| Name | JTC-801 |
| Description | JTC-801 is a selective opioid receptor-like 1 (ORL1) receptor antagonist with an IC50 of 94 nM and weak inhibitory effects on δ, κ, and μ receptors. |
| Kinase Assay | A suspension of membranes from human μ-opioid receptor-expressing CHO-K1 cells in 50 mM Tris-HCl buffer (pH 7.4) containing 5 mM MgCl2 and 10% sucrose is incubated at room temperature for 2.5 h with 0.33 nM 3H-labeled diprenorphine and various concentrations of JTC-801. The membranes are collected by filtration using Whatman 934-AH, and radioactivity is counted with a TopCount A9912V scintillation counter. Nonspecific binding (6.4%) is determined with 10 μM naloxone. Specific binding is calculated by subtracting nonspecific binding from the total binding. Data are the mean±SE (n=3). |
| In vitro | JTC-801 displays about 12.5-, 129-, and 1055-fold selectivity for ORL1 receptor (Ki = 8.2 nM) over μ-, κ-, and δ-opioid receptors, respectively. JTC-801 does not inhibit forskolin-stimulated cyclic AMP accumulation in human ORL1 receptor-expressing HeLa cells, but it prevents nociceptin-induced inhibition of cyclic AMP accumulation, indicating that JTC-801 possesses full antagonistic activity. [2] In rat cerebrocortical membrane, JTC-801 inhibits ORL1 receptor with IC50 of 472 nM and μ-receptor with IC50 of 1831 nM. JTC-801 completely antagonizes the suppression of nociceptin on forskolin-induced accumulation of cyclic AMP with IC50 of 2.58 μM in HeLa cells expressing ORL1 receptor. [1] |
| In vivo | Oral administration of JTC-801 (0.3-3 mg/kg) antagonizes nociceptin-induced allodynia in mice, and shows analgesic effect in a hot plate test using mice and in a formalin test using rats. [2] In mouse hot-plate test, JTC-801 prolongs escape response latency (ERL) or exposed heat stimulus with minimum effective doses (MED) of 0.01 mg/kg by i.v. or 1 mg/kg by p.o. In the rat formalin test, JTC-801 reduces both the first and second phases of the nociceptive response with MED of 0.01 mg/kg71 by i.v. or 1 mg/kg by p.o. [1] JTC-801 dose-dependently normalizes paw withdrawal latency (PWL). Although JTC-801 does not inhibit a chronic constriction injury (CCI)-induced decrease in bone mineral content (BMC) and bone mineral density (BMD), it inhibits an increase in the number of osteoclasts. [3] Tactile allodynia induced by L5/L6 spinal nerve ligation is reversed by both systemic (3-30 mg/kg) and spinal (22.5 and 45 pg) JTC-801 in a dose-dependent manner. Furthermore, systemic JTC-801 reduces Fos-like immunoreactivity in the dorsal horn of the spinal cord (laminae I/II). [4] JTC-801 produces dose-dependent mechanical and cold anti-allodynic effects with ED50 of 0.83 mg/kg and 1.02 mg/kg, respectively. [6] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 44.8 mg/mL (100.01 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.46 mM), Sonication is recommended.
Ethanol : 9 mg/mL (20.09 mM), Sonication is recommended.
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| Keywords | OpioidReceptor | Opioid receptor-like1 (ORL1) | Opioid Receptor | JTC-801 | Inhibitor | inhibit |
| Inhibitors Related | Docusate sodium | Bevenopran | Mirtazapine | Matrine | (-)-Menthol | Cuminaldehyde | Progesterone | Naltrexone hydrochloride | Cebranopadol | BTRX-335140 | Bisacodyl | Mianserin hydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Endocrinology-Hormone Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
