AZ3146/

溶解度:Unknown

储存条件:at -20℃ 2 years

生物活性

High affinity, selective NOP receptor antagonist (K_i = 8.2 nM). Displays approximately 12.5-, 129- and 1055-fold selectivity over human μ-, κ- and δ-opioid receptors respectively. Exhibits anti-nociceptive effects in acute pain models in vivo. Orally active.

参考文献

Shinkai et al (2000) 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J.Med.Chem 43 4667. PMID: 11101358.

Yamada et al (2002) Pharmacological profiles of a novel opioid receptor-like1 (ORL1) receptor antagonist, JTC-801. Br.J.Pharmacol. 135 323. PMID: 11815367.