英文名稱 | BAN ORL 24 2HCl | BAN-ORL-24 2HCl |
---|---|
中文名稱 | BAN ORL 24 2HCl | BAN-ORL-24 2HCl |
CAS號 | 1401463-54-4 |
分子式 | C27H35N3O2·2HCl |
分子量 | 506.51 | 433.60 (free) |
外觀 | White to off-white powder |
儲存條件 | -20°C, protect from light, stored under nitrogen |
英文名稱 | BAN ORL 24 2HCl | BAN-ORL-24 2HCl |
---|---|
中文名稱 | BAN ORL 24 2HCl | BAN-ORL-24 2HCl |
CAS號 | 1401463-54-4 |
分子式 | C27H35N3O2·2HCl |
分子量 | 506.51 | 433.60 (free) |
外觀 | White to off-white powder |
儲存條件 | -20°C, protect from light, stored under nitrogen |
BAN ORL 24 is an antagonist of the nociceptin (NOP) receptor (Ki = 0.24 nM in a radioligand binding assay using CHO cell membranes expressing the human receptor). It is selective for NOP receptors over μ-, δ-, and κ-opioid receptors (Kis = 0.19, 0.34, and >1 μM, respectively). BAN ORL 24 reduces NOP-induced GTPγS binding (pA2 = 9.98) and calcium mobilization (KB = 0.93 nM) in CHO cells. It inhibits electrically induced twitches in isolated mouse and rat vas deferens, as well as isolated guinea pig ileum, when used at a concentration of 100 nM. BAN ORL 24 (10 mg/kg) reverses thermal and mechanical antinociceptive activities induced by the dual agonist of μ-opioid and NOP receptors BPR1M97 in mice.
https://doi.org/10.1016/j.neuropharm.2019.107678
PMID: 19445927 DOI: 10.1016/j.ejphar.2009.04.054