JTC-801 displays about 12.5-, 129-, and 1055-fold selectivity for ORL1 receptor (Ki = 8.2 nM) over ¦Ì-, ¦Ê-, and ¦Ä-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 ¦Ì-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 ¦ÌM in HeLa cells expressing ORL1 receptor.

June 21, 2017

prudect name : JTC-801 displays about 12.5-, 129-, and 1055-fold selectivity for ORL1 receptor (Ki = 8.2 nM) over ¦Ì-, ¦Ê-, and ¦Ä-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 ¦Ì-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 ¦ÌM in HeLa cells expressing ORL1 receptor.
JTC 801

Synonyms: CAS NO: 244218-51-7Molecular Formula: C₂₆H₂₅N₃O₂.HClMolecular Weight: 447.96Purity: 98% minSolubility: In DMSOStorage: -20°C

PTC 124 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18520636