Home Neuronal Signaling Opioid Receptor antagonist JTC-801 For research use only.

JTC-801

JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.

JTC-801 Chemical Structure

JTC-801 Chemical Structure

CAS No. 244218-51-7

Purity & Quality Control

Batch: S272201 DMSO]90 mg/mL]false]Ethanol]31 mg/mL]false]Water]Insoluble]false Purity: 99.94%
99.94

JTC-801 Related Products

Signaling Pathway

Opioid Receptor Signaling Pathways

Opioid Receptor Signaling Pathway

Biological Activity

Description JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.
Targets
Opioid receptor-like1 (ORL1) [1]
94 nM
In vitro
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
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]
Animal Research Animal Models Male ICR (CD-1) subjected to nociceptin-induced allodynia test or hot plate test, and Male SD rats subjected to formalin-induced paw-licking response
Dosages ~10 mg/kg
Administration Orally or injected i.v.

Chemical Information & Solubility

Molecular Weight 447.96 Formula

C26H25N3O2.HCl
CAS No. 244218-51-7 SDF Download JTC-801 SDF
Smiles CCC1=CC=C(C=C1)OCC2=CC=CC=C2C(=O)NC3=CC4=C(C=C(N=C4C=C3)C)N.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (200.91 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 31 mg/mL

Water : Insoluble


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In vivo
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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