| Description | Picenadol (LY 150720) is a racemic mixture of N-methyl-4-phenylpiperidine derivatives with agonist-antagonist opioid properties.Picenadol has central analgesic activity. |
| In vivo | 在松鼠猴进行的一项试验中，研究了Picenadol (LY150720) (0.3-3.0 mg/kg)、其激动剂异构体(dextro) LY136596 (0.3-1.7 mg/kg)以及吗啡 (0.03-1.0 mg/kg)单独使用及与纳洛酮 (0.001-1.0 mg/kg)联用下，对维持在多重固定比率30反应定时5分钟 (mult FR-30 FI 5-min)食物呈现计划反应的影响。LY150720、LY136596和吗啡通常降低了双计划部分下的响应，尽管在FI部分下的响应增加了好几次，特别是在使用LY150720和LY136596后。吗啡、LY150720及LY136596的降低响应效果可被纳洛酮逆转；逆转这三种化合物效果所需的纳洛酮剂量相似。纳洛酮与吗啡结合可以将响应速率和模式恢复至对照值，而LY150720或LY136596与纳洛酮的组合使得FI组分下的响应增加超过了对照值。这些增加似乎是由于LY150720和LY136596的抗胆碱作用所致，因为它们可以被毒扁豆碱 (0.01 mg/kg)逆转，而类似的增加也可由东莨菪碱 (0.01-0.1 mg/kg)产生。[1] |
| Synonyms | LY-150720, LY150720, LY 150720 |
| molecular weight | 247.38 |
| Molecular formula | C16H25NO |
| CAS | 2650427-35-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (222.33 mM) |
| References | 1. Carter RB, et al. Effects of LY150720 (picenadol), a novel mixed-action opioid, on schedule-controlled responding in the squirrel monkey. Pharmacol Biochem Behav. 1984 Nov;21(5):779-86. 2. Carter RB, et al. Effects of picenadol (LY150720) and its stereoisomers on electric shock titration in the squirrel monkey. J Pharmacol Exp Ther. 1985 Aug;234(2):299-306. |