SR 48692对非洲爪蟾卵母细胞表达系统中神经降压素诱导的钙激活氯电流的影响：对左卡巴斯汀敏感的神经降压素受体具有激动剂样活性，对左卡巴斯汀不敏感的神经降压素受体无拮抗作用。

Effects of SR 48692 on neurotensin-induced calcium-activated chloride currents in the Xenopus oocyte expression system: agonist-like activity on the levocabastine-sensitive neurotensin receptor and absence of antagonist effect on the levocabastine insensitive neurotensin receptor.

作者信息

Botto J M, Guillemare E, Vincent J P, Mazella J

机构信息

Institut de Pharmacologie Moléculaire et Cellulaire, Centre National de la Recherche Scientifique, UPR 411, Université de Nice-Sophia Antipolis, Valbonne, France.

出版信息

Neurosci Lett. 1997 Feb 28;223(3):193-6. doi: 10.1016/s0304-3940(97)13437-1.

DOI:10.1016/s0304-3940(97)13437-1

PMID:9080465

Abstract

The effect of the drug SR 48692 on the Ca(2+)-activated Cl- current induced by neurotensin on Xenopus oocytes injected with cRNAs encoding rodent high and low affinity neurotensin receptors, was examined. In this receptor expression system, SR 48692 failed to antagonize electrophysiological measurement of neurotensin-evoked current via the rat high affinity neurotensin receptor, whereas its application onto oocytes expressing the mouse low affinity neurotensin receptor triggered an inward current, as well as neurotensin itself. However, no current activation was observed after application of the drug on oocytes expressing the rat high affinity neurotensin receptor. These observations in the oocyte expression system did not reflect typical antagonist properties of SR 48692 drug.

摘要

研究了药物SR 48692对由神经降压素诱导的、注射了编码啮齿动物高亲和力和低亲和力神经降压素受体的cRNAs的非洲爪蟾卵母细胞上Ca(2+)激活的Cl-电流的影响。在这个受体表达系统中，SR 48692未能通过大鼠高亲和力神经降压素受体拮抗神经降压素诱发电流的电生理测量，而将其应用于表达小鼠低亲和力神经降压素受体的卵母细胞时，会引发内向电流，神经降压素本身也会引发该电流。然而，将该药物应用于表达大鼠高亲和力神经降压素受体的卵母细胞后，未观察到电流激活。在卵母细胞表达系统中的这些观察结果并未反映出SR 48692药物的典型拮抗特性。