the regulation of visceral pain, decreasing gastrointestinal contraction and motility, and decreasing gastrointestinal secretions.

OB-2 is an inhibitor of stomatin-like protein-3 (STOML3) oligomerization. OB-2 reversibly reduces the sensitivity of mechanically gated currents in sensory neurons and silence mechanoreceptors in vivo.

Satratoxin G is a trichothecene mycotoxin of Stachybotrys chartarum and has been shown to selectively induces apoptosis in olfactory sensory neurons (OSNs) of the nose and brain.

δ14-Triamcinolone acetonide is a potential impurity found in commercial preparations of triamcinolone acetonide. Triamcinolone acetonide is a synthetic corticosteroid. It decreases cytokine levels, the firing rate of sensory neurons, and mechanical hypersensitivity in a rat spinal nerve ligation model when used at a dose of 1.5 mg/kg prior to and following surgery for three days. Triamcinolone acetonide also decreases outflow facility in a mouse model of steroid-induced glaucoma when 20 μl of a 40 mg/ml suspension is administered subconjunctivally. Formulations containing triamcinolone acetonide are used in the treatment of diabetic macular edema.

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.

12(S)-HpETE is a monohydroperoxy polyunsaturated fatty acid (PUFA) produced by the action of platelet or leukocyte 12-lipoxygenase (12-LO) on arachidonic acid. It activates human blood leukocyte 5-LOE. 12(S)-HpETE is the mediator of many biological functions, including induction of c-fos and c-jun, activation of AP-1, and endothelium-dependent vasoconstriction. It mediates the inhibitory synaptic response to FMRF-amide in Aplysia sensory neurons and inhibits Ca2+/calmodulin-dependent protein kinase II from rat brain cortex.

IAA65 is a potent and highly selective transient receptor potential ankyrin 1 (TRPA1) inhibitor (IC50 = 4.3 nM). It demonstrates significant analgesic activity in animal models of inflammatory and neuropathic pain by competitively blocking TRPA1-mediated calcium influx in sensory neurons.

DD04107 is a novel inhibitor of α-calcitonin gene-related peptide (α-CGRP) exocytotic release from primary sensory neurons, selectively interacting with Synaptotagmin 1.

Urocortin II, mouse, is a selective and potent endogenous peptide agonist for the type-2 corticotropin-releasing factor (CRF2) receptor, displaying K_i values of 0.66 nM for CRFR2 and >100 nM for CRFR1, signifying its high specificity. It engages CRF2 receptors through mechanisms dependent on cAMP/PKA and Ca2+/CaMKII. Additionally, Urocortin II, mouse is localized in specific regions of the central nervous system, influencing central neurons that process visceral sensory information and regulate autonomic functions [1] [2] [3].

Insulin-like Growth Factor II (IGF-2), the primary somatomedin in human serum, exerts both permissive and direct influences on neurite outgrowth and significantly improves the survival of sympathetic and sensory neurons [1] [2].

Sodium Channel inhibitor 4 is a potent and selective NaV1.7 inhibitor (IC50 = 33 nM). It blocks action potential conduction in sensory neurons, exhibiting significant analgesic activity for neuropathic pain research.

NMB-1, a conopeptide analogue, selectively inhibits sustained mechanically activated currents in sensory neurons with an IC50 of 1 μM, attenuating mechanical pain. It is utilized in research pertaining to hearing and pressure-evoked pain [1] [2].