Dubuc I, Pain C, Suaudeau C, Costentin J
European Institute for Peptide Research, Unité de Neuropsychopharmacologie Expérimentale U.R.A. 1170 du C.N.R.S., Faculté de Médecine et Pharmacie de Rouen, Saint Etienne du Rouvray, France.
Peptides. 1994;15(2):303-7. doi: 10.1016/0196-9781(94)90017-5.
The peptidase-resistant derivative of neurotensin, [D-Trp11]neurotensin, has been continuously infused intracerebroventricularly (75 ng/h) with an osmotic minipump for 10 days. On several days during this infusion the locomotor activity, the body temperature, the food intake, the body weight, and the nociceptive response in the plantar test were measured. A nonsignificant decrease of body temperature and a sustained analgesic effect were observed at each time considered. The response to a test dose of [D-Trp11]neurotensin (75 ng per rat) injected intracerebroventricularly at the 10th day of the chronic infusion revealed a complete tolerance to its hypothermic effect. Thus, it appears that the analgesic effect of [D-Trp11]neurotensin is independent of a hypothermic or an incapacitating effect of the peptide and does not give rise to tolerance after a 10-day continuous administration, in contrast to the hypothermic effect.
神经降压素的耐肽酶衍生物[D-色氨酸11]神经降压素，已通过渗透微型泵持续10天脑室内注射（75纳克/小时）。在注射期间的几天里，测量了自发活动、体温、食物摄入量、体重以及足底试验中的伤害性反应。在所考虑的每个时间点均观察到体温有不显著下降以及持续的镇痛作用。在慢性注射第10天，对脑室内注射的试验剂量[D-色氨酸11]神经降压素（每只大鼠75纳克）的反应显示对其降温作用完全耐受。因此，与降温作用相反，[D-色氨酸11]神经降压素的镇痛作用似乎与该肽的降温或失能作用无关，并且在连续给药10天后不会产生耐受性。
