opioid withdrawal

Dapiprazole Hydrochloride (Glamidolo Hydrochloride) 是 α-adrenergic 阻断剂的药物。

Mitraciliatine是一种在M. speciosa（泰国称为Kratom）中发现的生物碱，是μ-阿片受体（MOR）部分激动剂和κ-阿片受体（KOR）激动剂。该化合物对MOR和KOR具有选择性，与δ-阿片受体（DOR; EC50s分别为228, 218, 和 >1,000 nM，针对小鼠受体在GTPγS结合实验中的表现）。Mitraciliatine（100 nmol/动物，脑室内注射）在小鼠的热水尾部缩回实验中延长了撤回潜伏期，这一效果可以通过敲除MOR而非KOR来逆转。与吗啡不同，Mitraciliatine不会诱发过度活动或呼吸抑制。

UFP101是一种合成肽类物质，作为nociceptin受体的拮抗剂（Ki为0.06 nM，测试于表达人类受体的CHO细胞中）。它对nociceptin受体的选择性高于κ-opioid受体（Ki为204 nM，测试于表达大鼠受体的CHO细胞中）。UFP101能抑制表达于CHO细胞膜的nociceptin受体释放GTPγS（EC50为1.86 nM）。通过脑室内给药，UFP101（10 nmol/每只动物）能延长小鼠尾巴甩动试验中的尾巴撤回潜伏期。在由盲肠结扎和穿刺诱发的小鼠败血症模型中，UFP101（0.003、0.03及0.3 mg/kg）能提高生存率。

β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in mice with a median antinociceptive dose (AD50) of 1,500 pmol per animal. It inhibits antinociception induced by β-endorphin in mice in response to thermal stimuli when administered at a dose of 65 pmol per animal. In rats, β-endorphin (1-27) does not affect drug-associated place preference when administered at doses up to 20 μg, i.c.v., but inhibits β-endorphin-induced place preference when administered at a dose of 10 μg per animal.