JMV 449 is a pseudopeptide analogue of neurotensin-(8-13). It is about 3 times more potent than neurotensin in binding to mouse brain membranes and in contracting the guinea-pig ileum. Nurotensin is localized in discrete populations of neurons in the central nervous system of mammals. Neurotensin acts as a neuromodulator and, in particular, as a modulator of dopamine transmission in the nigrostriatal and mesocorticolimbic systems. Furthermore, neurotensin exerts potent hypothermic and analgesic effects when injected in the central nervous system. Neurotensin is also present in the mammalian gut. It acts as a paracrine and endocrine modulator of digestive functions. In particuIar, neurotensin is a potent inhibitor of gastric acid secretion. In addition to these and other effects, neurotensin exerts numerous actions on the cardiovascular system of mammals including the induction of hypotension to which it owes its name.

JMV 449 is a potent neurotensin receptor agonist. It 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 has highly potent and long-lasting hypothermic and analgesic effects in the mouse.In this study, JMV 449 shows highly potent and long-lasting hypothermic and analgesic effects in the mouse.

In summary, JMV 449 is a potent neurotensin receptor agonist. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse. In addition, the pseudopeptide analogue behaves as a highly potent and long-lasting neurotensin agonist. In addition, the analogue should prove very useful for studying the effects of chronic neurotensin receptor stimulation in vitro and in vivo.

Reference:

Lugrin D, et al. Eur J Pharmacol. 1991;205(2):191-198.; Dubuc I, et al. Eur J Pharmacol. 1992;219(2):327-329.