Van Kemmel F M, Dubuc I, Bourdel E, Fehrentz J A, Martinez J, Costentin J
Unité de Neuropsychopharmacologie expérimentale URA 1969-C.N.R.S., Faculté de Médecine, Saint Etienne du Rouvray, France.
Neurosci Lett. 1996 Oct 11;217(1):58-60. doi: 10.1016/0304-3940(96)13074-3.
A C-terminal cyclic 8-13 neurotensin fragment analog. JMV 1193, a direct agonist of central neurotensin receptors, is able to cross both the cerebrospinal fluid-brain barrier and the blood-brain barrier. When administered intracerebroventricularly (i.c.v.), its hypothermic effect was potentiated by the enkephalinase inhibition induced either by thiorphan (simultaneous intracerebroventricular administration of 10 micrograms) or by the thiorphan prodrug. acetorphan (intravenous (i.v.) administration of 10 mg/kg). Such a potentiation was not observed when both JMV 1193 and acetorphan were administered intravenously. Therefore it appears that the sensitivity of JMV 1193 to enkephalinase depends on its route of administration. It is exposed to this peptidase after i.c.v. injection (when crossing the cerebrospinal fluid-brain barrier), while it is not after i.v. administration (when crossing the blood-brain barrier).
一种C末端环状8 - 13神经降压素片段类似物。JMV 1193是中枢神经降压素受体的直接激动剂，能够穿越脑脊液 - 脑屏障和血 - 脑屏障。当脑室内给药时，其降温作用会因硫喷妥（同时脑室内给药10微克）或硫喷妥前体药物乙酰硫喷妥（静脉注射10毫克/千克）诱导的脑啡肽酶抑制作用而增强。当JMV 1193和乙酰硫喷妥均静脉给药时，未观察到这种增强作用。因此，似乎JMV 1193对脑啡肽酶的敏感性取决于其给药途径。脑室内注射后（穿越脑脊液 - 脑屏障时）它会接触到这种肽酶，而静脉给药后（穿越血 - 脑屏障时）则不会。
