非肽类神经降压素拮抗剂SR 48692，用作揭示假定神经降压素受体亚型的工具。
The nonpeptide neurotensin antagonist, SR 48692, used as a tool to reveal putative neurotensin receptor subtypes.
作者信息
Dubuc I, Costentin J, Terranova J P, Barnouin M C, Soubrié P, Le Fur G, Rostène W, Kitabgi P
机构信息
Unité de Neuropsychopharmacologie Expérimentale, UA 1170 CNRS, Faculté de Médecine-Pharmacie de Rouen, St-Etienne du Rouvray, France.
出版信息
Br J Pharmacol. 1994 Jun;112(2):352-4. doi: 10.1111/j.1476-5381.1994.tb13077.x.
Abstract
The nonpeptide neurotensin (NT) antagonist, SR 48692, was recently shown to inhibit NT binding to the cloned rat and human NT receptor and to antagonize NT effects in a variety of in vitro and in vivo assays. Here, we show that, in contrast to its antagonistic action on NT-induced hypomotility in the rat, SR 48692 failed to antagonize NT-induced hypothermia and analgesia in the mouse and rat. We suggest that these effects might be mediated through a subtype of SR 48692-insensitive NT receptor.
摘要
非肽类神经降压素（NT）拮抗剂SR 48692最近被证明可抑制NT与克隆的大鼠和人类NT受体的结合，并在多种体外和体内试验中拮抗NT的作用。在此，我们表明，与它对大鼠NT诱导的运动减退的拮抗作用相反，SR 48692未能拮抗小鼠和大鼠中NT诱导的体温过低和镇痛作用。我们认为这些效应可能是通过一种对SR 48692不敏感的NT受体亚型介导的。
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