The Sound of Evolution
Pentazocine
噴他佐辛
Mechanism of action:
Pentazocine 是一種鴉片類藥物（opioid）。Pentazocine 主要能活化 κ-阿片受體（κ-opioid receptor），透過 Gi/o 蛋白偶聯抑制腺苷酸環化酶（adenylyl cyclase），降低 cAMP，抑制突觸前鈣離子內流，減少麩胺酸（glutamate）、P 物質（substance P）等疼痛相關神經傳導物質釋放，降低痛覺訊號傳遞；此外也活化突觸後的鉀離子通道（potassium channel），使神經元膜電位超極化（hyperpolarization）。Pentazocine 對於 μ-阿片受體（μ-opioid receptor）的作用較微弱。
Reference(s):
1. Chien CC et al. (1995). (-)-Pentazocine analgesia in mice: interactions with a sigma receptor system. Eur J Pharmacol.
2. Colabufo NA et al. (2009). In vitro and ex vivo characterization of sigma-1 and sigma-2 receptors: agonists and antagonists in biological assays. Cent Nerv Syst Agents Med Chem.
3. Dun Y et al. (2007). Prevention of excitotoxicity in primary retinal ganglion cells by (+)-pentazocine, a sigma receptor-1 specific ligand. Invest Ophthalmol Vis Sci.