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Levorphanol

左啡諾
Mechanism of action:
Levorphanol 是一種鴉片類藥物(opioid),屬於嗎啡喃類(morphinan)衍生物。Levorphanol 能活化 μ-阿片受體(μ-opioid receptor),可抑制神經元的腺苷酸環化酶(adenylate cyclase),降低 cAMP 生成,抑制突觸前的電壓門控鈣離子通道(voltage-gated Ca²⁺ channel),阻止鈣離子內流,減少麩胺酸(glutamate)、P 物質(substance P) 等疼痛相關神經傳導物質的釋放;同時,活化突觸後的鉀離子通道(K⁺ channel),促進鉀離子外流,導致神經元超極化(hyperpolarization)。
Reference(s):
1. Allen RM et al. (2003). The competitive N-methyl-D-aspartate receptor antagonist (-)-6-phosphonomethyl-deca-hydroisoquinoline-3-carboxylic acid (LY235959) potentiates the antinociceptive effects of opioids that vary in efficacy at the mu-opioid receptor. J Pharmacol Exp Ther.
2. Prommer E et al. (2007). Levorphanol: the forgotten opioid. Support Care Cancer.
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