不同的受体位点调节阿片样激动和拮抗作用

来源 :国外医学.药学分册 | 被引量 : 0次 | 上传用户:zouwen111
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作者通过阿片激动剂和拮抗剂保护β-funaltrex-amine(β-FNA)对μ受体特异性不可逆拮抗作用的实验发现,它们的保护能力并不与其激动活性相关,而与拮抗活性密切相关,且呈明显的平行关系。又因为β-fuoxymorphamine(β-FOA)和β-FNA 在C_6位上都含有同样的亲电部位,但激动剂β-FOA 却无力保护β-FNA 诱发的不可逆拮抗作用。这些都提示,μ激动剂和拮抗剂在μ受体上存在各自的识别位点。 By opioid agonists and antagonists to protect the β-funaltrex-amine (β-FNA) μ receptors specific irreversible antagonistic experiments found that their protective ability is not related to their agonistic activity, but with the antagonistic activity is closely related, And showed a clear parallel relationship. Because β-FOA and β-FNA all contain the same electrophilic site in C 6, the agonist β-FOA is unable to protect β-FNA induced irreversible antagonism. These suggest that μ agonists and antagonists have their own recognition sites on the μ receptor.
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