JMV449acetate是一种有效的神经降压素受体(neurotensinreceptor)激动剂。JMV449acetate显示抑制125I-neurotensin与新生小鼠脑结合的IC50为0.15nM，对收缩豚鼠回肠的EC50为1.9nM。JMV449acetate对小鼠具有高效、持久的降温镇痛作用。
JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly potent and long-lasting hypothermic and analgesic effects in the mouse[1][2].
JMV 449 (120 pmol/mouse; i.c.v) shows analgesic effect[2]. Animal Model: Male Swiss albino mice[1]
[1]. Lugrin D, et al. Reduced peptide bond pseudopeptide analogues of neurotensin: binding and biological activities, and in vitro metabolic stability. Eur J Pharmacol. 1991;205(2):191-198. [2]. Dubuc I, et al. JMV 449: a pseudopeptide analogue of neurotensin-(8-13) with highly potent and long-lasting hypothermic and analgesic effects in the mouse. Eur J Pharmacol. 1992;219(2):327-329.
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