Martin C A, Gully D, Naline E, Advenier C
Département de Pharmacologie, Faculté de Médecine Paris-Ouest, France.
Neuropeptides. 1994 Mar;26(3):159-66. doi: 10.1016/0143-4179(94)90125-2.
Guinea-pig main bronchi were stimulated transmurally in vitro by electrical field stimulation in the presence of indomethacin 10(-6) M, propranolol 10(-6) M and phosphoramidon 10(-5) M. Two contractile neurogenic responses were successively observed. The second noncholinergic contraction was concentration dependently inhibited or abolished by neurotensin whereas the first cholinergic contraction was only partially inhibited. SR 48692, a novel antagonist of neurotensin receptors, reduced the inhibition induced by neurotensin (pKB = 9.75) whereas levocabastine, an antagonist of low-affinity neurotensin receptors, did not significantly modify the inhibitory effects of neurotensin on both neurally-mediated contractions. These results demonstrate that neurotensin exerts an inhibitory effect on neurotransmission in guinea-pig airways. Furthermore, the present study shows that the newly developed neurotensin receptors antagonist, SR 48692, is a potent inhibitor of the neurotensin inhibitory effects on cholinergic and noncholinergic contractions induced by electrical field stimulation of the guinea-pig isolated main bronchus.
在含有10(-6)M消炎痛、10(-6)M普萘洛尔和10(-5)M磷酰胺的条件下,体外对豚鼠主支气管进行跨壁电场刺激。先后观察到两种收缩性神经源性反应。第二种非胆碱能收缩被神经降压素浓度依赖性地抑制或消除,而第一种胆碱能收缩仅被部分抑制。新型神经降压素受体拮抗剂SR 48692降低了神经降压素诱导的抑制作用(pKB = 9.75),而低亲和力神经降压素受体拮抗剂左卡巴斯汀并未显著改变神经降压素对两种神经介导收缩的抑制作用。这些结果表明,神经降压素对豚鼠气道的神经传递具有抑制作用。此外,本研究表明,新开发的神经降压素受体拮抗剂SR 48692是神经降压素对豚鼠离体主支气管电场刺激诱导的胆碱能和非胆碱能收缩抑制作用的有效抑制剂。