纳洛酮可阻断内吗啡肽-1对豚鼠离体支气管速激肽能性收缩的抑制作用，但对内吗啡肽-2无此作用。
Naloxone blocks endomorphin-1 but not endomorphin-2 induced inhibition of tachykinergic contractions of guinea-pig isolated bronchus.
作者信息
Fischer A, Undem B J
机构信息
Institute for Anatomy & Cell Biology, Justus-Liebig-University, Giessen, Germany.
出版信息
Br J Pharmacol. 1999 Jun;127(3):605-8. doi: 10.1038/sj.bjp.0702630.
Abstract
The recently identified endogenous agonists on the mu-opioid-receptor (mu OR), endomorphin-1 (EM-1) and endomorphin-2 (EM-2), induce a concentration dependent inhibition of electrical field stimulation (EFS)-induced tachykinin-mediated contractions of the guinea-pig bronchus (ED50s < 10 nM for both compounds). Surprisingly, only endomorphin-1 effects could be blocked by naloxone (10 microM), whereas endomorphin-2 effects were not affected by specific antagonists for the mu-, kappa-, and delta-opioid-receptor.
摘要
最近在μ-阿片受体（μOR）上发现的内源性激动剂，内吗啡肽-1（EM-1）和内吗啡肽-2（EM-2），可诱导对电场刺激（EFS）引起的豚鼠支气管速激肽介导的收缩产生浓度依赖性抑制（两种化合物的半数有效剂量均<10 nM）。令人惊讶的是，只有内吗啡肽-1的作用可被纳洛酮（10 μM）阻断，而内吗啡肽-2的作用不受μ-、κ-和δ-阿片受体特异性拮抗剂的影响。
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