一种新型的孤啡肽受体选择性拮抗剂。
A new selective antagonist of the nociceptin receptor.
作者信息
Guerrini R, Calo G, Rizzi A, Bigoni R, Bianchi C, Salvadori S, Regoli D
机构信息
Department of Experimental and Clinical Medicine, University of Ferrara, Italy.
出版信息
Br J Pharmacol. 1998 Jan;123(2):163-5. doi: 10.1038/sj.bjp.0701640.
[Phe1psi(CH2-NH)Gly2]NC(1-13)NH2 has been tested in the electrically stimulated guinea pig ileum and mouse vas deferens, two nociceptin sensitive preparations. The new compound showed per se little or no effect in the two tissues, but it displaced to the right the concentration-response curves of nociceptin in a concentration-dependent manner. Schild analyses of the data indicated a competitive type of antagonism and pA2 values of 7.02 and 6.75 in the guinea-pig ileum and the mouse vas deferens, respectively. At 10 microM [Phe1psi(CH2-NH)Gly2]NC(1-13)NH2 does not modify either the inhibitory effect of deltorphin I (the selective delta opioid receptor agonist) in the mouse vas deferens or that of dermorphine (the selective mu opioid receptor agonist) in the guinea-pig ileum. The present findings indicate that [Phe1psi(CH2-NH)Gly2]NC(1-13)NH2 is a selective antagonist of the nociceptin receptor.
[苯丙氨酸 1ψ(CH₂-NH)甘氨酸 2]NC(1 - 13)NH₂已在电刺激的豚鼠回肠和小鼠输精管这两种对孤啡肽敏感的制剂中进行了测试。该新化合物本身在这两种组织中几乎没有或没有作用，但它以浓度依赖性方式使孤啡肽的浓度 - 反应曲线向右移动。对数据进行的希尔德分析表明存在竞争性拮抗作用，在豚鼠回肠和小鼠输精管中的 pA₂值分别为 7.02 和 6.75。在 10 μM 时，[苯丙氨酸 1ψ(CH₂-NH)甘氨酸 2]NC(1 - 13)NH₂既不改变小鼠输精管中 I 型强啡肽（选择性 δ 阿片受体激动剂）的抑制作用，也不改变豚鼠回肠中皮啡肽（选择性 μ 阿片受体激动剂）的抑制作用。目前的研究结果表明，[苯丙氨酸 1ψ(CH₂-NH)甘氨酸 2]NC(1 - 13)NH₂是孤啡肽受体的选择性拮抗剂。
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