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題 名 | The k-Opioid Receptor in Opioid Dependence=k-類鴉片受體於鴉片類藥物的依賴性所扮演的角色 |
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作 者 | Wongchanapai,Wichai; Tsang,Brian K.; Ho,Ing K.; | 書刊名 | 藥物食品分析 |
卷 期 | 7:1 1999.03[民88.03] |
頁 次 | 頁1-12 |
分類號 | 418.2132 |
關鍵詞 | k-類鴉片受體; 類鴉片藥物依賴性; 麩氨酸; 藍斑核; 脊髓; k-opioid receptor; Opioid dependence; Glutamate locus coeruleus; Spinal cord; |
語 文 | 英文(English) |
中文摘要 | 依賴性目前仍是臨床使用作用於u-類鴉片受體的鎮痛劑所主要關切的問題,因此 使用�� - 類鴉片受體的藥物以取代 u- 受體致效劑作為鎮痛劑的情形正逐漸成長中。 有些 研究報告指出慢性給予��-類鴉片受體致效劑, 如 U-50488H,U-69,593 及 butorphanol 也 能導致身體依賴性 / 脫癮症狀的產生, 而不論由全身或由脊髓給予 nor-binaltorphimine (一種高選擇性的�� - 類鴉片受體拮抗劑 ) 均可在依賴性的動物引起催癮現象, 更顯示不 論在腦或脊髓的�� - 類鴉片受體均在類鴉片藥物的依賴性 / 脫癮症狀上扮演了重要的角色 。 此外位於藍斑核 (locus coeruleus) 節前神經末端的�� - 類鴉片受體調控麩氨酸 (glutamate) 的釋放,可能與依賴性 / 脫癮症狀的表現有關。對�� - 類鴉片致效劑的身體 依賴性與脊髓及特殊腦區��類鴉片受體之減量和對拮抗劑敏感的狀態有關; 然而�� - 類鴉 片受體的改變可能無法完全解釋依賴性發生的機轉。 由最近�� - 類鴉片受體的選值 (clone) 成功及應用, 未來應該能闡明其在依賴性 / 脫癮發生的細胞生物機轉上與 u- 類 鴉片受體可能不同。 |
英文摘要 | Opioid dependence that particularly mediates through the u-opioid receptor remains a major concern of opioid analgesics. Drugs which interact with �� -opioid receptors are increasingly used as an alternative to u-agonist analgesic. Several studies have reported that chronic administration of �� -opioid agonists such as U-50488H, U-69,593, and butorphanol also results in development of physical dependence/withdrawal. In addition, the ability of a highly selective �� -opioid antagonist, nor-binaltorphimine, given systemically or spinally, to precipitate withdrawal behaviors in opioid-dependent animals further demonstrates that both supraspinal and spinal sites of �� -opioid receptors play an important role in opioid dependence/withdrawal. With regard to the role of glutamate in opioid dependence/withdrawal, the �� -opioid receptor located at the presynaptic nerve terminal within the locus coeruleus crucially regulates glutamate release during the expression of opioid withdrawal. Physical dependence on �� -opioid agonists is associated with the downregulation and antagonist-sensitive state of the �� -opioid receptor in the spinal cord and specific brain areas. However, alterations of the �� -opioid receptor may not completely explain the mechanisms of dependence development. With cloned �� -opioid receptors recently available, it could be elucidated that the cellular and biological mechanisms of �� -opioid receptors for the development of dependence/withdrawal may differ from those of u-opioid receptors. |
本系統中英文摘要資訊取自各篇刊載內容。