JTC-801 HCl
| CAS No. | 244218-51-7 | Cat. No. | BCP02544 |
| Name | JTC-801 HCl | ||
| Synonyms | JTC-801 hydrochloride;JTC-801; JTC 801; JTC801; | ||
| Formula | C26H25N3O2.HCl | M. Wt | 447.96 |
| Description | 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.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. | ||
| Pathways | Neuro Signaling Pathway Hormone Pathay GPCR/G Protein | ||
| Targets | Opioid Receptor | ||
Structure
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