Background:

Senktide is a tachykinin NK3 receptor agonist.

The selective NK3 receptor agonist Senktide excites 24 of 31 dopaminergic neurons in the substantia nigra pars compacta in a concentration-dependent manner. The effective concentration range is between 3 to 3000 nm. The mean EC50 for Senktide is 41.2±9 nm (n=5)[2].

I.c.v. injection of Senktide causes a dose-dependent increase in total distance traveled (F6,72=6.344, P<0.001). This increase reaches statistical significance compare to the vehicle-treated group at 0.06 nmol and higher. The Senktide-induced increase in locomotor activity brought about by 0.1 nmol of Senktide is significantly and dose-dependently decreased by the tachykinin NK3 receptor antagonists talnetant at 30 mg/kg and SB222200 at 30 mg/kg, but not by osanetant, when tested in parallel in a single experiment (F7,78=10.32, P<0.001), although a non-significant reduction is observed. However, when tested using another vehicle (Vitamin E and glycofurol), osanetant does decrease activity significantly compare to Senktide-treated gerbils (F2,30=10.10, P<0.001)[1].

参考文献:
[1]. Nordquist RE, et al. The tachykinin NK3 receptor agonist senktide induces locomotor activity in male Mongolian gerbils. Eur J Pharmacol. 2008 Dec 14;600(1-3):87-92.
[2]. Keegan KD, et al. The selective NK3 receptor agonist senktide excites a subpopulation of dopamine-sensitiveneurones in the rat substantia nigra pars compacta in vitro. Br J Pharmacol. 1992 Jan;105(1):3-5.